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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
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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CitedLXH254 Cited
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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CitedRegorafenib Cited
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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CitedDabrafenib Cited
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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CitedVemurafenib Cited
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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CitedEncorafenib Cited
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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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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Xl-281
T68170870603-16-0In house
Xl-281 (BMS-908662) is a BRAF inhibitor with anti-tumor activity for the study of colorectal cancer and melanoma.
- $293
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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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RAS GTPase inhibitor 1 Cited
T126922252242-32-1In house
RAS GTPase inhibitor 1 is a RAS GTPase inhibitor with potential antitumor activity.
- $373
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CitedPLX-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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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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Dabrafenib Mesylate Cited
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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CitedDonafenib
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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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.
- $44
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Pluripotin
T6948839707-37-8
Pluripotin (SC1) (SC1), which keep embryonic stem cell (ESC) self-renewal, is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP.
- $30
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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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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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SB-590885 Cited
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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CitedGSK2008607
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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GSK1904529A Cited
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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CitedSorafenib tosylate Cited
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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CitedGDC-0879
T6320905281-76-7
GDC-0879 (AR-00341677) is a novel, potent and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well.
- $32
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Doramapimod Cited
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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CitedBelvarafenib
Cited
T56341446113-23-0
Belvarafenib (HM95573) is a potent pan-RAF inhibitor with antitumor activity and inhibits B-RAF, B-RAFv600E, and C-RAF with IC50 values of 56, 7, and 5 nM.
- $34
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CitedPelitinib Cited
T2327257933-82-7
Pelitinib (EKB-569) (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
- $43
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CitedRo 5126766
T6971946128-88-7
RO5126766 (CH5126766) is a dual RAF MEK inhibitor with IC50 of 8.2 nM, 19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.
- $52
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AZ 628
T6318878739-06-1
AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.
- $38
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Sulindac sulfide
T1303749627-27-2In house
Sulindac sulfide (cis-Sulindac sulfide) is a non-steroidal anti-inflammatory compound that has a high affinity for COX-1 and acts as an inhibitor in Ras activation of Raf-1. Sulindac sulfide is a non-competitive inhibitor of gamma-secretase with an IC50 value of 20.2 μM. It is an active metabolite of sulinic acid.
- $31
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AD80 Cited
T43011384071-99-1
AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.
- $39
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CitedTBAP-001
T96931777832-90-2
TBAP-001 is a RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay and an IC50 of 18 nM in Cell-Based Phosho-ERK Assay.
- $41
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GW 5074 Cited
T6525220904-83-6
GW 5074 (Raf1 Kinase Inhibitor I)(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 c-Fms.
- $36
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CitedMRTX0902
T97552654743-22-1
MRTX0902 is an effective and high selective inhibitor of SOS1 with an IC50 of 46 nM and a Ki of 2 nM.
- $87
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GW 441756
T6052504433-23-2
GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.
- $51
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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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Claturafenib
T2010812754408-94-9
Claturafenib (PF-07799933) is a brain-permeable, selective, all-mutant BRAF inhibitor with broad inhibitory effects on pERK levels in HT29 cells.Claturafenib has shown antitumor activity in preclinical studies in both BRAF V600- and non-V600-mutant cancers and can be used in combination with MEK inhibitors.
- $81
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Lonafarnib Cited
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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CitedRAF265
T6296927880-90-8
RAF265 (CHIR-265) (CHIR-265) is a potent selective inhibitor of C-Raf B-Raf B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM. Phase 2.
- $39
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SOS1-IN-11
T600292654741-64-5
SOS1-IN-11 is an effective inhibitor of SOS1 (IC50 = 30 nM).
- $69
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BAY-293 Cited
T54182244904-70-7
BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM).
- $48
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CitedAgerafenib
T20701188910-76-0
Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.
- $35
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Plx-4032
T86541029872-54-5
Plx-4032 (Vemurafenib) is a small-molecule B-Raf inhibitor for the potential treatment of malignant melanoma.
- $50
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SGX-523 Cited
T22931022150-57-7
SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
- $30
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CitedLY3009120
T68821454682-72-4
LY3009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 values of 44 nM for A-raf, 31-47 nM for B-Raf, and 42 nM for C-Raf in A375 cells. Phase 1.
- $30
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Rineterkib Cited
T112241715025-32-3
Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1 2 activating mutations in the MAPK pathway.
- $96
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CitedMCP110
T24437521310-51-0
MCP110 is an inhibitor of the interaction of Ras with Raf-1 and can be used in studies about the treatment of human tumors.
- $31
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PLX7904
T69491393465-84-3
PLX7904 (PB04), 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 melanoma cells but does not hyperactivate ERK1 2 in mutant RAS-expressing cells.
- $42
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