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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TAK-632

Catalog No. A13323
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pan-RAF 抑制剂

TAK-632是一种有效的泛RAF抑制剂，具有良好的体外活性（BRAF（V600E）IC50，2.4 nM; BRAF（wt），8.3 nM; CRAF，1.4 nM; pMEK（A375）IC50，12 nM; pMEK（HMVII ），49 nM。了解更多

Product Citations (1)

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- Yosi Shamay, .et al. Quantitative Self-Assembly Prediction Yields Targeted Nanomedicines, Nat Mater, 2018, Apr; 17(4): 361-368 PMID: 29403054
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Sorafenib Tosylate (Nexavar)

Catalog No. A10001
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Raf 抑制剂

Sorafenib Tosylate (Nexavar)是几种酪氨酸蛋白激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂的新型小分子抑制剂，Raf-1，wt BRAF和V599E突变型BRAF的IC50为6、22、38 nM。了解更多

Product Citations (12)

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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
- 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
- Fangyuan Lai, .et al. Platelet-rich plasma enhances the proliferation of human adipose stem cells through multiple signaling pathways, Stem Cell Res Ther, 2018, 9: 107 PMID: 29661222
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Arum Park, .et al. Identification of Transcription Factor YY1 as a Regulator of a Prostate Cancer-Specific Pathway Using Proteomic Analysis, J Cancer, 2017, 8(12): 2303-2311 PMID: 28819434
- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Zhihong Li, .et al. Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3, J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
- Hideki Yamaguchi, .et al. Saracatinib impairs the peritoneal dissemination of diffuse-type gastric carcinoma cells resistant to Met and fibroblast growth factor receptor inhibitors, Cancer Sci, 2014, 105(5): 528-536 PMID: 24612061
- Yaping Zhang, .et al. FLT3 and CDK4/6 inhibitors: Signaling mechanisms and tumor burden in subcutaneous and orthotopic mouse models of acute myeloid leukemia, J Pharmacokinet Pharmacodyn., 2014, 41(6): 675-691 PMID: 25326874
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CEP-32496 hydrochloride

Catalog No. A15040
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Raf 抑制剂

CEP-32496 hydrochloride是野生型BRAF，V600E突变型BRAF和c-Raf的高效抑制剂，Kd值分别为14 nM，36 nM和39 nM。了解更多

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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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CEP-32496

Catalog No. A13772
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Raf 抑制剂

CEP-32496是一种口服v-raf鼠肉瘤病毒癌基因同源物B1（B-raf）丝氨酸/苏氨酸蛋白激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

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