Raf
Catalog No. | Inhibitor Name | Raf | C-Raf/Raf-1 | B-Raf | A-raf | Other |
---|---|---|---|---|---|---|
A10739 | Vemurafenib | * | ** | SRMS,ACK1,MAP4K5 (KHS1) | ||
A10002 | PLX-4720 | *** | *** | BRK,FRK,CSK | ||
A11381 | Dabrafenib | **** | **** | |||
A10420 | GDC-0879 | **** | ||||
A10773 | RAF265 | ** | VEGFR2 | |||
A11063 | AZ 628 | ** | ** | |||
A10661 | NVP-BHG712 | * | EphB4,c-Src,c-Abl | |||
A10829 | SB590885 | **** | ||||
A11077 | ZM 336372 | * | ||||
A10001 | Sorafenib | **** | ** | mVEGFR2(Flk1),mVEGFR3,mPDGFRβ | ||
A11436 | GW5074 | *** | ||||
A13323 | TAK-632 | **** | *** | Aurora B,PDGFRβ,FGFR3 | ||
A13772 | CEP-32496 | ** | *** | RET,PDGFRβ,LCK | ||
A13226 | Encorafenib | **** | ||||
A14019 | RO5126766 | * | *** | MEK1 | ||
A15855 | PLX7904 | |||||
A11240 | MLN2480 | |||||
A10250 | Regorafenib (BAY 73-4506) | **** | ** | FGFR1, Kit, PDGFRβ, RET, Tie-2 , VEGFR1, VEGFR2, VEGFR3 | ||
A11211 | ML 786 dihydrochloride | **** | **** | Abl-1, DDR2, EPHA2, RET, PERK | ||
A12739 | PF-04880594 | **** | **** | |||
A13525 | L-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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LUT014
Catalog No. A19449 B-Raf inhibitorLUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, and developed to reduce dose-limiting acneiform lesions associated EGFR Inhibitors treatment. Extracted from patent WO 2019026065A2 . Learn More -
TAK-632
Catalog No. A13323 pan-RAF inhibitorTAK-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. Learn More -
RO5126766 (CH5126766)
Catalog No. A14019 Raf/MEK dual inhibitorRO5126766, 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. Learn More -
Regorafenib (BAY 73-4506)
Catalog No. A10250 VEGFR inhibitorRegorafenib (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. Learn More -
CEP-32496 hydrochloride
Catalog No. A15040 Raf InhibitorCEP-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. Learn More -
Dabrafenib Mesylate
Catalog No. A15059 Raf inhibitorDabrafenib 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. Learn More -
PLX7904
Catalog No. A15855 Raf inhibitorPLX7904 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. Learn More -
ML 786 dihydrochloride
Catalog No. A11211 Raf inhibitorML 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). Learn More -
HG6-64-1
Catalog No. A16022 B-Raf inhibitorHG6-64-1 is a potent and selective B-Raf and mutant B-Raf inhibitor; more information can be found in Patent WO 2011090738. Learn More -
B-Raf-inhibitor 1
Catalog No. A14122 B-Raf inhibitorB-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 Learn More -
ERK-IN-1
Catalog No. A19080 RAF/ERK1/2 inhibitorERK-IN-1 (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. Learn More -
RAF mutant-IN-1
Catalog No. A19011 Raf nhibitorRAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF340D/Y341D, B-RAFV600E and B-RAFWT, respectively. Learn More -
Belvarafenib
Catalog No. A13177 pan RAF inhibitorBelvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. Learn More -
Regorafenib Hydrochloride
Catalog No. A11546 VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitorRegorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. Learn More -
LY3009120
Catalog No. A16603 pan RAF inhibitorLY3009120 is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively. Learn More -
B-Raf IN 1
Catalog No. A21055 B-Raf kinase inhibitorB-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM. Learn More -
B-Raf inhibitor 1 dihydrochloride
Catalog No. A21834 Raf kinase inhibitorB-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively. Learn More -
Lifirafenib
Catalog No. A20988 Raf/EGFR inhibitorLifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively. Learn More -
Sorafenib Tosylate (Nexavar)
Catalog No. A10001 Raf inhibitorSorafenib Tosylate (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. Learn More -
LGX 818 (Encorafenib)
Catalog No. A13226 Selective B-RAF InhibitorLGX818 is an orally available Raf kinase inhibitor with potential antineoplastic activity. Learn More -
PLX4032 (Vemurafenib)
Catalog No. A10739 Raf inhibitorPLX4032 (Vemurafenib) also known as RG7204, Vemurafenib, R7204; RO5185426. PLX4032 is a B-raf inhibitor with an IC50 of 44 nM. Learn More -
Dabrafenib (GSK2118436A)
Catalog No. A11381 Raf inhibitorDabrafenib is a potent and selective inhibitor of B-RAF protein kinase carrying V600E mutation, currently in clinical trial. Learn More -
NVP-BHG712
Catalog No. A10661 EphB4 inhibitorNVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3. Learn More -
Balamapimod (MKI-833)
Catalog No. A13119 Ras/Raf/MEK inhibitorBalamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor. Learn More -
LXH254
Catalog No. A16841 pan-RAF inhibitorLXH254 is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays. Learn More -
PLX-4720
Catalog No. A10002 Raf inhibitorPLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf. Learn More -
RAF265 (CHIR-265)
Catalog No. A10773 RAF/VEGFR InhibitorRAF265 (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. Learn More -
GDC-0879
Catalog No. A10420 B-Raf inhibitorGDC-0879 is a specific inhibitor of B-Raf kinase enzyme,targeting B-Raf (V600E) (IC50: 0.13 nM). Learn More -
AZ628
Catalog No. A11063 Raf inhibitorAZ628 is a RAF inhibitor with IC50 values: ca 30 nM for BRAF V600E and wild-type CRAF and 100 nM for wild-type BRAF. Learn More -
SB590885
Catalog No. A10829 B-Raf InhibitorSB590885 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. Learn More -
ZM 336372
Catalog No. A11077 C-Raf inhibitorZM 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. Learn More -
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New
AZ304
Catalog No. A17225 dual BRAF inhibitorAZ304 is a potent dual BRAF inhibitor targeting the kinase domains of wild type BRAF, V600E mutant BRAF. AZ304 exerted potent inhibitory effects on both wild type and V600E mutant forms of the serine/threonine-protein kinase BRAF, with IC50 values of 79?nM and 38?nM, respectively. Learn More -
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Lifirafenib (BGB-283)
Catalog No. A16844 BRAF inhibitorLifirafenib (BGB-283), also known as Beigene-283, potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant. Learn More -
RAF709
Catalog No. A16842 raf kinase inhibitorRAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), the only kinases with binding >80% at 1 μM. Learn More -
Locostatin
Catalog No. A16079 RKIP/Raf1 inhibitorLocostatin is a cell permeable, potent inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration. Learn More -
Raf265 derivative
Catalog No. A10774 RAF/VEGFR InhibitorRaf265 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. Learn More -
GW 5074
Catalog No. A11436 Raf-1 InhibitorGW 5074 is a potent, selective and cell-permeable c-Raf1 kinase inhibitor Learn More -
Regorafenib monohydrate
Catalog No. A15218 Tyrosine kinase inhibitorRegorafenib 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. Learn More -
MLN2480 (BIIB-024)
Catalog No. A11240 pan-Raf inhibitorMLN 2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials. Learn More -
PF-04880594
Catalog No. A12739 RAF inhibitorPF-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. Learn More -
CEP-32496
Catalog No. A13772 Raf inhibitorCEP-32496 is an orally available v-raf murine sarcoma viral oncogene homolog B1 (B-raf) serine/threonine protein kinase inhibitor with potential antineoplastic activity. Learn More -
Diazepinomicin
Catalog No. A12891 RAS/RAF/MAPK inhibitorDiazepinomicin, also known as TLN-4601, is a small-molecule inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity. Learn More -
BRAF inhibitor
Catalog No. A11333 -
L-779450
Catalog No. A13525 Raf inhibitorL-779450 is a raf kinase inhibitor, a potential treatment for neurotraumatic diseases. Learn More