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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.
T0093 Sorafenib tosylateHOT Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
T0093L SorafenibHOT Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-4/B-Raf).
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...
T4167 B-Raf inhibitor 1 dihydrochloride B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor.
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...
T4133 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
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 ...
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
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...
T8402 Regorafenib Hydrochloride Regorafenib Hydrochloride is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor a...
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...
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.
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...
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).
Lapatinib HOT
T0078CAS 231277-92-2
Lapatinib is a dual ErbB2/EGFR (IC50: 9.2/10.8 nM) inhibitor.
Sorafenib tosylate HOT
T0093CAS 475207-59-1
Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
Sorafenib HOT
T0093LCAS 284461-73-0
Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-4/B-Raf).
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...
B-Raf inhibitor 1 dihydrochloride
T4167CAS 1191385-19-9
B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor.
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...
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.
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 ...
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
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...
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...
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...
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.
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...
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).