Vemurafenib（PLX4032）是一种首创、选择性且强效的B-RAF激酶抑制剂，对RAFV600E和c-RAF-1的IC50分别为31 nM和48 nM。Vemurafenib诱导细胞自噬。

PLX 4720 is a potent and selective inhibitor of B-RafV600E (IC50=13 nM) and c-Raf-1Y340D/Y341D (IC50=6.7 nM), whth a 10-fold selectivity for B-RafV600E than wild-type B-Raf.

Dabrafenib (GSK2118436A) 是一种 ATP 竞争性的 Raf 抑制剂，对 C-Raf 和 B-RafV600E 的 IC50 值分别为 5 nM 和 0.6 nM。

GDC-0879 is a potent, and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well, displaying no inhibition known to other protein kinases.

RAF265 is a pan-inhibitor that inhibits C-Raf, B-Raf and B-Raf V600E with IC50 of 3 nM-60 nM. It also shows inhibition on phosphorylation of VEGFR2 with EC50 of 30 nM.

AZ 628 is a 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.

SB-590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.

TAK-632 is a selective pan-RAF kinase inhibitor with IC50 values of 2.4/1.4 nM for BRAF V600E/c-RAF with > 60 fold selectivity over VEGFR.

CEP-32496 is an inhibitor of BRAF V600E (IC50 = 14 nM), WT (IC50 = 34 nM) and c-Raf (IC50 = 39 nM). It also exhibits certain inhibitory activity against Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2.

In vitro, BGB-283 potently inhibits BRAFV600E-activated ERK phosphorylation and cell proliferation.

LY3009120（DP-4978）是一种广谱RAF抑制剂，抑制BRAFV600E、BRAFWT和CRAFWT的IC50值分别为5.8 nM、9.1 nM和15 nM。

Avutometinib（Ro 5126766）是一种双重MEK/RAF抑制剂，具有抗肿瘤活性。它对BRAFV600E、CRAF、MEK和BRAF的IC50值分别为8.2 nM、56 nM、160 nM和190 nM。

Encorafenib is a potent and selective B-Raf^V600E inhibitor, with no significant activity observed against a panel of 100 kinases (IC50>900nM).

Sorafenib is a multi-kinase inhibitor that inhibits Raf-1 and B-RAF (IC50s = 6 and 22 µM, respectively), as well as the receptor tyrosine kinases VEGFR2, VEGFR3, PDGFRβ, FLT3, and c-Kit (IC50s = 90, 15, 20, 57, and 58 nM, respectively).

CCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for BRAF, but not cancer cells that are wild-type for BRAF and NRAS. CCT196969 induces caspase 3 and PARP cleavage, thus induces apoptosis. CCT196969 does not drive paradoxical pathway activation and inhibit MEK/ERK in BRAF and NRAS mutant melanoma.