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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PLX4032 (Vemurafenib)

Catalog No. A10739
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Raf 抑制剂

PLX4032(Vemurafenib)也称为RG7204，Vemurafenib，R7204，RO5185426。PLX4032是B-raf抑制剂，IC50为44 nM。了解更多

Product Citations (11)

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- Guixin Zhu, .et al. TRIM15 and CYLD regulate ERK activation via lysine-63-linked polyubiquitination, Nat Cell Biol, 2021, Sep;23(9):978-991 PMID: 34497368
- 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
- Kudo K, .et al. Cell surface CD63 increased by up-regulated polylactosamine modification sensitizes human melanoma cells to the BRAF inhibitor PLX4032, FASEB J, 2018, Dec 3:fj201800664RR PMID: 30508500
- Min Ho Choe, .et al. miR-550a-3-5p acts as a tumor suppressor and reverses BRAF inhibitor resistance through the direct targeting of YAP, Cell Death Dis, 2018, Jun; 9(6): 640 PMID: 29844307
- Jan Dorrie, .et al. BRAF and MEK Inhibitors Influence the Function of Reprogrammed T Cells: Consequences for Adoptive T-Cell Therapy, Int J Mol Sci, 2018, Jan; 19(1): 289 PMID: 29346301
- Aishwarya Kundu, .et al. Inhibition of Oncogenic BRAF Activity by Indole-3-Carbinol Disrupts Microphthalmia-Associated Transcription Factor Expression and Arrests Melanoma Cell Proliferation, Mol Carcinog, 2017, Jan; 56(1): 49-61 PMID: 26878440
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Toshinori Sueda, .et al. BRAFV600E inhibition stimulates AMP-activated protein kinase-mediated autophagy in colorectal cancer cells, Sci Rep, 2016, 6: 18949 PMID: 26750638
- Yanling Li, .et al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells, Onco Targets Ther, 2015, 8: 1043-1051 PMID: 25999739