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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.
- SorafenibT0093L284461-73-0Sorafenib (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.
- $27.2
- $34
SizeQTY
Cited - RegorafenibT1792755037-03-7Regorafenib (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
SizeQTY Cited - BelvarafenibT56341446113-23-0Belvarafenib 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 C-RAF respectively.
- $40
SizeQTY - PLX-4720T2473918505-84-7PLX-4720, a potent and selective inhibitor of B-Raf (V600E) with an IC50 of 13 nM, is equally effective against c-Raf-1 (Y340D and Y341D mutations).
- $32
SizeQTY - Sorafenib tosylateT0093475207-59-1Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
- $37
SizeQTY Cited - Regorafenib monohydrateT1792L1019206-88-2Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.
- $30
SizeQTY - Dabrafenib MesylateT84741195768-06-9Dabrafenib Mesylate (GSK2118436 Mesylate) is a B-Raf inhibitor(IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively).
- $40
SizeQTY - VemurafenibT2382918504-65-1Vemurafenib (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
SizeQTY Cited - Regorafenib HydrochlorideT8402835621-07-3Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity
- $30
SizeQTY - Plx-4032T86541029872-54-5Plx-4032 (Vemurafenib) is a small-molecule B-Raf inhibitor for the potential treatment of malignant melanoma.
- $50
SizeQTY - DabrafenibT19031195765-45-7Dabrafenib (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
SizeQTY
Cited - RAS GTPase inhibitor 1T126922252242-32-1RAS GTPase inhibitor 1 is a RAS GTPase inhibitor with potential antitumor activity.
- $373
SizeQTY Cited - KRPEP-2D acetateTP2358KRPEP-2D acetate was identified as a K-Ras(G12D) selective inhibitory peptide against the G12D mutant of K-Ras, which is a key member of the Ras protein family and an attractive cancer therapeutic target.
- $76
SizeQTY - I-37 free base( 2359690-13-2(free base))T8721LI-37 free base is a novel benzylamino substituted pyridopyrimidinone as SOS1 inhibitor.
- $133
SizeQTY - I-49 free baseT8746LI-49 free base (Pyrido[4,3-d]pyrimidin-7(6H)-one, 2-methyl-4-[[(1R)-1-[2-methyl-3-(trifluoromethyl)phenyl]ethyl]amino]-6-(tetrahydro-2H-pyran-4-yl)-) is a novel benzylamino substituted pyridopyrimidinone as SOS1 inhibitor.
- $133
SizeQTY - B-Raf IN 16T798302304746-24-3B-Raf IN 16, a BRAF inhibitor, belongs to cyclic iminopyrimidine derivatives and can be used for cancer or tumour research.
- $195
SizeQTY - GSK2008607T274541244644-50-5In houseGSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers.
- $350
SizeQTY - CCT241161T96381163719-91-2CCT241161 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
SizeQTY - B-Raf IN 15T78183832107-31-0B-Raf IN 15 is a BRAF inhibitor that inhibits BRAFWT and BRAFV600E and can be used in the study of melanoma and cancer, and can be optimized for use as a more effective BRA F inhibitor.
- $52
SizeQTY - B-Raf IN 13T678622573782-74-6B-Raf IN 13 is a potent B-Raf inhibitor with anticancer activity, demonstrating an IC50 of 3.55 nM in the [BRAF V600E] enzyme assay.
- $1,520
SizeQTY - GSK1904529AT60031089283-49-7In houseGSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .
- $34
SizeQTY Cited - BMS-214662T10567195987-41-8In houseBMS-214662 is a potent and selective farnesyl transferase inhibitor that induces mitochondrial apoptosis in primitive CD34+ chronic myeloid leukemia (CML) stem cells progenitors and selectively targets CML stem cells progenitors with antitumor activity.
- $2,270
SizeQTY - Sulindac sulfideT1303749627-27-2Sulindac 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
SizeQTY - Xl-281T68170870603-16-0Xl-281 (BMS-908662) is a BRAF inhibitor with anti-tumor activity for the study of colorectal cancer and melanoma.
- $293
SizeQTY - EncorafenibT64871269440-17-6Encorafenib (LGX818) is an orally available mutated BRaf V600E inhibitor(IC50=0.3 nM) with potential antineoplastic activity.
- $47
SizeQTY Cited - GW 5074T6525220904-83-6GW 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
SizeQTY Cited - AD80T43011384071-99-1AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.
- $39
SizeQTY Cited - LonafarnibT6302193275-84-2Lonafarnib (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
SizeQTY Cited - DoramapimodT6277285983-48-4Doramapimod (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
SizeQTY Cited - RineterkibT112241715025-32-3Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1/2 activating mutations in the MAPK pathway.
- $96
SizeQTY Cited - Kobe0065T1876436133-68-5Kobe0065 is a novel and effective small-molecule compound that inhibits the Ras-Raf interaction by structure-based drug design (SBDD); it displays potent activity, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
- $39
SizeQTY Cited - LocostatinT8823133812-16-5Locostatin is a potent and cell permeable inhibitor of Raf kinase inhibitor protein (RKIP) Raf1 kinase interaction and an inhibitor of cell migration.
- $39
SizeQTY Cited - OSI-930T2624728033-96-3OSI-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 growth (angiogenesis) in tumors.
- $47
SizeQTY Cited - RAF709T37111628838-42-5RAF709 is a novel Raf kinase inhibitor with IC50s of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
- $34
SizeQTY Cited - PelitinibT2327257933-82-7Pelitinib (EKB-569) (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
- $43
SizeQTY Cited - SGX-523T22931022150-57-7SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
- $44
SizeQTY Cited - TAK-632T18861228591-30-7TAK-632, a potent pan-Raf inhibitor (GenScript, 2020), is characterized by its molecular weight [M] for [C 22 H 19 FN 2 O 2] of 362.4 by LC-MS, with a purity of 99% (HPLC). The compound exhibits white to off-white solid form and has a melting point [M] ranging from 178°C to 182°C (GenScript, 2020). Its solubility profile includes DMSO, in which it is soluble to 100mM (GenScript, 2020).
- $35
SizeQTY Cited - SB-590885T2295405554-55-4SB590885 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
SizeQTY Cited - KG5T41003877874-85-6KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.
- $48
SizeQTY - Ro 5126766T6971946128-88-7RO5126766 (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
SizeQTY - AZ304T5172942507-42-8AZ304 is an ATP-competitive dual BRAF kinase inhibitor, effectively inhibiting BRAF (WT), BRAF (V600E), and wild-type CRAF [IC50s: 79 38 68 nM].
- $42
SizeQTY - MRTX0902T97552654743-22-1MRTX0902 is an effective and high selective inhibitor of SOS1 with an IC50 of 46 nM and a Ki of 2 nM.
- $87
SizeQTY - K-Ras-IN-1T546984783-01-7K-Ras-IN-1, a K-Ras inhibitor, is characterized by its chemical formula C20H19ClN4O2S and is also known as N-[(1S)-3-cyclopropyl-1-[(6-fluoro-1H-benzimidazol-2-yl)sulfanyl]-2-oxo-1-(phenylmethyl)propyl]-4-fluorobenzenesulfonamide (compound [18, dashboard 819041] in brackets).
- $45
SizeQTY - GW 441756T6052504433-23-2GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.
- $51
SizeQTY - SOS1-IN-11T600292654741-64-5SOS1-IN-11 is an effective inhibitor of SOS1 (IC50 = 30 nM).
- $69
SizeQTY - B-Raf IN 1T1845950736-05-7B-Raf IN 1 is an inhibitor of B-Raf (IC50: 24 nM) and c-Raf (IC50: 25 nM).
- $84
SizeQTY - Raf inhibitor 2T4194220904-99-4Raf inhibitor 2 (CID 25014542) is novel inhibitor of Raf kinases.
- $39
SizeQTY - PROTAC BRAF-V600E degrader-1T87452417296-84-3PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.
- $191
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