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MAPK Raf

Raf

RAF kinases are a family of three serine/threonine-specific protein kinases that are related to retroviral oncogenes. The mouse sarcoma virus 3611 contains a RAF kinase-related oncogene that enhances fibrosarcoma induction. RAF is an acronym for Rapidly Accelerated Fibrosarcoma. RAF kinases participate in the RAS-RAF-MEK-ERK signal transduction cascade, also referred to as the mitogen-activated protein kinase (MAPK) cascade. Activation of RAF kinases requires interaction with RAS-GTPases.
Cat No. product name
T0078 LapatinibHOT Lapatinib is a dual ErbB2/EGFR (IC50: 9.2/10.8 nM) inhibitor.
T10567 BMS-214662 BMS-214662 is an effective and selective inhibitor of farnesyl transferase with potent antitumor activity (IC50: 1.35 nM).
T10599 BRAF inhibitor BRAF inhibitor is an inhibitor of B-Raf extracted from patent WO/2011103196 A1 (Compound P-0850).
T11224 ERK-IN-1 ERK-IN-1  is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is...
T11898 LXH254 LXH254 is a potent B/C RAF inhibitor.
T12556 PROTAC B-Raf degrader 1 PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf,PROTAC B-Raf degrader 1 With anti-cancer activity.
T12978 SOS1-IN-1 SOS1-IN-1 is an inhibitor of SOS1.
T13406L Zabofloxacin hydrochloride Zabofloxacin hydrochloride is a potent and seletive bacterial type II and IV topoisomerases inhibitor, has excellent activity against gram-positive pathogens in...
T15804 LY2452473 LY2452473 is an orally bioavailable and selective androgen receptor modulator.
T1792 RegorafenibHOT Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor (IC50s: 1.5/2.5/4.2/7/13/22 nM for RET/C-RAF/VEGFR2/c-Kit/VEGFR1/PDGFRβ).
T1845 B-Raf IN 1 B-Raf IN 1 is a B-Raf (IC50: 24 nM) and c-Raf (IC50: 25 nM) inhibitor.
T1851 ZM 336372 ZM 336372 is a potent and selective c-Raf inhibitor.
T1876 Kobe0065 Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; shows potent activity to competitively inhibit the binding o...
T1886 TAK632 TAK-632 is a potent pan-Raf inhibitor.
T1892 Kobe2602 Kobe 2602 is an inhibitor of Ras that exhibits anticancer chemotherapeutic activities.
T1903 DabrafenibHOT Dabrafenib is a selective inhibitor of mutated forms of BRAF kinase (IC50s: 0.7/5 nM for B-Raf (V600E)/C-Raf).
T1953 L-779450 L-779450, an effective, ATP-competitive Raf kinase inhibitor (IC50: 10 nM) , displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectivel...
T2074 B-Raf inhibitor 1 B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor.
T2293 SGX-523 SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
T2295 SB590885 SB590885 is an effective B-Raf inhibitor (Ki: 0.16 nM, in a cell-free assay). The selectivity of SB590885 for B-Raf is 11-fold greater over c-Raf, no acts to ot...
T2327 Pelitinib Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
T2382 VemurafenibHOT Vemurafenib (PLX4032) is a novel and potent B-Raf (V600E) inhibitor (IC50: 31 nM).
T2473 PLX4720HOT PLX-4720 is a potent and selective inhibitor of B-Raf (V600E) (IC50: 13 nM), equally potent to c-Raf-1(Y340D and Y341D mutations).
T2624 OSI 930 OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel...
T3641 BAW2881 BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and a...
T3711 RAF709 RAF709 is a novel Raf kinase inhibitor with IC50s of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
T3725 K-Ras(G12C) Inhibitor 6 K-Ras(G12C) inhibitor 6 is an irreversible, allosteric inhibitor of the K-Ras(G12C) mutant. K-Ras(G12C) inhibitor 6 (10 µM, 24 h) causes 100% modification of t...
T4133 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
T4167 B-Raf inhibitor 1 dihydrochloride B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor.
T4301 AD80 AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
T5172 AZ304 AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits BRAF (WT), BRAF (V600E), and wild type CRAF (IC50s: 79/38/68 nM).
T5418 BAY-293 BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM).
T5634 Belvarafenib Belvarafenib is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and ...
T6003 GSK1904529A GSK1904529A is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .
T6052 GW 441756 GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.
T6169 Indirubin Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 uM and 0.6 uM.
T6302 Lonafarnib Lonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9/5.2/2.8 nM).
T6320 GDC-0879 GDC-0879 is a novel, potent and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well.
T6348 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 ...
T6487 Encorafenib LGX818 is an orally available mutated BRaf V600E inhibitor(IC50=0.3 nM) with potential antineoplastic activity.
T6525 GW5074 GW5074(IC50=9 nM) is an effective and specific c-Raf inhibitor. It has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or ...
T6555 K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).
T6556 K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
T6882 LY3009120 LY03009120 is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.
T6895 MLN2480 MLN2480 is an oral, selective pan-Raf kinase inhibitor in clinical trials.
T6948 Pluripotin Pluripotin (SC1), which keep embryonic stem cell (ESC) self-renewal, is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP.
T6949 PLX7904 PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF mela...
T7414 ARS-853 ARS-853 is an inhibitor of K-RASG12C(IC50 : 2.5 μM), a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells
T8402 Regorafenib Hydrochloride Regorafenib Hydrochloride is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor a...
T8474 Dabrafenib Mesylate Dabrafenib Mesylate is a B-Raf inhibitor(IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively).
T8654 Plx-4032 PLX-4032 is a small-molecule B-Raf inhibitor for the potential treatment of malignant melanoma.
T8721 Pyrido[4,3-d]pyrimidin-7(6H)-one, 2-methyl-6-(1-methylcyclopropyl)-4-[[(1R)-1-[2-methyl-3-(trifluoromethyl)phenyl]ethyl]amino]- Pyrido[4,3-d]pyrimidin-7(6H)-one, 2-methyl-6-(1-methylcyclopropyl)-4-[[(1R)-1-[2-methyl-3-(trifluoromethyl)phenyl]ethyl]amino]- is a SOS1 inhibitor and is a nov...
TN2114 Pseudoginsenoside Rh2 Pseudoginsenoside Rh2 has cytotoxicity, it induces mitochondrial apoptosis in A549 cells and is responsible for excessive activation of the Ras/Raf/ERK/p53 path...
TN4166 Griffipavixanthone Griffipavixanthone inhibits the growth of human Non-small-cell lung cancer H520 cells in dose- and time-dependent manners, it induces cell apoptosis through mit...
TQ0048 BI-882370 BI-882370 is a specific RAF kinase inhibitor. BI-882370 inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases (IC50s: 0.4, 0.8 and 0.6 nM). BI-8...
Lapatinib HOT
T0078CAS 231277-92-2
Lapatinib is a dual ErbB2/EGFR (IC50: 9.2/10.8 nM) inhibitor.
BMS-214662
T10567CAS 195987-41-8
BMS-214662 is an effective and selective inhibitor of farnesyl transferase with potent antitumor activity (IC50: 1.35 nM).
BRAF inhibitor
T10599CAS 918505-61-0
BRAF inhibitor is an inhibitor of B-Raf extracted from patent WO/2011103196 A1 (Compound P-0850).
ERK-IN-1
T11224CAS 1715025-32-3
ERK-IN-1  is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is...
LXH254
T11898CAS 1800398-38-2
LXH254 is a potent B/C RAF inhibitor.
PROTAC B-Raf degrader 1
T12556CAS 2364367-27-9
PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf,PROTAC B-Raf degrader 1 With anti-cancer activity.
SOS1-IN-1
T12978CAS 4551-00-2
SOS1-IN-1 is an inhibitor of SOS1.
Zabofloxacin hydrochloride
T13406LCAS 623574-00-5
Zabofloxacin hydrochloride is a potent and seletive bacterial type II and IV topoisomerases inhibitor, has excellent activity against gram-positive pathogens in...
LY2452473
T15804CAS 1029692-15-6
LY2452473 is an orally bioavailable and selective androgen receptor modulator.
Regorafenib HOT
T1792CAS 755037-03-7
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor (IC50s: 1.5/2.5/4.2/7/13/22 nM for RET/C-RAF/VEGFR2/c-Kit/VEGFR1/PDGFRβ).
B-Raf IN 1
T1845CAS 950736-05-7
B-Raf IN 1 is a B-Raf (IC50: 24 nM) and c-Raf (IC50: 25 nM) inhibitor.
ZM 336372
T1851CAS 208260-29-1
ZM 336372 is a potent and selective c-Raf inhibitor.
Kobe0065
T1876CAS 436133-68-5
Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; shows potent activity to competitively inhibit the binding o...
TAK632
T1886CAS 1228591-30-7
TAK-632 is a potent pan-Raf inhibitor.
Kobe2602
T1892CAS 454453-49-7
Kobe 2602 is an inhibitor of Ras that exhibits anticancer chemotherapeutic activities.
Dabrafenib HOT
T1903CAS 1195765-45-7
Dabrafenib is a selective inhibitor of mutated forms of BRAF kinase (IC50s: 0.7/5 nM for B-Raf (V600E)/C-Raf).
L-779450
T1953CAS 303727-31-3
L-779450, an effective, ATP-competitive Raf kinase inhibitor (IC50: 10 nM) , displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectivel...
B-Raf inhibitor 1
T2074CAS 1093100-40-3
B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor.
SGX-523
T2293CAS 1022150-57-7
SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
SB590885
T2295CAS 405554-55-4
SB590885 is an effective B-Raf inhibitor (Ki: 0.16 nM, in a cell-free assay). The selectivity of SB590885 for B-Raf is 11-fold greater over c-Raf, no acts to ot...
Pelitinib
T2327CAS 257933-82-7
Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
Vemurafenib HOT
T2382CAS 918504-65-1
Vemurafenib (PLX4032) is a novel and potent B-Raf (V600E) inhibitor (IC50: 31 nM).
PLX4720 HOT
T2473CAS 918505-84-7
PLX-4720 is a potent and selective inhibitor of B-Raf (V600E) (IC50: 13 nM), equally potent to c-Raf-1(Y340D and Y341D mutations).
OSI 930
T2624CAS 728033-96-3
OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel...
BAW2881
T3641CAS 861875-60-7
BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and a...
RAF709
T3711CAS 1628838-42-5
RAF709 is a novel Raf kinase inhibitor with IC50s of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
K-Ras(G12C) Inhibitor 6
T3725CAS 2060530-16-5
K-Ras(G12C) inhibitor 6 is an irreversible, allosteric inhibitor of the K-Ras(G12C) mutant. K-Ras(G12C) inhibitor 6 (10 µM, 24 h) causes 100% modification of t...
CCT196969
T4133CAS 1163719-56-9
CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
B-Raf inhibitor 1 dihydrochloride
T4167CAS 1191385-19-9
B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor.
AD80
T4301CAS 1384071-99-1
AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
AZ304
T5172CAS 942507-42-8
AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits BRAF (WT), BRAF (V600E), and wild type CRAF (IC50s: 79/38/68 nM).
BAY-293
T5418CAS 2244904-70-7
BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM).
Belvarafenib
T5634CAS 1446113-23-0
Belvarafenib is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and ...
GSK1904529A
T6003CAS 1089283-49-7
GSK1904529A is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .
GW 441756
T6052CAS 504433-23-2
GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.
Indirubin
T6169CAS 479-41-4
Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 uM and 0.6 uM.
Lonafarnib
T6302CAS 193275-84-2
Lonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9/5.2/2.8 nM).
GDC-0879
T6320CAS 905281-76-7
GDC-0879 is a novel, potent and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well.
NVP-BHG712
T6348CAS 940310-85-0
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 ...
Encorafenib
T6487CAS 1269440-17-6
LGX818 is an orally available mutated BRaf V600E inhibitor(IC50=0.3 nM) with potential antineoplastic activity.
GW5074
T6525CAS 220904-83-6
GW5074(IC50=9 nM) is an effective and specific c-Raf inhibitor. It has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or ...
K-Ras(G12C) inhibitor 12
T6555CAS 1469337-95-8
K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).
K-Ras(G12C) inhibitor 9
T6556CAS 1469337-91-4
K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
LY3009120
T6882CAS 1454682-72-4
LY03009120 is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.
MLN2480
T6895CAS 1096708-71-2
MLN2480 is an oral, selective pan-Raf kinase inhibitor in clinical trials.
Pluripotin
T6948CAS 839707-37-8
Pluripotin (SC1), which keep embryonic stem cell (ESC) self-renewal, is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP.
PLX7904
T6949CAS 1393465-84-3
PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor. It is able to efficiently inhibit activation of ERK1/2 in mutant BRAF mela...
ARS-853
T7414CAS 1629268-00-3
ARS-853 is an inhibitor of K-RASG12C(IC50 : 2.5 μM), a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells
Regorafenib Hydrochloride
T8402CAS 835621-07-3
Regorafenib Hydrochloride is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor a...
Dabrafenib Mesylate
T8474CAS 1195768-06-9
Dabrafenib Mesylate is a B-Raf inhibitor(IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively).
Plx-4032
T8654CAS 1029872-54-5
PLX-4032 is a small-molecule B-Raf inhibitor for the potential treatment of malignant melanoma.
Pyrido[4,3-d]pyrimidin-7(6H)-one, 2-methyl-6-(1-methylcyclopropyl)-4-[[(1R)-1-[2-methyl-3-(trifluoromethyl)phenyl]ethyl]amino]-
T8721CAS 2359690-13-2
Pyrido[4,3-d]pyrimidin-7(6H)-one, 2-methyl-6-(1-methylcyclopropyl)-4-[[(1R)-1-[2-methyl-3-(trifluoromethyl)phenyl]ethyl]amino]- is a SOS1 inhibitor and is a nov...
Pseudoginsenoside Rh2
TN2114CAS 1370264-16-6
Pseudoginsenoside Rh2 has cytotoxicity, it induces mitochondrial apoptosis in A549 cells and is responsible for excessive activation of the Ras/Raf/ERK/p53 path...
Griffipavixanthone
TN4166CAS 219649-95-3
Griffipavixanthone inhibits the growth of human Non-small-cell lung cancer H520 cells in dose- and time-dependent manners, it induces cell apoptosis through mit...
BI-882370
TQ0048CAS 1392429-79-6
BI-882370 is a specific RAF kinase inhibitor. BI-882370 inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases (IC50s: 0.4, 0.8 and 0.6 nM). BI-8...