b-rafv600e

HG6-64-1 is a potent and selective inhibitor of B-Raf, with an IC50 of 0.09 μM on B-raf V600E-transformed Ba F3 cells.

PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.

GSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers.

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.

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.

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

Belvarafenib (HM95573) is a potent pan-RAF inhibitor with antitumor activity and inhibits B-RAF, B-RAFv600E, and C-RAF with IC50 values of 56, 7, and 5 nM.

RAF mutant-IN-1 is an inhibitor of RAF kinase(IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D Y341D, B-RAFV600E and B-RAFWT, respectively).

B-Raf inhibitor 1 (B-Raf inhibitor 1) is a potent and selective B-Raf inhibitor.

AMG-628 is an effective and ATP-competitive RAF kinase inhibitor. AMG-628 has been shown to inhibit growth and induce cell cycle arrest and apoptosis in colon and melanoma cell lines with B-RAFV600E mutations.

CAY10717 is a multi-targeted kinase inhibitor that exhibits greater than 40% inhibition of 34 of 104 kinases in an enzymatic assay at a concentration of 100 nM. It has activity at multiple oncogenic kinases, with IC50 values less than 50 nM against wild-type EGFR and ABL and mutant ABLG250E, ABLY253F, ABLE255K, and B-RafV600E. CAY10717 is highly cytotoxic against a cancer cell panel that includes chemotherapy-sensitive and -resistant cell lines (EC50s = 0.4-158 nM). It also inhibits the growth of human umbilical vein endothelial cells (HUVECs; EC50 = 34 nM), a model for tumor angiogenesis.

Raf inhibitor 1 dihydrochloride (B-Raf inhibitor 1 dihydrochloride) is a potent and selective B-Raf inhibitor.

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.

Belvarafenib TFA (HM95573 TFA) is a potent and broadly available inhibitor of fibrosarcoma kinase (RAF), acting on B-RAF (IC50: 56 nM), B-RAFv600E (IC50: 7 nM), and C-RAF (IC50: 5 nM).

RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1 2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen-activated protein kinase pathway activation. In vitro, RO5068760 demonstrates MEK1 kinase inhibitory activity with an IC50 of 0.025 μM in a cRaf MEK ERK cascade assay RO5068760 showed superior efficacy in tumors harboring B-RafV600E mutation.

AMG-628, (S)-, is the S isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.

Lifirafenib, also known as Beigene-283, is a Novel potent and selective RAF Kinase and EGFR inhibitor. BGB-283-displays Potent Antitumor Activity in B-RAF Mutated Colorectal Cancers. In vitro, BGB-283 potently inhibits B-RAFV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harbouring B-RAFV600E and EGFR mutation amplification. In B-RAFV600E CRC cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. In vivo, BGB-283 treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell-line derived and primary human colorectal tumor xenografts bearing B-RAFV600E mutation. BGB-283 as a potent antitumor drug candidate with clinical potential for treating CRC harbouring B-RAFV600E mutation.

EBI-907 is a highly potent and orally efficacious B-RafV600E inhibitor. EBI-907 displays a low single-digit nanomolar activity (IC50 = 4.9 nM), which is >10-fold more potent than Vemurafenib (IC50 = 59 nM). EBI-907 also exhibits high potency in selectively inhibiting the proliferation of BRAF (V600E)-dependent cell lines (A375 and Colo205) and cellular Erk phosporylation, with superior activity to Vemurafenib. EBI-907, displaying potent activity against a number of important oncogenic kinases including BRK, FGFR1, c-Kit, and PDGFRb.

AMG-628, (R)- is the R isomer of AMG-628 --- a potent, ATP-competitive inhibitor of Raf kinases. AMG-628 displays selectivity for Raf kinases and inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. AMG-628 has shown to inhibit growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.

MAPK-IN-2 (compound 3h) is an efficacious MAPK inhibitor with antineoplastic properties that significantly hinders proliferation across various cancer cell lines. It demonstrates robust suppression of the MAPK pathway (EGFR WT IC50 = 281 nM, c-MET IC50 = 205 nM, B-RAF WT IC50 = 112 nM, CDK4 6 IC50 = 95 and 184 nM, respectively) and exhibits pronounced activity against mutated forms of EGFR and B-RAF (EGFR T790M IC50 = 69 nM and B-RAF V600E IC50 = 83 nM) [1].