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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
Cited
Bay 43-9006
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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CitedEncorafenib
Cited
LGX818
T64871269440-17-6
Encorafenib (LGX818) is an oral, highly selective inhibitor of the BRAF V600E mutation with an IC50 of 0.3 nM, exhibiting antitumor activity. Encorafenib can be used for studying tumor signaling pathway regulation and mechanisms of drug resistance.
- $47
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CitedDabrafenib Cited
GSK2118436A, GSK2118436
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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CitedRegorafenib Cited
Fluoro-Sorafenib, BAY 73-4506
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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CitedVemurafenib Cited
RO5185426, RG7204, PLX4032
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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CitedLonafarnib Cited
Sch66336, Sarasar
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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CitedDonafenib
Sorafenib-d3, Sorafenib (D3), Bay 43-9006 (D3)
T169091130115-44-4
Donafenib is a deuterium-labeled Sorafenib (T0093L) 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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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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Dabrafenib Mesylate
GSK2118436 Mesylate, GSK 2118436B
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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PROTAC BRAF-V600E degrader-1
Compound 23
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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Exarafenib
RAF/KIN_2787
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.
- $68
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PLX-4720
PLX4720
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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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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Rineterkib Cited
ERK-IN-1
T112241715025-32-3
Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1/2 activating mutations in the MAPK pathway.
- $84
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CitedPepinh-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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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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Doramapimod Cited
BIRB 796
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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CitedSorafenib tosylate Cited
Bay 43-9006
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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CitedBrimarafenib
Brimarafenibum, BGB-3245, BGB3245, BGB245, BGB 245
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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