Raf

Inhibitory Selectivity
Catalog No.Inhibitor Name RafC-Raf/Raf-1B-RafA-rafOther
A10739Vemurafenib
*
**
SRMS,ACK1,MAP4K5 (KHS1)
A10002PLX-4720
***
***
BRK,FRK,CSK
A11381Dabrafenib
****
****
A10420GDC-0879
****
A10773RAF265
**
VEGFR2
A11063AZ 628
**
**
A10661NVP-BHG712
*
EphB4,c-Src,c-Abl
A10829SB590885
****
A11077ZM 336372
*
A10001Sorafenib
****
**
mVEGFR2(Flk1),mVEGFR3,mPDGFRβ
A11436GW5074
***
A13323TAK-632
****
***
Aurora B,PDGFRβ,FGFR3
A13772CEP-32496
**
***
RET,PDGFRβ,LCK
A13226Encorafenib
****
A14019RO5126766
*
***
MEK1
A15855PLX7904
A11240MLN2480
A10250Regorafenib (BAY 73-4506)
****
**
FGFR1, Kit, PDGFRβ, RET, Tie-2 , VEGFR1, VEGFR2, VEGFR3
A11211ML 786 dihydrochloride
****
****
Abl-1, DDR2, EPHA2, RET, PERK
A12739PF-04880594
****
****
A13525L-779450
****
p38α, GSK3β, Lck

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.



31 Item(s)

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Catalog No. Product Name Application Product Information
A13226

LGX 818 (Encorafenib)

Selective B-RAF Inhibitor
LGX818 is an orally available Raf kinase inhibitor with potential antineoplastic activity.
A16022

HG6-64-1

B-Raf inhibitor
HG6-64-1 is a potent and selective B-Raf and mutant B-Raf inhibitor; more information can be found in Patent WO 2011090738.
A11211

ML 786 dihydrochloride

Raf inhibitor
ML 786 dihydrochloride is a potent Raf kinase inhibitor (IC50 values are 2.1, 2.5 and 4.2 nM for B-RafV600E, C-Raf and wild-type B-Raf respectively).
A15855

PLX7904

Raf inhibitor
PLX7904 is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF melanoma cells but does not hyperactivate ERK1/2 in mutant RAS-expressing cells.
A15059 SALE

Dabrafenib Mesylate

Raf inhibitor
Dabrafenib Mesylate is a novel, potent, and selective Raf kinase inhibitor that is capableof inhibiting the kinase activity of wild-type B-Raf, B-RafV600Eand c-Raf with IC50 values of 3.2, 0.8, and 5.0 nM, respectively.
A15040

CEP-32496 hydrochloride

Raf Inhibitor
CEP-32496 hydrochloride is a highly potent inhibitor of wild-type BRAF, V600E mutant BRAF and c-Raf with Kd values of 14 nM, 36 nM and 39 nM, respectively.
A14122 SALE

B-Raf-inhibitor 1

B-Raf inhibitor
B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively
A14019

RO5126766 (CH5126766)

Raf/MEK dual inhibitor
RO5126766, also known as CH5126766, is a protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity.
A13323

TAK-632

pan-RAF inhibitor
TAK-632 is a potent pan-RAF inhibitor with favorable in vitro activity (BRAF(V600E) IC50, 2.4 nM; BRAF(wt), 8.3 nM; CRAF, 1.4 nM; pMEK (A375) IC50, 12 nM; pMEK (HMVII), 49 nM; V/B ratio.
A13119

Balamapimod (MKI-833)

Ras/Raf/MEK inhibitor
Balamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor.
A11381 SALE

Dabrafenib (GSK2118436A)

Raf inhibitor
Dabrafenib is a potent and selective inhibitor of B-RAF protein kinase carrying V600E mutation, currently in clinical trial.
A11436 SALE

GW 5074

Raf-1 Inhibitor
GW 5074 is a potent, selective and cell-permeable c-Raf1 kinase inhibitor
A11240

MLN2480 (BIIB-024)

pan-Raf inhibitor
MLN 2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials.
A12739

PF-04880594

RAF inhibitor
PF-04880594 is an inhibitor of RAF with IC50 values of 0.19 nM/0.13 nM and 0.39 nM for BRAF/BRAFV599E and c-RAF, respectively.
A12891

Diazepinomicin

RAS/RAF/MAPK inhibitor
Diazepinomicin, also known as TLN-4601, is a small-molecule inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity.
A13525

L-779450

Raf inhibitor
L-779450 is a raf kinase inhibitor, a potential treatment for neurotraumatic diseases.
A11333

BRAF inhibitor

BRAF inhibitor
BRAF inhibitor is a potent BRAF inhibitor.
A13772 SALE

CEP-32496

Raf inhibitor
CEP-32496 is an orally available v-raf murine sarcoma viral oncogene homolog B1 (B-raf) serine/threonine protein kinase inhibitor with potential antineoplastic activity.
A15218

Regorafenib monohydrate

Tyrosine kinase inhibitor
Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
A10774

Raf265 derivative

RAF/VEGFR Inhibitor
Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM.
A10661 SALE

NVP-BHG712

EphB4 inhibitor
NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.
A10250 SALE

Regorafenib (BAY 73-4506)

VEGFR inhibitor
Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.
A10001 SALE

Sorafenib (Nexavar)

Raf inhibitor
Sorafenib (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.
A10002

PLX-4720

Raf inhibitor
PLX-4720 is a B-raf inhibitor with IC50 of 160 nM.
A10739 SALE

PLX4032 (Vemurafenib)

Raf inhibitor
PLX4032 (Vemurafenib) also known as RG7204, Vemurafenib, R7204; RO5185426. PLX4032 is a B-raf inhibitor with an IC50 of 44 nM.
A10773 SALE

RAF265 (CHIR-265)

RAF/VEGFR Inhibitor
RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers.
A10420 SALE

GDC-0879

B-Raf inhibitor
GDC-0879 is a specific inhibitor of B-Raf kinase enzyme,targeting B-Raf (V600E) (IC50: 0.13 nM).
A11063

AZ628

Raf inhibitor
AZ628 is a RAF inhibitor with IC50 values: ca 30 nM for BRAF V600E and wild-type CRAF and 100 nM for wild-type BRAF.
A10829

SB590885

B-Raf Inhibitor
SB590885 is a selective small-molecule inhibitor of the B-Raf kinase and Ki app values are 0.16 and 1.72 nM for B-Raf and c-Raf respectively.
A11077 SALE

ZM 336372

C-Raf inhibitor
ZM 336372 is a potent ATP-competitive inhibitor of Raf-1 in vitro (IC50 = 70 nM) with the paradoxical effect of inducing >100-fold activation of Raf-1 in whole cells.
A16079

Locostatin

RKIP/Raf1 inhibitor
Locostatin is a cell permeable, potent inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration.

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