b-raf

B-Raf IN 13 is a potent B-Raf inhibitor with anticancer activity, demonstrating an IC50 of 3.55 nM in the [BRAF V600E] enzyme assay.

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.

Xl-281 (BMS-908662) is a BRAF inhibitor with anti-tumor activity for the study of colorectal cancer and melanoma.

BRAF inhibitor is an inhibitor of B-Raf.

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.

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

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.

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).

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.

B-Raf IN 15 is a BRAF inhibitor that inhibits BRAFWT and BRAFV600E and can be used in the study of melanoma and cancer, and can be optimized for use as a more effective BRA F inhibitor.

B-Raf IN 16, a BRAF inhibitor, belongs to cyclic iminopyrimidine derivatives and can be used for cancer or tumour research.

B-Raf IN 14 is a BRAF inhibitor.

PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf,PROTAC B-Raf degrader 1 With anti-cancer activity.

Uplarafenib (B-Raf IN 10) is a potent BRAF inhibitor with an IC50 of 50-100 nM. B-Raf IN 10 exhibits antitumor activity that may influence cell proliferation and differentiation, making it suitable for studying solid tumors.

B-Raf IN 6 is a potent inhibitor (IC50: 1.7 nM) of the protein kinase B-Raf, which does not bind the secondary target PXR and is resistant to rapid metabolism.B-Raf IN 6 has shown research potential in cancer diseases.

B-Raf IN 8 (compound 7g) is a potent inhibitor of B-Raf (IC50 = 70.65 nM) with antitumor activity, demonstrating IC50 values of 9.78, 13.78, 18.52, and 29.85 μM against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7), and human prostate cancer (PC-3) cells [1].

B-Raf IN 2, compound Ia, is a highly effective and specific inhibitor of BRAF. It exhibits significant potential for cancer research.

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

B-Raf IN 9 (compound 8b) is an effective B-Raf inhibitor (IC50=24.79 nM) that blocks the cell cycle at the G2 M phase, induces apoptosis, and exhibits potent anti-tumor activity on human prostate cancer PC-3 cells (IC50=7.83 μM).

B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor with an IC50 of 110.23 nM. It exhibits antitumor activity against colon carcinoma cells (HCT-116), mammary gland cells (MCF-7), hepatocellular carcinoma cells (HEPG-2), human cervical carcinoma cells (Hela), and human prostate cancer cells (PC-3), with IC50 values of 7.50, 9.87, 10.57, 11.63, and 12.83 μM, respectively [1].

B-Raf IN 5 is a potent inhibitor of the protein kinase B-Raf (IC50: 2.0 nM). B-Raf IN 5 resists rapid metabolism and does not bind to the secondary target PXR.

B-Raf IN 11 is a novel selective inhibitor. The DFG-in conformation of the B-Raf kinase V600E mutant is superior to the DFG-out conformation in colorectal cancer.

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.