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Raf Inhibitors | Chemicals (16)
water-soluble

Cat.No.	Product Name	Information	Product Citations	Customer Reviews
S1267	Vemurafenib (PLX4032, RG7204)	Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-Raf^V600E with IC50 of 31 nM.	Nature, 2012, 483(7387):100-3 Nature, 2014, 508(7494):118-22 Cell, 2012, 151(5):937-50
S1040	Sorafenib Tosylate	Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.	Hepatology, 2013, 59(4):1435-47 Blood, 2012, 120(19):4104-15 Blood, 2013, 122(9):1621-33
S1152	PLX-4720	PLX4720 is a potent and selective inhibitor of B-Raf^V600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.	Nature, 2013, 498(7452):109-12 Nature, 2014, 10.1038/nature14136 Nature, 2012, 483(7387):100-3
S2807	Dabrafenib (GSK2118436)	Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively.	J Clin Invest, 2014, 124(3):1406-17 J Clin Invest, 2014, 124(11):5074-84 Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1392
S1104	GDC-0879	GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well; no inhibition known to other protein kinases.	Cancer Discov, 2013, 3(3):350-62 J Natl Cancer Inst, 2012, 104(21):1673-9 Proc Natl Acad Sci U S A, 2011, 108(15):6067-72
S7108	Encorafenib (LGX818)	Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM. Phase 3.
S2161	RAF265 (CHIR-265)	RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM. Phase 2.	Hepatology, 2012, 56(6):2363-74 Mol Cell Proteomics, 2012, 11(6):M112.017764 Pigment Cell Melanoma Res, 2014, 27(1):124-33
S2746	AZ 628	AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.	Cancer Discov, 2013, 3(3):350-62 J Med Chem, 2014, 10.1021/jm501603h Cell Death Dis, 2014, 5:e1278
S2202	NVP-BHG712	NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.	Anticancer Res, 2014, 34(6):2913-8
S2220	SB590885	SB590885 is a potent B-Raf inhibitor with K_i of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.	Cell Death Dis, 2014, 5:e1278 Invest New Drugs, 2014, 32(4):626-35

Inhibitory Selectivity
Activation Selectivity
Solubility

Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S1267	Vemurafenib (PLX4032, RG7204)	<1 mg/mL	98 mg/mL	<1 mg/mL
S1040	Sorafenib Tosylate	0.01 mg/mL	127 mg/mL	<1 mg/mL
S1152	PLX-4720	<1 mg/mL	83 mg/mL	<1 mg/mL
S2807	Dabrafenib (GSK2118436)	<1 mg/mL	30 mg/mL	<1 mg/mL
S1104	GDC-0879	<1 mg/mL	67 mg/mL	5 mg/mL
S7108	Encorafenib (LGX818)	<1 mg/mL	100 mg/mL	100 mg/mL
S2161	RAF265 (CHIR-265)	<1 mg/mL	100 mg/mL	33 mg/mL
S2746	AZ 628	<1 mg/mL	90 mg/mL	<1 mg/mL
S2202	NVP-BHG712	<1 mg/mL	101 mg/mL	3 mg/mL
S2220	SB590885	<1 mg/mL	5 mg/mL	<1 mg/mL
S2720	ZM 336372	<1 mg/mL	78 mg/mL	2 mg/mL
S7397	Sorafenib	<1 mg/mL	63 mg/mL	<1 mg/mL
S2872	GW5074	<1 mg/mL	104 mg/mL	<1 mg/mL
S7291	TAK-632	<1 mg/mL	100 mg/mL	2 mg/mL
S2200	Raf265 derivative	<1 mg/mL	101 mg/mL	101 mg/mL
S8015	CEP-32496	<1 mg/mL	9 mg/mL	<1 mg/mL

Tags: B-Raf inhibition | Raf inhibition | B-Raf mutation | B-Raf cancer | Raf tumor | Raf pathway | Raf inhibitor drugs | Raf activation | Raf targets | Raf activity | Raf phosphorylation | B-Raf assay | Raf kinase assay | B-Raf inhibitor clinical trial | B-Raf inhibitor drug | Raf inhibitor review

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