Raf

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Raf	C-Raf/Raf-1	B-Raf	Other
A10739	Vemurafenib		*	**	SRMS,ACK1,MAP4K5 (KHS1)
A10002	PLX-4720		***	***	BRK,FRK,CSK
A11381	Dabrafenib		****	****
A10420	GDC-0879			****
A10773	RAF265			**	VEGFR2
A11063	AZ 628		**	**
A10661	NVP-BHG712		*		EphB4,c-Src,c-Abl
A10829	SB590885			****
A11077	ZM 336372		*
A10001	Sorafenib		****	**	mVEGFR2(Flk1),mVEGFR3,mPDGFRβ
A11436	GW5074		***
A13323	TAK-632		****	***	Aurora B,PDGFRβ,FGFR3
A13772	CEP-32496		**	***	RET,PDGFRβ,LCK
A13226	Encorafenib			****
A14019	RO5126766		*	***	MEK1
A15855	PLX7904
A11240	MLN2480
A10250	Regorafenib (BAY 73-4506)		****	**	FGFR1, Kit, PDGFRβ, RET, Tie-2 , VEGFR1, VEGFR2, VEGFR3
A11211	ML 786 dihydrochloride		****	****	Abl-1, DDR2, EPHA2, RET, PERK
A12739	PF-04880594		****	****
A13525	L-779450	****			p38α, GSK3β, Lck

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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Regorafenib (BAY 73-4506)

Catalog No. A10250
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VEGFR 抑制剂

Regorafenib (BAY 73-4506)是一种多激酶抑制剂，IC50为17、40和69 nM c-KIT，VEGFR2，B-Raf。Regorafenib（BAY 73-4506）是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。了解更多

Product Citations (9)

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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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Regorafenib monohydrate

Catalog No. A15218
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Tyrosine kinase 抑制剂

Regorafenib monohydrate是VEGFR1/VEGFR2/VEGFR3/PDGFRβ/Kit/RET和Raf-1的多靶点抑制剂，IC50分别为13 nM/4.2 nM/46 nM/22 nM/7 nM/1.5 nM和2.5 nM。了解更多

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RAF265 (CHIR-265)

Catalog No. A10773
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RAF/VEGFR 抑制剂

RAF265 (CHIR-265)是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，可控制或正常化VEGFR-2，同时抑制B-raf和c-Raf突变以预防癌症。了解更多

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Raf265 derivative

Catalog No. A10774
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RAF/VEGFR 抑制剂

Raf265 derivative是Raf265的衍生物，Raf265是一种口服，高度选择性的RAF和VEGFR激酶抑制剂，IC50为5至10μM。了解更多

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