Drug Class Detail

Drug Class RAF Inhibitor (Pan)

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Drug Name Trade Name Synonyms Drug Classes Drug Description
AZ628 AZD628|AZD-628 RAF Inhibitor (Pan) 17 AZ628 is an irreversible pan-RAF inhibitor with activity against RAF1 and BRAF, including BRAF V600E, which leads to increased cell-cycle arrest and apoptosis of tumor cells (PMID: 18020980, PMID: 23288408).
CCT196969 RAF Inhibitor (Pan) 17 SRC Inhibitor 26 CCT196969 is a paradox-breaking pan-RAF inhibitor, with additional activity against SRC and LCK, which potentially results in decreased growth of tumor cells, including cells resistant to BRAF inhibitors (PMID: 25500121).
LY3009120 DP-4978 RAF Inhibitor (Pan) 17 LY3009120 is a Pan-RAF inhibitor that inhibits signaling of all RAF isoforms and RAF dimers, which leads to inhibition of tumor cell growth (PMID: 26343583).
CCT241161 RAF Inhibitor (Pan) 17 SRC Inhibitor 26 CCT241161 is a paradox-breaking pan-RAF inhibitor, with additional activity against SRC and LCK, which potentially results in decreased growth of tumors, including those resistant to BRAF inhibitors (PMID: 25500121).
L779450 L-779,450 RAF Inhibitor (Pan) 17 L779450 is a pan-RAF inhibitor, which may lead to decreased tumor cell proliferation and increased apoptosis (PMID: 23955071, PMID: 12970777).
Vemurafenib Zelboraf RO5185426|PLX4032 RAF Inhibitor (Pan) 17 Zelboraf (vemurafenib) inhibits BRAF V600E, wild-type BRAF, ARAF, and CRAF (PMID: 20179705), which may result in an inhibition of the MAPK signaling pathway resulting in a reduction of tumor cell proliferation (PMID: 20823850). Zelboraf (vemurafenib) is FDA approved for BRAF V600E-mutant melanoma and for BRAF V600-positive Erdheim-Chester disease (FDA.gov).
TAK-632 RAF Inhibitor (Pan) 17 TAK-632 is an inhibitor of Raf, which has been shown to suppress the kinase activity of the Raf dimer thereby resulting in diminished paradoxical activation of Raf (PMID: 24121489).
Sorafenib Nexavar BAY 43-9006 CSF1R Inhibitor 22 FLT3 Inhibitor 48 KIT Inhibitor 48 PDGFR-beta Inhibitor 13 RAF Inhibitor (Pan) 17 RET Inhibitor 36 VEGFR2 Inhibitor 34 Nexavar (sorafenib) is a multikinase inhibitor with activity against several kinases, including RAF kinases, VEGFR2, VEGFR3, PDGFR-beta, KIT, FLT3, RET, and CSF1R, potentially resulting in decreased tumor growth (PMID: 18445656, PMID: 15466206, PMID: 21517818). Nexavar (sorafenib) is approved for metastatic differentiated thyroid carcinoma, hepatocellular carcinoma, and renal cell carcinoma (FDA.gov).
BGB659 RAF Inhibitor (Pan) 17 BGB659 is a pan-RAF inhibitor that results in inhibition of MEK/ERK signaling generated by either RAF dimers or RAF monomers and thus, prevents cell proliferation (PMID: 26343582).
RO5126766 CH5126766 MEK inhibitor (Pan) 20 MEK1 Inhibitor 20 MEK2 Inhibitor 18 RAF Inhibitor (Pan) 17 RO5126766 is dual RAF-MEK1/2 inhibitor with effectiveness against both BRAF and RAS mutated cells (PMID: 25422890).
ARQ736 RAF Inhibitor (Pan) 17 ARQ736 is a pan-RAF inhibitor with activity against BRAF V600E, BRAF wild-type, and c-RAF (PMID: 23617957).
LXH 254 LXH254 RAF Inhibitor (Pan) 17 LXH 254 is a pan-RAF inhibitor that inhibits proliferation of tumor cells (NCI Drug Dictionary).
PF-04880594 RAF Inhibitor (Pan) 17 PF-04880594 is a Raf inhibitor, which has been shown to inhibit tumor growth in xenograft models (PMID: 19764794).
XL281 BMS-908662 RAF Inhibitor (Pan) 17 XL281 is a pan-RAF kinase inhibitor, which blocks RAS/RAF/MEK/ERK signaling to prevent cell proliferation (PMID: 25476894).
LSN3074753 RAF Inhibitor (Pan) 17 LSN3074753 is a Pan-RAF inhibitor that inhibits signaling of all RAF isoforms and RAF dimers, which leads to inhibition of tumor cell growth (PMID: 28611205).
INU-152 RAF Inhibitor (Pan) 17 INU-152 is a small molecule pan-RAF inhibitor, which reduces downstream MAPK pathway signaling and may inhibit growth of BRAF-mutant tumors (PMID: 28645859).
MLN2480 BIIB-024|TAK-580 RAF Inhibitor (Pan) 17 MLN2480 is an inhibitor of pan-Raf kinases, which interrupts RAF/MEK/ERK signal transduction pathways to inhibit tumor cell growth (NCI Drug Dictionary).