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(221)
MAPKRaf
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.
Sorafenib
T0093L284461-73-0
Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.
- $34
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Regorafenib
T1792755037-03-7
Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.
- $30
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LXH254
T118981800398-38-2
LXH254 is a B C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.
- $48
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Vemurafenib
T2382918504-65-1
Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31 48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.
- $50
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Dabrafenib
T19031195765-45-7
Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5 0.6 nM) and is ATP-competitive. Dabrafenib exhibits antitumor activity for the treatment of B-RafV600E-mutated melanoma.
- $41
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Encorafenib
T64871269440-17-6
Encorafenib (LGX818) is an orally available mutated BRaf V600E inhibitor(IC50=0.3 nM) with potential antineoplastic activity.
- $47
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Lonafarnib
T6302193275-84-2
Lonafarnib (Sch66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9 5.2 2.8 nM).
- $41
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NVP-BHG712
T6348940310-85-0
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 c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
- $30
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PLX-4720
T2473918505-84-7
PLX-4720 is a potent and selective B-Raf (V600E) inhibitor designed to block the ATP-binding site of oncogenic B-Raf with IC50 of 13 nM.
- $32
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Exarafenib
T636442639957-39-2
Exarafenib (RAF KIN_2787) is a potent, orally available pan-RAF inhibitor with antitumor activity that acts by inhibiting downstream MAPK pathway signaling. It is used in cancer research.
- $131
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Dabrafenib Mesylate
T84741195768-06-9
Dabrafenib Mesylate (GSK2118436 Mesylate) is a B-Raf inhibitor(IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively).
- $40
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cct241161
T96381163719-91-2In house
CCT241161 is an orally active pan-RAF inhibitor, with IC50 values of 3, 6, 10, 15, and 30 nM for LCK, CRAF, SRC, V600E-BRAF, and BRAF, respectively. It exhibits significant activity against BRAF and NRAS mutant melanomas and demonstrates anticancer cell proliferative effects [1].
- $139
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Donafenib
T169091130115-44-4
Donafenib (Bay 43-9006 (D3)) is a deuterium-labeled Sorafenib which is a multikinase inhibitor(IC50s: 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively).
- $84
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GSK2008607
T274541244644-50-5In house
GSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers.
- $350
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protac braf-v600e degrader-1
T87452417296-84-3
PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.
- $115
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SB-590885
T2295405554-55-4
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 other human kinases.
- $36
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Pepinh-TRIF TFA
T76089
Pepinh-TRIF TFA is a 30 aa peptide associated with the immune system that blocks TRIF signaling by interfering with TLR-TRIF interaction (TLR-TRIF interaction ).
- $128
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Sorafenib tosylate
T0093475207-59-1
Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6 20 22 nM for Raf-1 VEGFR-3 B-Raf).
- $37
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Brimarafenib
T891161643326-82-2
Brimarafenib is a selective RAF dimerization inhibitor, which can inhibit the activity of BRAF and CRAF, and exhibits significant inhibitory effects on a variety of RAF mutations (including BRAF I II III mutations, BRAF fusion and CRAF heterodimerization), and is used for the treatment of colorectal and pancreatic cancers and other solid tumors with MAPK mutations.
- $190
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PLX8394
T35791393466-87-9
Plixorafenib (PLX8394) is an orally active inhibitor of the serine threonine protein kinase B-Raf (BRAF) protein.Plixorafenib can selectively bind to and inhibit the activity of wild-type and mutant forms of BRAF, inhibiting the proliferation of tumor cells expressing mutant forms of BRAF.
- $35
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Doramapimod
T6277285983-48-4
Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.
- $31
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GSK1904529A
T60031089283-49-7In house
GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .
- $34
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AD80
T43011384071-99-1
AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.
- $39
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Indirubin
T6169479-41-4
Indirubin (Couroupitine B) is a potent inhibitor of cyclin-dependent kinases and GSK-3β, with IC50 values of approximately 5 µM and 0.6 µM, respectively.
- $45
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