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Foretinib c-Met 저해제

Name: Foretinib
Brand: Selleck Chemicals
SKU: S1111
Rating: 5 (94 reviews)

제품 번호S1111

Foretinib은 HGFR 및 VEGFR의 ATP 경쟁적 저해제로, 주로 Met (c-Met) 및 KDR에 대해 세포 없는 분석에서 0.4 nM 및 0.9 nM의 IC50을 갖는다. Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β 및 Tie-2에 대해서는 덜 강력하며, FGFR1 및 EGFR에 대해서는 거의 활성이 없다. 2상.

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분자량: 632.65

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품질 관리

배치: 순도: 99.94%

99.94

관련 타겟	EGFR VEGFR PDGFR FGFR Src MEK CSF-1R FLT3 HER2 c-Kit
기타 c-Met 억제제	Tepotinib Dihexa SGX-523 PHA-665752 SU11274 BMS-777607 JNJ-38877605 Tivantinib PF-04217903 Savolitinib (AZD6094)

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
Daoy	Function Assay	0.5/1/2.5 μM	24 h	DMSO	inhibits the HGF-induced cMET pathway activation	25391241
ONS76	Function Assay	0.5/1/2.5 μM	24 h	DMSO	inhibits the HGF-induced cMET pathway activation	25391241
Daoy	Function Assay	0.5/1/2.5 μM	24 h	DMSO	inhibits HGF-mediated migration and invasion	25391241
ONS76	Function Assay	0.5/1/2.5 μM	24 h	DMSO	inhibits HGF-mediated migration and invasion	25391241
Daoy	Apoptosis Assay	1 μM	24 h	DMSO	induces apoptosis	25391241
Daoy	Growth Inhibition Assay	0.5/1/2.5 μM	24-96 h	DMSO	inhibits cell growth in a dose dependent manner	25391241
U251	Function Assay	100/300/900 nM	1 h	DMSO	inhibits the phosphorylation of MerTK	24658326
A172	Function Assay	100/300/900 nM	1 h	DMSO	inhibits the phosphorylation of MerTK	24658326
SF188	Function Assay	100/300/900 nM	1 h	DMSO	inhibits the phosphorylation of MerTK	24658326
U251	Function Assay	100/300/900 nM	1 h	DMSO	inhibits the activity of Axl, Tyro3	24658326
A172	Function Assay	100/300/900 nM	1 h	DMSO	inhibits the activity of Axl, Tyro3	24658326
SF188	Function Assay	100/300/900 nM	1 h	DMSO	inhibits the activity of Axl, Tyro3	24658326
U251	Function Assay	100/300/900 nM	1 h	DMSO	decreases Akt phosphorylation in a concentration dependent manner	24658326
A172	Function Assay	100/300/900 nM	1 h	DMSO	decreases Akt phosphorylation in a concentration dependent manner	24658326
SF188	Function Assay	100/300/900 nM	1 h	DMSO	decreases Akt phosphorylation in a concentration dependent manner	24658326
U251	Function Assay	100/300/900 nM	28 h	DMSO	induces PARP cleavage	24658326
SF188	Function Assay	100/300/900 nM	28 h	DMSO	induces PARP cleavage	24658326
SF188	Growth Inhibition Assay	100/300/900 nM	48 h	DMSO	reduces cell survival at 900 nM significantly	24658326
U251	Growth Inhibition Assay	100/300/900 nM	48 h	DMSO	reduces cell survival at 900 nM significantly	24658326
A172	Growth Inhibition Assay	100/300/900 nM	48 h	DMSO	reduces cell survival at 900 nM significantly	24658326
SF188	Function Assay	100/300/900 nM	24 h	DMSO	abrogates migration and invasion of glioma cells in a dose dependent manner	24658326
U251	Function Assay	100/300/900 nM	24 h	DMSO	abrogates migration and invasion of glioma cells in a dose dependent manner	24658326
A172	Function Assay	100/300/900 nM	24 h	DMSO	abrogates migration and invasion of glioma cells in a dose dependent manner	24658326
Ba/F3	Cell Viability Assay	0.0001-10 μM	72 h		inhibits cell growth in a dose dependent manner	24218589
HCC78	Cell Viability Assay	0.01-10 μM	72 h		inhibits cell growth in a dose dependent manner	24218589
SK-HEP1	Cell Viability Assay	0.25-1.5 μM	24 h		inhibits cell growth in a dose dependent manner	22187171
SK-HEP2	Function Assay	1 μM	24 h		blocks HGF-induced cell motility	22187171
SK-HEP2	Function Assay	1 μM	24 h		causes G2/M phase arrest with reduction in the G0/G1 and S phases	22187171
MKN-45	Growth Inhibition Assay	0.01-10 μM	5 d		IC50=8 nM	21655918
KATO-III	Growth Inhibition Assay	0.01-10 μM	5 d		IC50=30 nM	21655918
MKN-45	Function Assay	1 μM	24 h		inhibits phosphorylation of MET, Akt, and ERK1/2 in MKN-45	21655918
KATO-III	Function Assay	1 μM	24 h		inhibits phosphorylation of MET, Akt, and ERK1/2 in MKN-45	21655918
H1648	Growth Inhibition Assay				IC50=1.28 ±0.12 μM	21252284
H1573	Growth Inhibition Assay				IC50=1.62 ± 0.05 μM	21252284
H596	Growth Inhibition Assay				IC50=1.21 ± 0.17 μM	21252284
HOP92	Growth Inhibition Assay				IC50=0.81 ± 0.29 μM	21252284
H69	Growth Inhibition Assay				IC50=1.18 ± 0.08 μM	21252284
H1975	Growth Inhibition Assay				IC50=1.39 ± 0.33 μM	21252284
SCC15	Growth Inhibition Assay				IC50=0.63 ± 0.04 μM	21252284
HN5	Growth Inhibition Assay				IC50=0.65 ± 0.26 μM	21252284
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against c-Met-dependent human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.03 μM.	23628470
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against c-Met-dependent human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.08 μM.	23628470
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against c-Met-dependent human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.15 μM.	23628470
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against c-Met-independent human H460 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.18 μM.	23628470
SMMC7721	Cytotoxicity assay		72 hrs		Cytotoxicity against c-Met-dependent human SMMC7721 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.44 μM.	23628470
U87MG	Cytotoxicity assay		72 hrs		Cytotoxicity against c-Met-dependent human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.9 μM.	23628470
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.031 μM.	23644189
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.12 μM.	23644189
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.18 μM.	23644189
SMMC7721	Cytotoxicity assay		72 hrs		Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50 = 0.3 μM.	23644189
U87MG	Cytotoxicity assay		72 hrs		Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.04 μM.	23644189
MKN45	Cytotoxicity assay				Cytotoxicity against human MKN45 cells, IC50 = 0.008 μM.	23838381
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.023 μM.	23838381
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by DAPI staining-based fluorescence assay, IC50 = 0.029 μM.	23838381
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by DAPI staining-based fluorescence assay, IC50 = 0.165 μM.	23838381
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.17 μM.	23838381
NCI-H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.21 μM.	23838381
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	23838381
SMMC7721	Cytotoxicity assay		72 hrs		Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50 = 0.32 μM.	23838381
U87MG	Cytotoxicity assay		72 hrs		Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.47 μM.	23838381
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM.	24012712
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.11 μM.	24012712
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.19 μM.	24012712
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.21 μM.	24012712
U87MG	Cytotoxicity assay		72 hrs		Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.08 μM.	24012712
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM.	24485123
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.13 μM.	24485123
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.16 μM.	24485123
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.19 μM.	24485123
U87MG	Cytotoxicity assay		72 hrs		Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 1.1 μM.	24485123
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM.	24882675
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.19 μM.	24882675
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.21 μM.	24882675
MDA-MB-231	Cytotoxicity assay		72 hrs		Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 0.54 μM.	24882675
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.032 μM.	24996144
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.11 μM.	24996144
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.19 μM.	24996144
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.21 μM.	24996144
U87MG	Cytotoxicity assay		72 hrs		Cytotoxicity against human U87MG cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 1.08 μM.	24996144
MKN45	Antiproliferative assay		72 hrs		Antiproliferative activity against human MKN45 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.032 μM.	25282672
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.12 μM.	25282672
HT-29	Antiproliferative assay		72 hrs		Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.19 μM.	25282672
H460	Antiproliferative assay		72 hrs		Antiproliferative activity against human H460 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 0.21 μM.	25282672
U87MG	Antiproliferative assay		72 hrs		Antiproliferative activity against human U87MG cells assessed as inhibition of cell growth after 72 hrs by MTT assay, IC50 = 1.02 μM.	25282672
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.032 μM.	25438768
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.13 μM.	25438768
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.16 μM.	25438768
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.19 μM.	25438768
U87MG	Cytotoxicity assay		72 hrs		Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.92 μM.	25438768
BA/F3	Function assay				Inhibition of ROS1 (unknown origin) expressed in mouse BA/F3 cells, IC50 = 0.01 μM.	25461320
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.032 μM.	26169763
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.12 μM.	26169763
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.19 μM.	26169763
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.21 μM.	26169763
BT474	Function assay				Inhibition of AXL in lapatinib-sensitive human BT474 cells, IC50 = 0.1 μM.	26555154
PC3	Cytotoxicity assay		72 hrs		Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 0.39 μM.	26810712
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.64 μM.	26810712
MCF7	Cytotoxicity assay		72 hrs		Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 9.47 μM.	26810712
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.023 μM.	26897090
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.17 μM.	26897090
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	26897090
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 0.26 μM.	26923692
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 0.49 μM.	26923692
PC3	Cytotoxicity assay		72 hrs		Cytotoxicity against human PC3 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 0.89 μM.	26923692
MCF7	Cytotoxicity assay		72 hrs		Cytotoxicity against human MCF7 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50 = 6.25 μM.	26923692
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.032 μM.	26944614
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.13 μM.	26944614
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.16 μM.	26944614
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.19 μM.	26944614
U87MG	Cytotoxicity assay		72 hrs		Cytotoxicity against human U87MG cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 1.1 μM.	26944614
PC3	Cytotoxicity assay		72 hrs		Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 0.39 μM.	26964675
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.64 μM.	26964675
MCF7	Cytotoxicity assay		72 hrs		Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 9.47 μM.	26964675
BA/F3	Antiproliferative assay		72 hrs		Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay, IC50 = 0.0092 μM.	27068889
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells measured after 72 hrs by MTT assay, IC50 = 0.032 μM.	27155466
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells measured after 72 hrs by MTT assay, IC50 = 0.11 μM.	27155466
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells measured after 72 hrs by MTT assay, IC50 = 0.19 μM.	27155466
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells measured after 72 hrs by MTT assay, IC50 = 0.21 μM.	27155466
MKN45	Cytotoxicity assay				Cytotoxicity against human MKN45 cells, IC50 = 0.008 μM.	27187857
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.023 μM.	27187857
HT-29	Cytotoxicity assay				Cytotoxicity against human HT-29 cells, IC50 = 0.029 μM.	27187857
A549	Cytotoxicity assay				Cytotoxicity against human A549 cells, IC50 = 0.165 μM.	27187857
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.17 μM.	27187857
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	27187857
MDA-MB-231	Cytotoxicity assay		72 hrs		Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 0.54 μM.	27187857
Sf9	Function assay		60 mins		Inhibition of NH2-terminal His-tagged MET kinase domain (1051 to 1348 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells preincubated for 60 mins followed by (poly(Glu, Tyr) 4:1) substrate addition for 2 to 4 hrs by luciferase-c, IC50 = 0.0004 μM.	27299736
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against c-Met over-expressed human MKN45 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.032 μM.	27490023
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against c-Met over-expressed human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.14 μM.	27490023
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against c-Met over-expressed human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.19 μM.	27490023
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against c-Met over-expressed human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.21 μM.	27490023
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.15 μM.	28011202
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.25 μM.	28011202
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.32 μM.	28011202
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.25 μM.	28384549
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.29 μM.	28384549
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.36 μM.	28384549
U87MG	Cytotoxicity assay		72 hrs		Cytotoxicity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.96 μM.	28384549
MKN45	Antiproliferative assay		72 hrs		Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.03 μM.	28716639
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.15 μM.	28716639
HT-29	Antiproliferative assay		72 hrs		Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.21 μM.	28716639
H460	Antiproliferative assay		72 hrs		Antiproliferative activity against human H460 cells after 72 hrs by MTT assay, IC50 = 0.22 μM.	28716639
U87MG	Antiproliferative assay		72 hrs		Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.96 μM.	28716639
HCC827	Function assay				Displacement of [3H]-cyclopamine from SMO V404M mutant in gefitinib resistant human HCC827 cells by scintillation counting, Ki = 0.0668 μM.	28787156
HCC827	Antiproliferative assay	72 hrs			Antiproliferative activity against gefitinib resistant EGFR-mutated human HCC827 cells after 72 hrs by MTT assay, IC50 = 0.5 μM.	28787156
HCC827	Antitumor assay	15 mg/kg			Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 15 mg/kg/day, po	28787156
HCC827	Apoptosis assay	0.01 to 1 uM	72 hrs		Induction of apoptosis in gefitinib resistant human HCC827 cells at 0.01 to 1 uM after 72 hrs by annexin V-FITC-propidium iodide staining-based flow cytometry method relative to control	28787156
HCC827	Function assay	0.1 to 0.5 uM	72 hrs		Inhibition of MET phosphorylation at Tyr1234/1235 in gefitinib resistant human HCC827 cells at 0.1 to 0.5 uM after 72 hrs by Western blotting method	28787156
HCC827	Function assay	0.1 to 0.5 uM	72 hrs		Downregulation of SMO expression in gefitinib resistant human HCC827 cells at 0.1 to 0.5 uM after 72 hrs by Western blotting method	28787156
HCC827	Function assay	0.1 to 0.5 uM	72 hrs		Inhibition of MET in gefitinib resistant human HCC827 cells assessed as decrease in MAPK44/42 phosphorylation at Thr202/Tyr204 at 0.1 to 0.5 uM after 72 hrs by Western blotting method	28787156
HCC827	Function assay	0.1 to 0.5 uM	72 hrs		Inhibition of MET in gefitinib resistant human HCC827 cells assessed as decrease in AKT phosphorylation at Ser473 at 0.1 to 0.5 uM after 72 hrs by Western blotting method	28787156
HCC827	Function assay	0.1 to 0.5 uM	72 hrs		Inhibition of MET/SMO V404M mutant in gefitinib resistant human HCC827 cells assessed as decrease in vimentin expression at 0.1 to 0.5 uM after 72 hrs by Western blotting method	28787156
HCC827	Antitumor assay	20 mg/kg			Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 20 mg/kg/day, po	28787156
HCC827	Antitumor assay	20 mg/kg			Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 20 mg/kg/day, po in presence of gefitinib	28787156
HCC827	Antitumor assay	20 mg/kg			Antitumor activity against gefitinib resistant human HCC827 cells xenografted in balb/c athymic nu/nu mouse assessed as decrease in tumor size at 20 mg/kg/day, po in presence of osimertinib	28787156
PC3	Cytotoxicity assay		72 hrs		Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.48 μM.	29107421
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 1.74 μM.	29107421
HepG2	Cytotoxicity assay		72 hrs		Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.88 μM.	29107421
MCF7	Cytotoxicity assay		72 hrs		Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 3.92 μM.	29107421
HT-29	Antiproliferative assay		72 hrs		Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	29197731
NCI-H460	Antiproliferative assay		72 hrs		Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.28 μM.	29197731
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.32 μM.	29197731
U87MG	Antiproliferative assay		72 hrs		Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay, IC50 = 0.91 μM.	29197731
HepG2	Cytotoxicity assay		72 hrs		Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 2.27 μM.	29203143
MCF7	Cytotoxicity assay		72 hrs		Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 2.76 μM.	29203143
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 3.13 μM.	29203143
PC3	Antiproliferative assay		72 hrs		Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50 = 0.39 μM.	29331754
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.64 μM.	29331754
MCF7	Antiproliferative assay		72 hrs		Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 9.47 μM.	29331754
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh30	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 0.32 μM.	30216852
HepG2	Antiproliferative assay		72 hrs		Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 0.48 μM.	30216852
MCF7	Antiproliferative assay		72 hrs		Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.76 μM.	30216852
MKN45	Antiproliferative assay		72 hrs		Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.0023 μM.	30248654
EBC1	Antiproliferative assay		72 hrs		Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0048 μM.	30248654
SNU5	Antiproliferative assay		72 hrs		Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay, IC50 = 0.0089 μM.	30248654
BAF3	Function assay		72 hrs		Inhibition of TPR-tagged met (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.0092 μM.	30248654
NCI-H460	Antiproliferative assay		72 hrs		Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.0396 μM.	30248654
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity in human MKN45 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.041 μM.	31079967
NCI-H460	Cytotoxicity assay		72 hrs		Cytotoxicity in human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.18 μM.	31079967
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.22 μM.	31079967
MDA-MB-231	Cytotoxicity assay		72 hrs		Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.52 μM.	31079967
sf21	Function assay		60 mins		Inhibition of wild type N-terminal NH-tagged and avi-tagged dephosphorylated c-MET (956 to 1390 residues) (unknown origin) expressed in sf21 cells using poly (Glu,Tyr) as substrate measured after 60 mins by ADP-Glo kinase assay, IC50 = 0.002512 μM.	31531204
sf21	Function assay		60 mins		Inhibition of N-terminal NH-tagged and avi-tagged dephosphorylated c-MET D1228V mutant (956 to 1390 residues) (unknown origin) expressed in sf21 cells using poly (Glu,Tyr) as substrate measured after 60 mins by ADP-Glo kinase assay, IC50 = 0.002512 μM.	31531204
NCI-H1993	Growth inhibition assay		3 days		Growth inhibition of CRISPR/Cas9 modified human NCI-H1993 cells harboring cMET D1228V mutant incubated for 3 days by cell titer-glo luminescent cell viability assay, GI50 = 0.05248 μM.	31531204
NCI-H1993	Growth inhibition assay		3 days		Growth inhibition of wild type human NCI-H1993 cells incubated for 3 days by cell titer-glo luminescent cell viability assay, GI50 = 0.06166 μM.	31531204
NCI-H1993	Function assay		4 hrs		Inhibition of c-Met phosphorylation at Tyr 1234/Tyr1235 residues in human NCI-H1993 cells incubated for 4 hrs by HTRF assay, IC50 = 0.2138 μM.	31531204
NCI-H1993	Function assay		4 hrs		Inhibition of c-MET D1228V mutant phosphorylation at Tyr1234/Tyr1235 residues in CRISPR/Cas9 modified human NCI-H1993 cells incubated for 4 hrs by HTRF assay, IC50 = 0.2138 μM.	31531204
NCI-H1993	Function assay	1 uM	4 hrs		Inhibition of c-MET D1228V mutant in CRISPR/Cas9 modified human NCI-H1993 cells assessed as reduction in AKT phosphorylation at 1 uM after 4 hrs by Western blot analysis	31531204
NCI-H1993	Function assay	1 uM	4 hrs		Inhibition of c-Met phosphorylation in human NCI-H1993 cells at 1 uM after 4 hrs by Western blot analysis	31531204
NCI-1993	Function assay	1 uM	4 hrs		Inhibition of c-MET in human NCI-1993 cells assessed as reduction in AKT phosphorylation at 1 uM after 4 hrs by Western blot analysis	31531204
NCI-H1993	Function assay	1 uM	4 hrs		Inhibition of c-Met D1228V mutant phosphorylation in CRISPR/Cas9 modified human NCI-H1993 cells at 1 uM after 4 hrs by Western blot analysis	31531204
sf21	Function assay				Binding affinity to wild type N-terminal NH-tagged and avi-tagged dephosphorylated c-MET (956 to 1390 residues) (unknown origin) expressed in sf21 cells by SPR analysis	31531204
sf21	Function assay				Binding affinity to N-terminal NH-tagged and avi-tagged dephosphorylated c-MET D1228V mutant (956 to 1390 residues) (unknown origin) expressed in sf21 cells by SPR analysis	31531204
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.4 μM.	31546197
MCF7	Antiproliferative assay		72 hrs		Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.4 μM.	31546197
HepG2	Antiproliferative assay		72 hrs		Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.4 μM.	31546197
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 0.2 μM.	31629631
H460	Cytotoxicity assay		72 hrs		Cytotoxicity against human H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 1.14 μM.	31629631
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 1.49 μM.	31629631
HT-29	Cytotoxicity assay		72 hrs		Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 1.76 μM.	31629631
U87MG	Cytotoxicity assay		72 hrs		Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 2.17 μM.	31629631
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	632.65	화학식	C₃₄H₃₄F₂N₄O₆	보관 (수령일로부터)	3년-20°C분말
CAS 번호	849217-64-7	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	GSK1363089, EXEL-2880, XL-880, GSK089			Smiles	COC1=CC2=C(C=CN=C2C=C1OCCCN3CCOCC3)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F

용해도

In vitro
배치:

DMSO : 100 mg/mL (158.06 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (158.06 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 127 mg/mL (200.74 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (158.06 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (158.06 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	30.000mg/ml (47.42mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

Targets/IC₅₀/Ki	Met (Cell-free assay) 0.4 nM KDR (Cell-free assay) 0.86 nM Tie-2 (Cell-free assay) 1.1 nM VEGFR3/FLT4 (Cell-free assay) 2.8 nM RON (Cell-free assay) 3 nM FLT3 (Cell-free assay) 3.6 nM PDGFRα (Cell-free assay) 3.6 nM Kit (Cell-free assay) 6.7 nM VEGFR1/FLT1 (Cell-free assay) 6.8 nM PDGFRβ (Cell-free assay) 9.6 nM
시험관 내(In vitro)	XL880은 Met에 대해 0.4 nM, Ron에 대해 3 nM의 IC50 값으로 HGF 수용체 계열 Protein Tyrosine Kinases를 억제합니다. XL880은 또한 KDR, Flt-1 및 Flt-4를 각각 0.9 nM, 6.8 nM 및 2.8 nM의 IC50 값으로 억제합니다. XL880은 B16F10, A549 및 HT29 세포의 콜로니 성장을 각각 40 nM, 29 nM 및 165 nM의 IC50으로 억제합니다. 최근 연구에 따르면 XL880은 위암 세포주 MKN-45 및 KATO-III에서 세포 성장에 다르게 영향을 미칩니다. XL880은 MKN-45 세포에서 MET 및 하류 신호 전달 분자의 인산화를 억제하는 반면, KATO-III 세포에서는 GFGR2를 표적으로 합니다.
키나아제 분석	키나아제 억제 분석
키나아제 분석	키나아제 억제는 [³³P]인산 전이, 루시페라제 결합 화학발광 또는 AlphaScreen Protein Tyrosine Kinase 기술의 세 가지 분석 형식 중 하나를 사용하여 조사됩니다. IC50은 XLFit을 사용한 비선형 회귀 분석으로 계산됩니다. ³³P-인산 전이 키나아제 분석 반응은 384웰 흰색, 투명 바닥, 고결합 마이크로타이터 플레이트 (Greiner, Monroe, NC)에서 수행됩니다. 플레이트는 코팅 버퍼 50 μL 부피에 2 μg/웰의 단백질 또는 펩타이드 기질을 사용하여 코팅되었습니다. 코팅 버퍼는 40 μg/mL 기질 (poly(Glu, Tyr) 4:1, 22.5 mM Na2CO₃, 27.5 mM NaHCO₃, 50 mM NaCl 및 3 mM NaN₃를 포함합니다. 코팅된 플레이트는 실온(RT)에서 밤새 인큐베이션한 후 50 μL의 분석 버퍼로 한 번 세척됩니다. 테스트 화합물과 효소는 총 20 μL 부피로 ³³P-γ-ATP (3.3 μCi/nmol)와 결합됩니다. 반응 혼합물은 RT에서 2시간 동안 인큐베이션되고 흡인으로 종료됩니다. 마이크로타이터 플레이트는 이어서 0.05% Tween-PBS 버퍼 (PBST)로 6회 세척됩니다. 섬광액 (50 μL/웰)이 첨가되고 통합된 ³³P는 MicroBeta 섬광 카운터를 사용하여 액체 섬광 분광법으로 측정됩니다. 루시페라제 결합 화학발광 분석 반응은 384웰 흰색, 중간 결합 마이크로타이터 플레이트 (Greiner)에서 수행됩니다. 첫 번째 단계에서 효소와 화합물을 결합하고 60분 동안 인큐베이션합니다. 반응은 ATP 및 펩타이드 기질 (poly(Glu, Tyr) 4:1)을 최종 부피 20 μL로 첨가하여 시작되며, RT에서 2-4시간 동안 인큐베이션됩니다. 키나아제 반응 후, Kinase Glo (Promega, Madison, WI) 20 μL 분액을 첨가하고 Victor 플레이트 리더를 사용하여 발광 신호를 측정합니다. 총 ATP 소비는 50%로 제한됩니다. AlphaScreen™ Protein Tyrosine Kinase 분석 스트렙타비딘으로 코팅된 공여체 비드와 PY100 항인산화티로신 항체로 코팅된 수용체 비드가 사용됩니다. 비오틴화된 poly(Glu,Tyr) 4:1이 기질로 사용됩니다. 기질 인산화는 공여체-수용체 비드 복합체 형성 후 발광에 의한 공여체/수용체 비드 첨가로 측정됩니다. 키나아제와 테스트 화합물을 결합하고 60분 동안 사전 인큐베이션한 다음, ATP 및 비오틴화된 poly(Glu, Tyr)을 총 20 μL 부피로 384웰 흰색, 중간 결합 마이크로타이터 플레이트 (Greiner)에 첨가합니다. 반응 혼합물은 실온에서 1시간 동안 인큐베이션됩니다. 반응은 75 mM Hepes, pH 7.4, 300 mM NaCl, 120 mM EDTA, 0.3% BSA 및 0.03% Tween-20을 포함하는 15-30 μg/mL AlphaScreen 비드 현탁액 10 μL를 첨가하여 중단됩니다. 실온에서 2-16시간 인큐베이션한 후 AlphaQuest 리더를 사용하여 플레이트를 읽습니다.
생체 내(In vivo)	XL880 100 mg/kg 단회 경구 투여는 B16F10 종양 Met의 인산화와 간의 Met 및 폐의 Flk-1/KDR에서 리간드(예: HGF 또는 VEGF) 유도 수용체 인산화를 실질적으로 억제하며, 이 둘 모두 24시간 동안 지속됩니다. XL880(30-100 mg/kg, 1일 1회, 경구 투여) 치료는 종양 부담을 감소시킵니다. 폐 표면 종양 부담은 XL880 30 및 100 mg/kg 투여 후 각각 50% 및 58% 감소했습니다. B16F10 고형 종양을 가진 마우스에 대한 XL880 치료는 또한 30 및 100 mg/kg에서 각각 64% 및 87%의 용량 의존적 종양 성장 억제를 초래합니다. 두 연구 모두에서 XL880 투여는 유의미한 체중 감소 없이 잘 내약되었습니다. XL880은 Met을 통한 HGF의 비정상적인 신호 전달을 표적으로 하고 동시에 종양 혈관 신생에 관여하는 여러 수용체 Protein Tyrosine Kinase를 표적으로 하도록 개발되었습니다. XL880은 인간 이종이식에서 2-4시간 이내에 종양 출혈과 괴사를 유발했으며, 최대 종양 괴사는 96시간(5일간의 일일 투여 후)에 관찰되어 완전한 퇴행을 초래했습니다.
참조	[1] http://www.ncbi.nlm.nih.gov/pubmed?term=19808973%20 [2] https://pubmed.ncbi.nlm.nih.gov/21655918/ [3] https://pubmed.ncbi.nlm.nih.gov/20472683/

적용 분야

방법	바이오마커	이미지	PMID
Western blot	pROS1 / tROS1 / pSHP2 / pERK / ERK p-MDM2 / p53 / PUMA p-Met / Met / p-Akt / Akt		24218589
Growth inhibition assay	Cell viability		29854314

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT00920192	Completed	Carcinoma Hepatocellular	GlaxoSmithKline	August 12 2009	Phase 1
NCT00742261	Completed	Solid Tumours	GlaxoSmithKline	August 11 2008	Phase 1
NCT00725764	Completed	Neoplasms Head and Neck	GlaxoSmithKline	August 27 2007	Phase 2
NCT00725712	Completed	Neoplasms Gastrointestinal Tract	GlaxoSmithKline	March 31 2007	Phase 2
NCT00743067	Completed	Solid Tumours	GlaxoSmithKline	August 9 2006	Phase 1

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