| S2872 |
GW5074 |
GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. |
Selective |
C-Raf, IC50: 9 nM |
| S2720 |
ZM 336372 |
ZM 336372 is a potent and selective c-Raf inhibitor with IC50 of 70 nM, 10-fold selectivity over B-RAF, no inhibition to PKA/B/C, AMPK, p70S6, etc. |
Selective |
C-Raf, IC50: 70 nM |
| S2202 |
NVP-BHG712 |
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively. |
Selective |
C-Raf, IC50: 0.395 μM |
| S7291 |
TAK-632 |
TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases. |
Pan |
C-Raf, IC50: 1.4 nM |
| S2807 |
Dabrafenib (GSK2118436) |
Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. |
Pan |
C-Raf, IC50: 5.0 nM |
| S1040 |
Sorafenib Tosylate |
Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. |
Pan |
Raf-1, IC50: 6 nM |
| S7397 |
Sorafenib |
Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. |
Pan |
Raf-1, IC50: 6 nM |
| S1152 |
PLX-4720 |
PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf. |
Pan |
C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM |
| S2746 |
AZ 628 |
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. |
Pan |
C-Raf-1, IC50: 29 nM |
| S8015 |
CEP-32496 |
CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. |
Pan |
C-Raf, Kd: 39 nM |
| S1267 |
Vemurafenib (PLX4032, RG7204) |
Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM. |
Pan |
C-Raf, IC50: 48 nM |