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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.



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Catalog No. Product Name Application Product Information
A13226

LGX 818 (Encorafenib)

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

HG6-64-1

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

Dabrafenib (GSK2118436A)

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

MLN2480 (BIIB-024)

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

PF-04880594

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

BRAF inhibitor

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

CEP-32496

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

PLX4032 (Vemurafenib)

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

AZ628

Raf 抑制剂
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 抑制剂
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 抑制剂
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 抑制剂
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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