raf kinases

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.

Encorafenib (LGX818) is an oral, highly selective inhibitor of the BRAF V600E mutation with an IC50 of 0.3 nM, exhibiting antitumor activity. Encorafenib can be used for studying tumor signaling pathway regulation and mechanisms of drug resistance.

BRAF inhibitor is an inhibitor of B-Raf.

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5/0.6 nM) and is ATP-competitive. Dabrafenib exhibits antitumor activity for the treatment of B-RafV600E-mutated melanoma.

PLX-4720 is a potent and selective B-Raf (V600E) inhibitor designed to block the ATP-binding site of oncogenic B-Raf with IC50 of 13 nM.

Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity

Dabrafenib Mesylate (GSK2118436 Mesylate) is a B-Raf inhibitor(IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively).

L-779450, an effective, ATP-competitive Raf kinase inhibitor (IC50: 10 nM) , displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively.

Raf inhibitor 2 (CID 25014542) is novel inhibitor of Raf kinases.

Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1/2 activating mutations in the MAPK pathway.

LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.

LUT014, a B-Raf inhibitor (IC50: 11.7 nM), is developed to reduce dose-limiting acneiform lesions associated with EGFR inhibitors treatment.

B-Raf IN 1 is an inhibitor of B-Raf (IC50: 24 nM) and c-Raf (IC50: 25 nM).

ZM 336372 is a potent and selective c-Raf inhibitor.

TAK-632, a potent pan-Raf inhibitor (GenScript, 2020), is characterized by its molecular weight [M] for [C 22 H 19 FN 2 O 2] of 362.4 by LC-MS, with a purity of 99% (HPLC). The compound exhibits white to off-white solid form and has a melting point [M] ranging from 178°C to 182°C (GenScript, 2020). Its solubility profile includes DMSO, in which it is soluble to 100mM (GenScript, 2020).

Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.

Lifirafenib (Beigene-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant respectively.

Takeda-6d, a novel, potent DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor, inhibits B-RAF and VEGFR2 with IC50 of 7.0nM and 2.2nM.

SB590885 is an effective B-Raf inhibitor (Ki: 0.16 nM, in a cell-free assay). The selectivity of SB590885 for B-Raf is 11-fold greater over c-Raf, no acts to other human kinases.

Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.