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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 Cell, 2012, 151(5):937-50 Nat Med, 2012, 18(8):1239-47
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, 10.1002/hep.26790 Int J Cancer, 2012, 132(3):738-43 Blood, 2012, 120(19):4104-15
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, 2012, 483(7387):100-3 Nat Biotechnol, 2013, 31(7):630-7
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
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 Proc Natl Acad Sci U S A, 2011, 108(15):6067-72 Cell Death Differ, 2012, 19(12):2029-39
S7108	LGX818	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.
S7397	Sorafenib	Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.	J Neurosci, 2013, 33(7):3079-93 Molecular Oncology, 2014, 10.1016/j.molonc.2014.05.005 Biochem Pharmacol, 2012, 83(12):1674-81
S7291	TAK-632	TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.
S8015	CEP-32496	CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with K_d of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2.
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, 2013, 27(1):124-33

Inhibitory 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	LGX818	<1 mg/mL	100 mg/mL	100 mg/mL
S7397	Sorafenib	<1 mg/mL	93 mg/mL	<1 mg/mL
S7291	TAK-632	<1 mg/mL	100 mg/mL	2 mg/mL
S8015	CEP-32496	<1 mg/mL	9 mg/mL	<1 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
S2872	GW5074	<1 mg/mL	104 mg/mL	<1 mg/mL
S2200	Raf265 derivative	<1 mg/mL	101 mg/mL	101 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