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Nilotinib (AMN-107) Bcr-Abl 억제제

Name: Nilotinib (AMN-107)
Brand: Selleck Chemicals
SKU: S1033
Rating: 5 (154 reviews)

제품 번호S1033

Nilotinib은 생쥐 골수 전구 세포에서 IC50이 30 nM 미만인 선택적 Bcr-Abl 억제제입니다. Nilotinib은 AMPK 활성화를 통해 Autophagy를 유도합니다.

Nilotinib (AMN-107) Bcr-Abl 억제제 Chemical Structure

화학 구조

분자량: 529.52

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품질 관리

배치: 순도: 99.97%

99.97

관련 타겟	EGFR VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2
기타 Bcr-Abl 억제제	Degrasyn (WP1130) Bafetinib Rebastinib (DCC-2036) GNF-5 GNF-2 Berbamine Olverembatinib (GZD824) dimesylate PD173955 GNF-7 Radotinib

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
EoL-1-cell	Growth Inhibition Assay			IC50=0.000144 μM	SANGER
KU812	Growth Inhibition Assay			IC50=0.00248 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=0.0041 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=0.0049 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=0.00828 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=0.01089 μM	SANGER
KASUMI-1	Growth Inhibition Assay			IC50=0.02413 μM	SANGER
NB7	Growth Inhibition Assay			IC50=0.13439 μM	SANGER
BHT-101	Growth Inhibition Assay			IC50=0.64263 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=0.6487 μM	SANGER
HMV-II	Growth Inhibition Assay			IC50=0.74874 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=0.9015 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=1.02228 μM	SANGER
NCI-H1703	Growth Inhibition Assay			IC50=1.1887 μM	SANGER
BE-13	Growth Inhibition Assay			IC50=1.27416 μM	SANGER
ACN	Growth Inhibition Assay			IC50=1.55077 μM	SANGER
A204	Growth Inhibition Assay			IC50=1.57205 μM	SANGER
HOP-62	Growth Inhibition Assay			IC50=1.82077 μM	SANGER
H9	Growth Inhibition Assay			IC50=2.73793 μM	SANGER
HCC1806	Growth Inhibition Assay			IC50=2.74327 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=2.87102 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=2.90623 μM	SANGER
JAR	Growth Inhibition Assay			IC50=2.92084 μM	SANGER
T98G	Growth Inhibition Assay			IC50=3.01313 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay			IC50=3.40092 μM	SANGER
SK-MEL-1	Growth Inhibition Assay			IC50=3.43029 μM	SANGER
L-363	Growth Inhibition Assay			IC50=3.61107 μM	SANGER
SW982	Growth Inhibition Assay			IC50=3.64169 μM	SANGER
HT-1080	Growth Inhibition Assay			IC50=3.91775 μM	SANGER
G-402	Growth Inhibition Assay			IC50=4.31203 μM	SANGER
HOS	Growth Inhibition Assay			IC50=4.80282 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=4.83191 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=4.88242 μM	SANGER
SBC-1	Growth Inhibition Assay			IC50=4.90907 μM	SANGER
CTV-1	Growth Inhibition Assay			IC50=5.48938 μM	SANGER
LCLC-103H	Growth Inhibition Assay			IC50=5.77471 μM	SANGER
RVH-421	Growth Inhibition Assay			IC50=5.77536 μM	SANGER
K-562	Growth Inhibition Assay			IC50=5.9036 μM	SANGER
CAL-33	Growth Inhibition Assay			IC50=6.31359 μM	SANGER
MDA-MB-361	Growth Inhibition Assay			IC50=6.33699 μM	SANGER
IGROV-1	Growth Inhibition Assay			IC50=6.47191 μM	SANGER
NY	Growth Inhibition Assay			IC50=6.53599 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=6.66931 μM	SANGER
HuO9	Growth Inhibition Assay			IC50=6.73964 μM	SANGER
MS-1	Growth Inhibition Assay			IC50=7.11953 μM	SANGER
RPMI-8226	Growth Inhibition Assay			IC50=7.28287 μM	SANGER
HDLM-2	Growth Inhibition Assay			IC50=7.40149 μM	SANGER
D-566MG	Growth Inhibition Assay			IC50=7.47155 μM	SANGER
SK-MEL-24	Growth Inhibition Assay			IC50=7.63392 μM	SANGER
COLO-679	Growth Inhibition Assay			IC50=7.98671 μM	SANGER
EW-13	Growth Inhibition Assay			IC50=8.32054 μM	SANGER
A388	Growth Inhibition Assay			IC50=8.38481 μM	SANGER
UM-UC-3	Growth Inhibition Assay			IC50=8.43956 μM	SANGER
NUGC-3	Growth Inhibition Assay			IC50=8.53582 μM	SANGER
COLO-668	Growth Inhibition Assay			IC50=8.59491 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=8.62353 μM	SANGER
D-423MG	Growth Inhibition Assay			IC50=8.83756 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=8.87128 μM	SANGER
BCPAP	Growth Inhibition Assay			IC50=9.02562 μM	SANGER
GCT	Growth Inhibition Assay			IC50=9.09831 μM	SANGER
ACHN	Growth Inhibition Assay			IC50=9.23632 μM	SANGER
KYSE-520	Growth Inhibition Assay			IC50=9.33482 μM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=9.76497 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=10.0132 μM	SANGER
HEC-1	Growth Inhibition Assay			IC50=10.2804 μM	SANGER
HL-60	Growth Inhibition Assay			IC50=10.6853 μM	SANGER
A101D	Growth Inhibition Assay			IC50=10.8923 μM	SANGER
A2058	Growth Inhibition Assay			IC50=10.9245 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=11.0635 μM	SANGER
697	Growth Inhibition Assay			IC50=11.2101 μM	SANGER
NCI-N87	Growth Inhibition Assay			IC50=11.7731 μM	SANGER
DSH1	Growth Inhibition Assay			IC50=11.7953 μM	SANGER
HLE	Growth Inhibition Assay			IC50=11.8839 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=12.6801 μM	SANGER
EW-3	Growth Inhibition Assay			IC50=12.9307 μM	SANGER
AGS	Growth Inhibition Assay			IC50=13.0351 μM	SANGER
ES5	Growth Inhibition Assay			IC50=13.0512 μM	SANGER
DB	Growth Inhibition Assay			IC50=13.3256 μM	SANGER
A4-Fuk	Growth Inhibition Assay			IC50=13.4102 μM	SANGER
A427	Growth Inhibition Assay			IC50=13.4972 μM	SANGER
MN-60	Growth Inhibition Assay			IC50=13.5843 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=13.5856 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=13.8137 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=14.1184 μM	SANGER
JVM-3	Growth Inhibition Assay			IC50=14.2656 μM	SANGER
NCI-H2029	Growth Inhibition Assay			IC50=14.2727 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=14.6046 μM	SANGER
WM-115	Growth Inhibition Assay			IC50=15.5683 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=16.0241 μM	SANGER
NCI-H1693	Growth Inhibition Assay			IC50=16.3802 μM	SANGER
KARPAS-299	Growth Inhibition Assay			IC50=16.6203 μM	SANGER
UACC-257	Growth Inhibition Assay			IC50=17.0582 μM	SANGER
RKO	Growth Inhibition Assay			IC50=17.6433 μM	SANGER
HT-29	Growth Inhibition Assay			IC50=17.7889 μM	SANGER
ES7	Growth Inhibition Assay			IC50=18.1122 μM	SANGER
DEL	Growth Inhibition Assay			IC50=18.3172 μM	SANGER
BT-549	Growth Inhibition Assay			IC50=18.4092 μM	SANGER
NCI-H1755	Growth Inhibition Assay			IC50=18.5723 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=18.8341 μM	SANGER
LU-139	Growth Inhibition Assay			IC50=19.0458 μM	SANGER
ECC10	Growth Inhibition Assay			IC50=19.2475 μM	SANGER
769-P	Growth Inhibition Assay			IC50=19.6335 μM	SANGER
BALL-1	Growth Inhibition Assay			IC50=19.6775 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=19.8979 μM	SANGER
TYK-nu	Growth Inhibition Assay			IC50=19.9315 μM	SANGER
NCI-H630	Growth Inhibition Assay			IC50=19.9378 μM	SANGER
EW-18	Growth Inhibition Assay			IC50=20.3802 μM	SANGER
KYSE-150	Growth Inhibition Assay			IC50=20.7047 μM	SANGER
LOXIMVI	Growth Inhibition Assay			IC50=20.7586 μM	SANGER
HuP-T3	Growth Inhibition Assay			IC50=21.0852 μM	SANGER
MFE-280	Growth Inhibition Assay			IC50=21.5679 μM	SANGER
SK-OV-3	Growth Inhibition Assay			IC50=21.8408 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=22.0478 μM	SANGER
NCI-H69	Growth Inhibition Assay			IC50=22.4299 μM	SANGER
TE-5	Growth Inhibition Assay			IC50=22.4965 μM	SANGER
NCI-H1993	Growth Inhibition Assay			IC50=22.4971 μM	SANGER
NCI-H1092	Growth Inhibition Assay			IC50=23.2843 μM	SANGER
RH-1	Growth Inhibition Assay			IC50=23.5357 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay			IC50=23.8472 μM	SANGER
Mo-T	Growth Inhibition Assay			IC50=23.9 μM	SANGER
HD-MY-Z	Growth Inhibition Assay			IC50=24.2362 μM	SANGER
NCI-H2342	Growth Inhibition Assay			IC50=24.6767 μM	SANGER
C32	Growth Inhibition Assay			IC50=24.9576 μM	SANGER
HTC-C3	Growth Inhibition Assay			IC50=25.3577 μM	SANGER
NCI-H358	Growth Inhibition Assay			IC50=25.3943 μM	SANGER
CAL-85-1	Growth Inhibition Assay			IC50=25.4577 μM	SANGER
HT-1197	Growth Inhibition Assay			IC50=25.5319 μM	SANGER
A172	Growth Inhibition Assay			IC50=25.7136 μM	SANGER
SW1573	Growth Inhibition Assay			IC50=25.7785 μM	SANGER
EW-24	Growth Inhibition Assay			IC50=25.962 μM	SANGER
SK-MEL-2	Growth Inhibition Assay			IC50=26.0312 μM	SANGER
LU-65	Growth Inhibition Assay			IC50=26.0452 μM	SANGER
KMOE-2	Growth Inhibition Assay			IC50=26.0915 μM	SANGER
H-EMC-SS	Growth Inhibition Assay			IC50=26.4114 μM	SANGER
H4	Growth Inhibition Assay			IC50=26.4243 μM	SANGER
DU-4475	Growth Inhibition Assay			IC50=27.1872 μM	SANGER
HCT-116	Growth Inhibition Assay			IC50=27.4349 μM	SANGER
MSTO-211H	Growth Inhibition Assay			IC50=27.6255 μM	SANGER
NCI-H292	Growth Inhibition Assay			IC50=27.9617 μM	SANGER
NCI-H446	Growth Inhibition Assay			IC50=28.2105 μM	SANGER
NCI-H2009	Growth Inhibition Assay			IC50=29.1431 μM	SANGER
MHH-ES-1	Growth Inhibition Assay			IC50=29.3685 μM	SANGER
TI-73	Growth Inhibition Assay			IC50=29.4001 μM	SANGER
NCI-H2228	Growth Inhibition Assay			IC50=29.458 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=29.5505 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay			IC50=29.6097 μM	SANGER
KY821	Growth Inhibition Assay			IC50=29.6433 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=29.8366 μM	SANGER
NBsusSR	Growth Inhibition Assay			IC50=29.9904 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=30.5716 μM	SANGER
NB14	Growth Inhibition Assay			IC50=31.0446 μM	SANGER
HCC1419	Growth Inhibition Assay			IC50=31.24 μM	SANGER
KG-1	Growth Inhibition Assay			IC50=31.7429 μM	SANGER
A2780	Growth Inhibition Assay			IC50=31.8358 μM	SANGER
NCI-H28	Growth Inhibition Assay			IC50=31.9861 μM	SANGER
C2BBe1	Growth Inhibition Assay			IC50=32.2634 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay			IC50=32.31 μM	SANGER
SBC-5	Growth Inhibition Assay			IC50=32.8511 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=33.4848 μM	SANGER
COR-L88	Growth Inhibition Assay			IC50=34.0741 μM	SANGER
SW954	Growth Inhibition Assay			IC50=34.0752 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=34.3404 μM	SANGER
HCC70	Growth Inhibition Assay			IC50=34.9514 μM	SANGER
NCI-H1770	Growth Inhibition Assay			IC50=34.961 μM	SANGER
NCI-H1666	Growth Inhibition Assay			IC50=35.8253 μM	SANGER
YH-13	Growth Inhibition Assay			IC50=35.92 μM	SANGER
DJM-1	Growth Inhibition Assay			IC50=36.8049 μM	SANGER
KNS-62	Growth Inhibition Assay			IC50=36.9438 μM	SANGER
SK-MEL-30	Growth Inhibition Assay			IC50=37.8737 μM	SANGER
SJRH30	Growth Inhibition Assay			IC50=38.7341 μM	SANGER
GP5d	Growth Inhibition Assay			IC50=38.8653 μM	SANGER
SW1116	Growth Inhibition Assay			IC50=39.2805 μM	SANGER
COLO-800	Growth Inhibition Assay			IC50=39.3638 μM	SANGER
RD	Growth Inhibition Assay			IC50=39.5258 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay			IC50=39.6916 μM	SANGER
HuO-3N1	Growth Inhibition Assay			IC50=40.108 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=40.5674 μM	SANGER
SK-MEL-3	Growth Inhibition Assay			IC50=40.5932 μM	SANGER
SK-MEL-28	Growth Inhibition Assay			IC50=40.6435 μM	SANGER
SCC-4	Growth Inhibition Assay			IC50=41.2137 μM	SANGER
no-11	Growth Inhibition Assay			IC50=41.7354 μM	SANGER
HT-144	Growth Inhibition Assay			IC50=42.0567 μM	SANGER
MFM-223	Growth Inhibition Assay			IC50=42.402 μM	SANGER
ONS-76	Growth Inhibition Assay			IC50=42.8018 μM	SANGER
ES8	Growth Inhibition Assay			IC50=43.3698 μM	SANGER
T-24	Growth Inhibition Assay			IC50=43.4369 μM	SANGER
GAMG	Growth Inhibition Assay			IC50=43.4517 μM	SANGER
LU-135	Growth Inhibition Assay			IC50=44.0923 μM	SANGER
HCC1187	Growth Inhibition Assay			IC50=44.8262 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=45.1654 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay			IC50=45.4315 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=45.8952 μM	SANGER
D-392MG	Growth Inhibition Assay			IC50=45.9256 μM	SANGER
KALS-1	Growth Inhibition Assay			IC50=46.7257 μM	SANGER
MMAC-SF	Growth Inhibition Assay			IC50=46.9952 μM	SANGER
HSC-3	Growth Inhibition Assay			IC50=47.3608 μM	SANGER
KM-H2	Growth Inhibition Assay			IC50=47.6007 μM	SANGER
LoVo	Growth Inhibition Assay			IC50=48.1002 μM	SANGER
NCI-H510A	Growth Inhibition Assay			IC50=48.1871 μM	SANGER
EW-11	Growth Inhibition Assay			IC50=48.2348 μM	SANGER
HCC2998	Growth Inhibition Assay			IC50=48.6236 μM	SANGER
J82	Growth Inhibition Assay			IC50=48.7242 μM	SANGER
ML-2	Growth Inhibition Assay			IC50=49.4605 μM	SANGER
NCI-H2030	Growth Inhibition Assay			IC50=49.7117 μM	SANGER
NCI-H1792	Growth Inhibition Assay			IC50=49.8518 μM	SANGER
KU812	Antiproliferative assay		72 hrs	Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.001 μM.	26789553
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay, IC50 = 0.00154 μM.	23088644
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.002 μM.	26789553
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.003 μM.	23301703
KU812	Antiproliferative assay			Antiproliferative activity against human KU812 cells, IC50 = 0.0034 μM.	21376587
Ba/F3	Function assay		48 hrs	Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00352 μM.	30137981
HEK293	Function assay			Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA, IC50 = 0.0037 μM.	20817538
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00371 μM.	30137981
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0039 μM.	26814890
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.004 μM.	26789553
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00482 μM.	30137981
HEK293	Function assay			Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA, IC50 = 0.0052 μM.	20817538
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay, IC50 = 0.00634 μM.	23088644
K562	Antiproliferative assay			Antiproliferative activity against human K562 cells, IC50 = 0.0065 μM.	21376587
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay, IC50 = 0.00838 μM.	23088644
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.00921 μM.	30137981
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.0095 μM.	23301703
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay, IC50 = 0.0103 μM.	23088644
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0128 μM.	23301703
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, IC50 = 0.015 μM.	23521020
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0158 μM.	23301703
MEG01	Antiproliferative assay		72 hrs	Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.016 μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.017 μM.	26789553
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0189 μM.	30137981
Ba/F	Function assay			Inhibition of autophosphorylation of BCR-ABL1 expressed in Ba/F cells, IC50 = 0.02 μM.	20817538
K562	Antiproliferative assay			Antiproliferative activity against human K562 cells, IC50 = 0.021 μM.	20817538
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay, IC50 = 0.021 μM.	23088644
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.021 μM.	26789553
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.022 μM.	23301703
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50 = 0.022 μM.	26195136
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.023 μM.	26789553
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0242 μM.	23301703
BA/F3	Antiproliferative assay			Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells, IC50 = 0.025 μM.	20817538
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.025 μM.	26789553
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0278 μM.	23301703
K562	Function assay		30 mins	Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 0.028 μM.	28280261
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0296 μM.	30137981
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0299 μM.	23301703
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0369 μM.	30137981
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay, IC50 = 0.0386 μM.	23088644
K562	Function assay			Inhibition of BCR-ABL1 autophosphorylation in human K562 cells, IC50 = 0.042 μM.	20817538
insect cells	Function assay		30 mins	Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay, IC50 = 0.0435 μM.	23301703
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.0546 μM.	26789553
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay, IC50 = 0.0607 μM.	23088644
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.0616 μM.	30137981
BA/F3	Antiproliferative assay			Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells, IC50 = 0.062 μM.	20817538
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay, IC50 = 0.0652 μM.	23088644
A31	Function assay			Inhibition of human PDGFRalpha autophosphorylation in human A31 cells by ELISA, IC50 = 0.071 μM.	20817538
A31	Function assay			Inhibition of PDGFRbeta autophosphorylation in human A31 cells by ELISA, IC50 = 0.071 μM.	20817538
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay, IC50 = 0.0872 μM.	23088644
K562	Function assay		30 mins	Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 0.1 μM.	28280261
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.12 μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.12 μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.13 μM.	23301703
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.132 μM.	30137981
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay, IC50 = 0.15 μM.	23088644
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.15 μM.	23301703
GIST882	Antiproliferative assay			Antiproliferative activity against human GIST882 cells, IC50 = 0.151 μM.	20817538
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay, IC50 = 0.159 μM.	23088644
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.16 μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 0.17 μM.	23301703
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.202 μM.	26789553
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.2153 μM.	23301703
GIST882	Function assay			Inhibition of human KIT autophosphorylation in human GIST882 cells by ELISA, IC50 = 0.217 μM.	20817538
K562	Antiproliferative assay			Antiproliferative activity against human imatinib-resistant K562 cells, IC50 = 0.26 μM.	21376587
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay, IC50 = 0.292 μM.	23088644
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay, IC50 = 0.314 μM.	23088644
BA/F3	Function assay		72 hrs	Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.47 μM.	26789553
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay, IC50 = 0.473 μM.	23088644
HEK293	Function assay			Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA, IC50 = 0.677 μM.	20817538
insect cells	Function assay		30 mins	Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay, IC50 = 0.7024 μM.	23301703
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay, IC50 = 0.775 μM.	23088644
M-NFS-60	Antiproliferative assay			Antiproliferative activity against mouse M-NFS-60 cells, IC50 = 0.838 μM.	20817538
BA/F3	Function assay		72 hrs	Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 0.87 μM.	26789553
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1 μM.	23301703
BA/F3	Function assay		72 hrs	Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.093 μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.1 μM.	26789553
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1.2 μM.	23301703
BA/F3	Function assay		72 hrs	Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.3 μM.	26789553
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 1.4 μM.	23301703
BA/F3	Function assay		72 hrs	Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 1.4 μM.	26789553
NCI-H2286	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay, IC50 = 1.8 μM.	26191369
K562	Function assay		30 mins	Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method, IC50 = 1.8 μM.	28280261
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 2.1 μM.	26789553
Ba/F3	Function assay		48 hrs	Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 2.262 μM.	30137981
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2.39 μM.	23521020
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against apoptosis-resistant, Philadelphia chromosome-positive human K562 cells after 72 hrs by PrestoBlue colorimetric assay, IC50 = 2.4 μM.	24835982
MDA-MB-435S	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay, IC50 = 2.66 μM.	23521020
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay, IC50 = 2.7 μM.	26814890
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 2.9 μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 3 μM.	23301703
NCI-H23	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay, IC50 = 3.05 μM.	23521020
HEL	Antiproliferative assay		72 hrs	Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 3.9 μM.	26789553
BA/F3	Function assay		72 hrs	Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 4.1 μM.	26789553
CHL	Antiproliferative assay		72 hrs	Antiproliferative activity against human CHL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay, GI50 = 4.2 μM.	26789553
CHO	Function assay			Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits, IC50 = 4.7 μM.	23812503
T47D	Antiproliferative assay		72 hrs	Antiproliferative activity against human T47D cells after 72 hrs by MTT assay, IC50 = 6.08 μM.	23521020
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 6.63 μM.	23521020
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 6.92 μM.	23521020
BJ	Antiproliferative assay		72 hrs	Antiproliferative activity against human BJ cells after 72 hrs by PrestoBlue colorimetric assay, IC50 = 12.8 μM.	24835982
NCI-H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 14.41 μM.	23521020
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 15.1 μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 16 μM.	23301703
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay, IC50 = 21.1 μM.	23301703
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay, IC50 = 40.75 μM.	23088644
BA/F3	Antitumor assay	75 mg/kg	19 days	Antitumor activity against mouse BA/F3 cells expressing wild type Bcr-Abl xenografted in CB17 SCID mouse assessed as median survival time at 75 mg/kg, po administered on day 3 once daily for 19 days relative to control	19572547
BA/F3	Antitumor assay	75 mg/kg	19 days	Antitumor activity against mouse BA/F3 cells expressing wild type Bcr-Abl xenografted in CB17 SCID mouse assessed as increase in mouse survival at 75 mg/kg, po administered on day 3 once daily for 19 days relative to control	19572547
vascular smooth muscle cells	Antiangiogenic assay	0.15 uM	72 hrs	Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of cell growth at 0.15 uM after 72 hrs	22853993
vascular smooth muscle cells	Antiangiogenic assay	10 to 15 uM	72 hrs	Antiangiogenic activity in HUVEC co-cultured with vascular smooth muscle cells assessed as inhibition of network formation at 10 to 15 uM after 72 hrs	22853993
HEK293	Function assay	0.1 to 1 uM	16 hrs	Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting	26191369
HEK293	Function assay	0.1 to 1 uM	16 hrs	Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting	26191369
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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
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
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 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
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	529.52	화학식	C₂₈H₂₂F₃N₇O	보관 (수령일로부터)	3년-20°C분말
CAS 번호	641571-10-0	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	AMN-107			Smiles	CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5

용해도

In vitro
배치:

DMSO : 52 mg/mL (98.2 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 35 mg/mL (66.09 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 50 mg/mL (94.42 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 27 mg/mL (50.98 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 13 mg/mL (24.55 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.
Clear solution	2%DMSO 1 40%PEG300 2 5%Tween80 3 53%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.000mg/ml (3.78mM)	Taking the 1 mL working solution as an example, add 20 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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	4%DMSO 1 30%PEG300 2 5%Tween80 3 61%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	3.000mg/ml (5.67mM)	Taking the 1 mL working solution as an example, add 40 μL of 75 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 610 μL of ddH2O 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

특징	A selective inhibitor of native and mutant Bcr-Abl.
Targets/IC₅₀/Ki	Bcr-Abl (Murine myeloid progenitor cells) <30 nM
시험관 내(In vitro)	Nilotinib은 활성화된 HSC에서 증식, 이동, 액틴 필라멘트 형성을 억제하며, α-SMA 및 콜라겐의 발현도 억제합니다. 이 화합물은 HSC의 세포자멸사를 유도하며, 이는 bcl-2 발현 감소, p53 발현 증가, PARP 절단, 그리고 PPARγ 및 TRAIL-R 발현 증가와 관련이 있습니다. 또한 p27 발현 증가 및 cyclin D1 하향 조절과 함께 세포 주기 정지를 유도합니다. 흥미롭게도 이 화학 물질은 PDGFR 활성화뿐만 아니라 Src를 통한 TGFRII도 억제합니다. PDGF 및 TGFβ-모의 ERK 및 Akt 인산화를 유의하게 억제합니다. 또한 사람 HSC에서 PDGF 및 TGFβ에 의해 활성화된 Abl의 인산화 형태는 이 약물에 의해 억제됩니다. 이 억제제는 T315I를 제외한 대부분의 imatinib 내성 Bcr-Abl 변이를 억제합니다. PDGF-DD 매개 ERK1/2 활성화, 기저 및 PDGF-DD 매개 PDGFRβ 및 Akt 활성화, 슈반종 증식을 억제합니다. 이 화합물은 imatinib보다 강력하며, 정상 상태 최저 혈장 농도보다 낮은 농도에서 최대 억제 효과를 발휘합니다. 또한 TGF-β1 및 혈소판 유래 성장 인자(PDGF) 유전자 발현 수준을 유의하게 감소시킵니다. 이 치료법은 PDGF 유도 폐 섬유아세포 증식도 유의하게 억제합니다. p210- 및 p190-Bcr-Abl을 발현하는 Ba/F3 세포 또는 IC50 값이 ≤12 nM인 K562 및 Ku-812F 세포의 증식을 억제합니다.
생체 내(In vivo)	Nilotinib은 CCl₄ 및 BDL 유도 섬유증에서 콜라겐 침착 및 α-SMA 발현을 감소시킵니다. 이 화합물은 HSC의 세포자멸사를 유도할 수 있으며, 이는 bcl-2의 하향 조절과 관련이 있습니다. 이는 폐 손상 및 섬유증의 정도를 완화합니다. 이 치료법은 14일 및 21일에 하이드록시프롤린 수치를 유의하게 감소시키며, 이는 변형 성장 인자(TGF)-β1 및 PDGFRβ의 발현 수준 감소를 동반합니다. 이 화학 물질은 Bcr-Abl 전환 조혈모세포주 또는 원시 골수 세포를 주입한 마우스의 생존을 연장시키고, imatinib 내성 CML 마우스 모델에서 생존을 연장시킵니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/17068153/ [2] https://pubmed.ncbi.nlm.nih.gov/21251937/ [3] https://pubmed.ncbi.nlm.nih.gov/21220945/ [4] https://pubmed.ncbi.nlm.nih.gov/21727212/ [5] https://pubmed.ncbi.nlm.nih.gov/21659722/ [6] https://pubmed.ncbi.nlm.nih.gov/15710326/

적용 분야

방법	바이오마커	이미지	PMID
Western blot	p-AMPKα / AMPKα / p-AMPKβ1 / AMPKγ2 / p-LKB1 / LKB1 / CaMKIIβ DNMT1 / DNMT3a / DNMT3b pABL1 / p-NF-κB1 / NF-κB / STAT3 / p-STAT3 / IL-1β / IL-6 / COX2		23677989
Growth inhibition assay	Cell viability		23677989

임상시험 정보

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT06409936	Not yet recruiting	CML Chronic Phase\|Chronic Myeloid Leukemia Chronic Phase\|Chronic Myeloid Leukemia BCR/ABL-Positive\|Chronic Myeloid Leukemia	Gruppo Italiano Malattie EMatologiche dell''Adulto\|Fundacion Espanola para la Curacion de la Leucemia Mieloide Cronica	September 2024	Phase 2
NCT05185947	Recruiting	Gynecologic Cancer\|Gynecologic Neoplasms\|Peritoneal Carcinomatosis\|Peritoneal Neoplasms\|Ovarian Cancer\|Ovarian Neoplasms\|Colorectal Cancer\|Colorectal Neoplasms\|Appendiceal Cancer\|Appendiceal Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	October 13 2022	Phase 2
NCT04326933	Unknown status	Patients Diagnosed as Chronic Meyloid Leukemia	Assiut University	January 1 2020	--
NCT04002674	Recruiting	Dementia With Lewy Bodies	Georgetown University\|National Institutes of Health (NIH)	July 1 2019	Phase 2

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자주 묻는 질문

질문 1:
I would like to use it for in vivo studies in mice, can you give me some suggestions about the in vivo formulation?

답변:
For in vivo study, we recommend to use 4% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 3mg/ml for it.

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