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Regorafenib (BAY 73-4506) 다중 키나아제 억제제

Name: Regorafenib (BAY 73-4506)
Brand: Selleck Chemicals
SKU: S1178
Rating: 5 (216 reviews)

제품 번호S1178

Regorafenib은 무세포 분석에서 VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) 및 Raf-1에 대한 다중 표적 억제제로, 각각 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM 및 2.5 nM의 IC50 값을 가집니다. Regorafenib은 Autophagy를 유도합니다.

Regorafenib (BAY 73-4506) VEGFR 억제제 Chemical Structure

화학 구조

분자량: 482.82

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품질 관리

배치: 순도: 99.91%

99.91

관련 타겟	EGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
기타 VEGFR 억제제	SAR131675 SU 5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Anlotinib (AL3818) Dihydrochloride Linifanib (ABT-869) Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 ZM 323881 HCl

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
Hep3B	Apoptosis Assay	1–5 μM	48 h		inhibits cell growth	26329608
PLC/PRF/5	Apoptosis Assay	1–5 μM	48 h		inhibits cell growth	26329608
HepG2	Apoptosis Assay	1–5 μM	48 h		inhibits cell growth	26329608
HEK293	Function Assay	0.5 μM	2/4/6 h		reduces GRP78 expression	25858032
GEO	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW48	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
HT29	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW480	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW620	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
HCT116	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
LOVO	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
HCT150	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW48-CR	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
GEO-CR	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
KB-31	Growth Inhibition Assay				IC50=5.5±0.3 nM	25753361
KB-G2	Growth Inhibition Assay				IC50=9.1±0.1 nM	25753361
LLC-PK1	Growth Inhibition Assay				IC50=42.0±3.2 nM	25753361
LLC-PK1/MRP2	Growth Inhibition Assay				IC50=82.4±2.7 nM	25753361
HEK293	Growth Inhibition Assay				IC50=11.0±1.2 nM	25753361
HEK293/OATP1B1	Growth Inhibition Assay				IC50=6.2±0.3 nM	25753361
HROC18	Growth Inhibition Assay				IC50=1.3 μM	25309914
HROC24	Growth Inhibition Assay				IC50=4.6 μM	25309914
HROC43	Growth Inhibition Assay				IC50=5.3 μM	25309914
HROC46	Growth Inhibition Assay				IC50=2.4 μM	25309914
RJ345	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
RJ348	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
MCF-7	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
MDA-MB-231	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
HT15	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
DLD1	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
HT-29	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
Hct-116	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
HT15	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
DLD1	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
HT-29	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
Hct-116	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
GBM5	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
GBM6	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
GBM12	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
GBM14	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
Hep3B	Growth Inhibition Assay	1–2.5 μM	24/48/72 h		inhibits cell growth	24885890
PLC/PRF/5	Growth Inhibition Assay	1–2.5 μM	24/48/72 h		inhibits cell growth	24885890
HepG2	Growth Inhibition Assay	1–2.5 μM	24/48/72 h		inhibits cell growth	24885890
HCT116	Function Assay	10/20/40 μM	24 h		induces PUMA protein and mRNA expression in a dose- and time-dependent manner	24763611
Lim2405	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
LoVo	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
Lim1215	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW48	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
RKO	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW837	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW1463	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW480	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
Vaco432	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
Vaco400	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
DLD1	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
HT29	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
PLC/PRF/5	Growth Inhibition Assay	1–5µM	24/48/72 h		inhibits cell growth	23169148
HepG2	Growth Inhibition Assay	1–5µM	24/48/72 h		inhibits cell growth	23169148
Hep3B	Growth Inhibition Assay	1–5µM	24/48/72 h		inhibits cell growth	23169148
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.021 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.029 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.033 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.047 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.049 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.051 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.063 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.094 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.108 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.13 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.231 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.29 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.38 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs		Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.522 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.549 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.833 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.834 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.943 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 1.27 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 1.35 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 2.371 μM.	30204441
GIST430	Cytotoxicity assay		72 hrs		Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 3 μM.	28991465
BA/F3	Cytotoxicity assay		72 hrs		Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 9.953 μM.	30204441
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
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
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
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	482.82	화학식	C₂₁H₁₅ClF₄N₄O₃	보관 (수령일로부터)	3년-20°C분말
CAS 번호	755037-03-7	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	Fluoro-Sorafenib, BAY 73-4506			Smiles	CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F

용해도

In vitro
배치:

DMSO : 97 mg/mL (200.9 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 3 mg/mL

Water : Insoluble

DMSO : 96 mg/mL (198.83 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 97 mg/mL (200.9 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 97 mg/mL (200.9 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 97 mg/mL (200.9 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 2 mg/mL

Water : 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.
Clear solution	2% DMSO 1 30% PEG 300 2 5% Tween 80 3 ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	5.000mg/ml (10.36mM)	Taking the 1 mL working solution as an example, add 20 μL of 250 mg/ml clarified DMSO stock solution to 300 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; Then continue to add 630 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	2%DMSO 1 98% Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	5.000mg/ml (10.36mM)	Taking the 1 mL working solution as an example, add 20 μL of 250 mg/ml clarified DMSO stock solution to 980 μL of corn oil and mix evenly. 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.
Clear solution	5%DMSO 1 95% Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	5.000mg/ml (10.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 950 μL of corn oil and mix evenly. 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.
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.

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	RET (Cell-free assay) 1.5 nM Raf-1 (Cell-free assay) 2.5 nM VEGFR2 (Cell-free assay) 4.2 nM Kit (Cell-free assay) 7 nM VEGFR1 (Cell-free assay) 13 nM B-Raf (V600E) (Cell-free assay) 19 nM PDGFRβ (Cell-free assay) 22 nM B-Raf (Cell-free assay) 28 nM VEGFR3 (Cell-free assay) 46 nM
시험관 내(In vitro)	Regorafenib은 NIH-3T3/VEGFR2 세포에서 VEGFR2 자가인산화를 3 nM의 IC50으로 강력하게 억제합니다. HAoSMC에서 이 화합물은 PDGF-BB 자극 후 PDGFR-β 자가인산화를 90 nM의 IC50으로 억제합니다. 또한 FGF10으로 자극된 MCF-7 유방암(BC) 세포에서 FGFR 신호 전달을 억제합니다. 이 화학물질은 돌연변이 수용체 KIT^K642E 및 RET^C634W를 각각 약 20 nM 및 10 nM의 IC50으로 매우 강력하게 억제했습니다. VEGF¹⁶⁵로 자극된 HUVEC의 증식을 약 3 nM의 IC50으로 억제합니다. 이 화합물은 FGF2로 자극된 HUVEC과 PDGF-BB로 자극된 HAoSMC의 증식을 각각 127 nM 및 146 nM의 IC50으로 억제합니다. 이는 Protein Tyrosine Kinase (VEGFR, KIT, RET, FGFR, PDGFR) 및 세린/트레오닌 키나아제 (Raf 및 p38MAPK) 수용체 억제를 통해 종양 세포 증식과 종양 혈관 모두를 표적으로 합니다. 이 화학물질은 인간 Hep3B, PLC/PRF/5 및 HepG2 세포의 성장을 농도 및 시간 의존적으로 억제합니다.
키나아제 분석	키나아제 분석
키나아제 분석	재조합 VEGFR2 (쥐 aa785–aa1367), VEGFR3 (쥐 aa818–aa1363), PDGFRβ (aa561–aa1106), Raf-1 (aa305–aa648) 및 BRafV600E (aa409–aa765) 키나아제 도메인을 사용한 시험관 내 분석이 수행됩니다. 초기 시험관 내 키나아제 억제 프로파일링은 이 화합물의 1 μM 고정 농도에서 수행됩니다. 50% 억제 농도(IC50) 값은 선택된 반응성 키나아제, 예를 들어 VEGFR1 및 RET에서 결정됩니다. TIE2 키나아제 억제는 글루타티온-S-트랜스퍼라제, TIE2의 세포내 도메인 및 펩타이드 바이오틴-Ahx-EPKDDAYPLYSDFG를 기질로 사용하는 재조합 융합 단백질을 이용한 균일 시간 분해 형광(HTRF) 분석으로 측정됩니다.
생체 내(In vivo)	Regorafenib은 마우스의 다양한 전임상 인간 이종이식 모델에서 강력한 용량 의존적 TGI를 나타내며, 유방 MDA-MB-231 및 신장 786-O 암종 모델에서 종양 축소를 보였습니다. 이 화합물은 지방 패드에 정위적으로 성장하는 동계 원발성 4T1 유방 종양의 성장을 막을 뿐만 아니라 폐에서의 종양 전이 형성도 억제합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/21170960/ [2] https://pubmed.ncbi.nlm.nih.gov/21789125/ [3] https://pubmed.ncbi.nlm.nih.gov/22777740/

적용 분야

방법	바이오마커	PMID
Western blot	p-STAT3 / STAT3 / PARP / Caspase-9 Cyclin D / Cyclin E / Cyclin A / Cyclin B / p27 / p21 p-FGFR2 / p-FRS2α / p-AKT / p-MAPK / p-P90RSK / FGFR2 / AKT / MAPK / p90RSK p-p65(S536) / p65 Bim / Bid / Bak / Bcl-Xl / Mcl-1 PUMA / p53	25071018
Immunofluorescence	F-actin / Vimentin / E-cadherin p65	27580057
Growth inhibition assay	Cell viability GI50	25071018

임상시험 정보

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT06321055	Not yet recruiting	Advanced Gastrointestinal Stromal Tumor	Bayer	March 20 2024	--
NCT06137170	Active not recruiting	Metastatic Colorectal Cancer	Bayer	March 1 2024	--
NCT06029010	Completed	Metastatic Colorectal Cancer	Bayer	August 31 2023	--
NCT05370807	Recruiting	Melanoma Stage III\|Melanoma Stage IV	Universitair Ziekenhuis Brussel	October 3 2022	Phase 2

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자주 묻는 질문

질문 1:
How to resuspend it for in vivo studies?

답변:
For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 5mg/ml for it.

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