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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.

  • Regorafenib
    T1792755037-03-7
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.
    • $30
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  • Sorafenib
    T0093L284461-73-0
    Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits 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. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic ferroptosis.
    • $34
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  • Belvarafenib
    T56341446113-23-0
    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 C-RAF respectively.
    • $40
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  • LXH254
    T118981800398-38-2
    LXH254 is a potent C-Raf and B-Raf inhibitor.
    • $48
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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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  • PLX-4720
    T2473918505-84-7
    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).
    • $32
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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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  • 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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  • KRPEP-2D acetate
    TP2358
    KRPEP-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
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  • RAS GTPase inhibitor 1
    T126922252242-32-1In house
    RAS GTPase inhibitor 1 is a RAS GTPase inhibitor with potential antitumor activity.
    • $373 TargetMol
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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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  • I-37 free base( 2359690-13-2(free base))
    T8721L
    I-37 free base is a novel benzylamino substituted pyridopyrimidinone as SOS1 inhibitor.
    • $133
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  • I-49 free base
    T8746L
    I-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
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  • B-Raf IN 16
    T798302304746-24-3In house
    B-Raf IN 16, a BRAF inhibitor, belongs to cyclic iminopyrimidine derivatives and can be used for cancer or tumour research.
    • $195 TargetMol
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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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  • 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 displays significant activity against BRAF and NRAS mutant melanomas, as well as demonstrating anticancer cell proliferative effects [1].
    • $139
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  • B-Raf IN 15
    T78183832107-31-0In house
    B-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
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  • B-Raf IN 13
    T678622573782-74-6In house
    B-Raf IN 13 is a potent B-Raf inhibitor with anticancer activity.B-Raf IN 13 has an IC50 of 3.55 nM in the BRAF V600E enzyme assay.
    • $1,520
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  • BMS-214662
    T10567195987-41-8In house
    BMS-214662 is a potent and selective farnesyl transferase inhibitor that induces mitochondrial apoptosis in primitive CD34+ chronic myeloid leukemia (CML) stem cells/progenitors, and has the ability to selectively target CML stem cells/progenitors with antitumor activity.
    • $2,270
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  • BRAF inhibitor
    T10599918505-61-0In house
    BRAF inhibitor is an inhibitor of B-Raf.
    • $39
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  • AD80
    T43011384071-99-1
    AD80, a multikinase inhibitor, inhibits RET, RAF, SRCand S6K, with greatly reduced mTOR activity.
    • $39
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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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  • Rineterkib
    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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  • 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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  • 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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  • 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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  • OSI-930
    T2624728033-96-3
    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 growth (angiogenesis) in tumors.
    • $47
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  • Kobe0065
    T1876436133-68-5
    Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; shows potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
    • $39
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  • Locostatin
    T8823133812-16-5
    Locostatin is a potent and cell permeable inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration.
    • $39
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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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  • RAF709
    T37111628838-42-5
    RAF709 is a novel Raf kinase inhibitor with IC50s of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
    • $34
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  • Pelitinib
    T2327257933-82-7
    Pelitinib (EKB-569) (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
    • $43
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  • SGX-523
    T22931022150-57-7
    SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
    • $44
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  • TAK-632
    T18861228591-30-7
    TAK-632 is a potent pan-Raf inhibitor.
    • $35
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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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  • Cyclorasin 9A5
    T826371782098-79-6
    Cyclorasin 9A5 is a cell-permeable, 11-residue cyclic peptide that orthosterically disrupts the Ras-Raf protein interaction, demonstrating an inhibition concentration (IC50) of 120 nM [1].
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  • Pseudoginsenoside Rh2
    TN21141370264-16-6
    Pseudoginsenoside Rh2 has cytotoxicity, it induces mitochondrial apoptosis in A549 cells and is responsible for excessive activation of the Ras/Raf/ERK/p53 pathway. (20Z) -Pseudoginsenoside Rh2 and (20E)-Pseudoginsenoside Rh2 have antioxidative activity.
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  • AZ304
    T5172942507-42-8
    AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits BRAF (WT), BRAF (V600E), and wild type CRAF (IC50s: 79/38/68 nM).
    • $42
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  • KG5
    T41003877874-85-6
    KG5 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
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  • K-Ras-IN-1
    T546984783-01-7
    K-Ras-IN-1 is a K-Ras inhibitor.
    • $45
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  • Raf inhibitor 2
    T4194220904-99-4
    Raf inhibitor 2 (CID 25014542) is novel inhibitor of Raf kinases.
    • $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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  • Vem-L-Cy5
    T78777
    Vem-L-Cy5 (compound 3), a Vemurafenib-based BRAF inhibitor conjugated with the near-infrared (NIR) fluorophore cyanine-5 (Cy5), selectively targets the BRAF V600E mutation and inhibits MEK phosphorylation. This compound demonstrates cell permeability and has been shown to inhibit the growth of various cancer cell types [1].
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  • Effusanin A
    TN392030220-43-0
    Effusanin A has antibacterial activity. It exhibits DNA-damaging activity in assay which employed DNA-repair deficient (RAD 52Y) and repair proficient (RAD +) yeast strains. Effusanin A shows inhibitory effects on DU145 cells with IC50 value of 3.16 micro
    • $179
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  • Griffipavixanthone
    TN4166219649-95-3
    Griffipavixanthone inhibits the growth of human Non-small-cell lung cancer H520 cells in dose- and time-dependent manners, it induces cell apoptosis through mitochondrial apoptotic pathway accompanying with ROS production. It can inhibit tumor metastasis
    • $2,569
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  • 6H05
    T19311469338-01-9
    6H05 (K-Ras inhibitor) is a selective, allosteric inhibitor of oncogenic mutant K-Ras(G12C).
    • $129
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  • PROTAC B-Raf degrader 1
    T125562364367-27-9
    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.
    • $431
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  • BI-882370
    TQ00481392429-79-6
    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-882370 also inhibits SRC family kinases.
    • $36
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  • Ro 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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  • Uplarafenib
    T633331425485-87-5
    Uplarafenib (B-Raf IN 10) is a potent BRAF inhibitor with an IC50 in the range of 50-100 nM.B-Raf IN 10 has antitumor activity that may affect cell proliferation and differentiation did not, and can be used to study solid tumors.
    • $87
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