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RAF Inhibitor

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187

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Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14660
    Dabrafenib
    75+ Cited Publications

    GSK2118436A; GSK2118436

    Raf Cancer
    Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively .
    Dabrafenib
  • HY-10331
    Regorafenib
    85+ Cited Publications

    BAY 73-4506

    VEGFR Autophagy PDGFR Raf RET c-Kit FGFR Tie Cancer
    Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity .
    Regorafenib
  • HY-12057
    Vemurafenib
    100+ Cited Publications

    PLX4032; RG7204; RO5185426

    Raf Autophagy Cancer
    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
    Vemurafenib
  • HY-15246
    Tovorafenib
    5+ Cited Publications

    TAK-580; MLN 2480; BIIB-024

    Raf Cancer
    Tovorafenib (TAK-580, MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase. Tovorafenib can be used for the study of glioma .
    Tovorafenib
  • HY-10966
    SB-590885
    5+ Cited Publications

    Raf Apoptosis Neurological Disease Metabolic Disease Cancer
    SB-590885 is a BRAF/c-Raf kinase inhibitor that selectively targets B-Raf, and it amplifies the ERK/MAPK signaling pathway in RAS-activated cells. SB-590885 effectively inhibits the malignant proliferation, transformation and tumorigenicity of oncogenic B-Raf cells; it also induces the proliferation of erythroid progenitor cells, delays their differentiation and promotes hemoglobin synthesis, thereby improving ineffective erythropoiesis and reducing apoptosis. SB-590885 exerts a synergistic effect with TGF-β inhibitors and glucocorticoids, significantly promoting the formation of erythroid colonies in cells from patients with Diamond-Blackfan anemia (DBA). SB-590885 is mainly used in relevant studies on DBA, cisplatin-induced myelosuppression-related anemia, and pan-cancers such as melanoma and colorectal cancer .
    SB-590885
  • HY-14660A
    Dabrafenib Mesylate
    75+ Cited Publications

    GSK2118436 Mesylate; GSK 2118436B

    Raf Cancer
    Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for Raf V600E and c-Raf, respectively.
    Dabrafenib Mesylate
  • HY-51424
    PLX-4720
    15+ Cited Publications

    Raf Cancer
    PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
    PLX-4720
  • HY-158115

    Molecular Glues Raf MEK Cancer
    NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors .
    NST-628
  • HY-132844

    HL-085

    MEK Cancer
    Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) .
    Tunlametinib
  • HY-109080
    Belvarafenib
    5 Publications Verification

    HM95573; GDC-5573; RG6185

    Raf Cancer
    Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAF v600E and C-RAF respectively .
    Belvarafenib
  • HY-147268

    RAF/KIN_2787

    Raf p38 MAPK Cancer
    Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity .
    Exarafenib
  • HY-50864
    GDC-0879
    4 Publications Verification

    Raf Cancer
    GDC-0879 is a potent and selective B-Raf inhibitor with an IC50 of 0.13 nM.
    GDC-0879
  • HY-10248
    RAF265
    5+ Cited Publications

    CHIR-265

    Raf VEGFR Autophagy Apoptosis Cancer
    RAF265 is a potent and orally active RAF/VEGFR2 inhibitor.
    RAF265
  • HY-101963

    Raf Src Ribosomal S6 Kinase (RSK) RET Cancer
    AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
    AD80
  • HY-N6670

    Antibiotic Raf ERK Ras MEK Bacterial Infection
    Cefotetan is a binding agent that targets human Raf1 kinase inhibitor protein (hRKIP). Cefotetan binds to hRKIP, reduces the binding space between hRKIP and Raf1 kinase, relieves hRKIP's inhibition of the Ras/Raf1/MEK/ERK signaling pathway, and enhances ERK phosphorylation. Cefotetan can be used to study diseases associated with dysregulated Ras/Raf1/MEK/ERK signaling pathways. Cefotetan is also a broad-spectrum antibacterial agent that disrupts cell wall synthesis by binding to bacterial penicillin-binding proteins (PBPs). It is used to study bacterial infections such as bone, skin, urinary tract, and lower respiratory tract .
    Cefotetan
  • HY-10331A
    Regorafenib monohydrate
    85+ Cited Publications

    BAY 73-4506 monohydrate

    VEGFR Autophagy PDGFR Raf RET FGFR c-Kit Tie Cancer
    Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity .
    Regorafenib monohydrate
  • HY-11004
    AZ 628
    10+ Cited Publications

    Raf Apoptosis Cancer
    AZ 628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
    AZ 628
  • HY-10201S
    Sorafenib-d3
    1 Publications Verification

    Donafenib; Bay 43-9006-d3

    Raf VEGFR FLT3 Ferroptosis Autophagy Apoptosis Cancer
    Sorafenib-d3 (Donafenib), a deuterated compound of Sorafenib, is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively .
    Sorafenib-d3
  • HY-14177
    Raf inhibitor 1
    3 Publications Verification

    Raf Cancer
    Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
    Raf inhibitor 1
  • HY-100510
    RAF709
    5+ Cited Publications

    Raf Cancer
    RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively . Antitumor efficacy .
    RAF709
  • HY-13308
    Regorafenib Hydrochloride
    85+ Cited Publications

    BAY 73-4506 hydrochloride

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively .
    Regorafenib Hydrochloride
  • HY-15716
    Kobe0065
    4 Publications Verification

    Ras Apoptosis Cancer
    Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
    Kobe0065
  • HY-12846

    Raf Cancer
    CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRaf V600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively.
    CCT196969
  • HY-123673
    MCP110
    2 Publications Verification

    Ras Raf Cancer
    MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 blocks the interaction of Ras with Raf. MCP110 disrupts this interaction might can be used for the research of human tumors .
    MCP110
  • HY-12787
    L-779450
    1 Publications Verification

    Raf Autophagy Cancer
    L-779450 is a potent and selective B-Raf kinase inhibitor with a Kd of 2.4 nM.
    L-779450
  • HY-10247
    BRAF inhibitor
    1 Publications Verification

    Raf Cancer
    BRAF inhibitor (Compound P-0850) is a B-Raf inhibitor with anti-tumor activity .
    BRAF inhibitor
  • HY-138294
    RAS/RAS-RAF-IN-1
    2 Publications Verification

    Ras Raf Cancer
    RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity .
    RAS/RAS-RAF-IN-1
  • HY-15717
    Kobe2602
    1 Publications Verification

    Ras Cancer
    Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki of 149 μM. Kobe2602 has antitumor activity .
    Kobe2602
  • HY-10201S2
    Sorafenib-13C,d3
    1 Publications Verification

    Bay 43-9006-13C,d3

    Raf VEGFR FLT3 Autophagy Apoptosis Ferroptosis Cancer
    Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator .
    Sorafenib-13C,d3
  • HY-10201R

    Bay 43-9006 (Standard)

    Reference Standards Raf VEGFR FLT3 Autophagy Apoptosis Ferroptosis Cancer
    Sorafenib (Standard) is the analytical standard of Sorafenib. This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator .
    Sorafenib (Standard)
  • HY-I0678

    Drug Metabolite PDGFR Cancer
    Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
    Regorafénib N-oxyde (M2)
  • HY-109574
    Raf inhibitor 2
    1 Publications Verification

    Raf Cancer
    Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research .
    Raf inhibitor 2
  • HY-P10438

    Raf Cancer
    TAT-Braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by TAT-Braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers .
    TAT-Braftide
  • HY-77113

    Raf Cancer
    B-Raf IN 11 is a B-Raf V600E mutant kinase inhibitor with an IC50 of 76 nM, and exhibits an IC50 of 238 nM against wild-type B-Raf kinase. B-Raf IN 11 inhibits the kinase activities of B-Raf V600E mutant and wild-type B-Raf kinase. B-Raf IN 11 is applicable to relevant research on colorectal cancer .
    B-Raf IN 11
  • HY-18227

    Raf Cancer
    B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM.
    B-Raf IN 1
  • HY-N13009

    Raf HIF/HIF Prolyl-Hydroxylase ERK MEK Reactive Oxygen Species (ROS) Apoptosis Caspase Cancer
    MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer .
    MO-2097
  • HY-W013411A
    Locostatin
    3 Publications Verification

    UIC-1005

    Raf G Protein-coupled Receptor Kinase (GRK) Cancer
    Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .
    Locostatin
  • HY-14947

    MKI 833

    MEK Cancer
    Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
    Balamapimod
  • HY-177511

    Ras p38 MAPK Raf MEK ERK Cancer
    KRAS G12D-IN-30 (Compound 4) is a KRAS inhibitor. KRAS G12D-IN-30 inhibits the activation of the downstream MAPK signaling cascade (Raf1-MEK-ERK) by blocking the activity of the KRAS G12 mutant. KRAS G12D-IN-30 can be used for the research of cancer .
    KRAS G12D-IN-30
  • HY-148059

    B-RAF IN 10

    Raf Cancer
    Uplarafenib (B-Raf IN 10) (Compound C09) is a BRAF inhibitor with an IC50 between 50 and 100 nM. Uplarafenib shows antitumor activity .
    Uplarafenib
  • HY-10201S1

    Bay 43-9006-d4

    Raf VEGFR FLT3 Ferroptosis Autophagy Apoptosis Cancer
    Sorafenib-d4 (Bay 43-9006-d4) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
    Sorafenib-d4
  • HY-159534

    FlezuRAFenib

    Raf Cancer
    Flezurafenibum (Flezurafenib) is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor, with antineoplastic effect .
    Flezurafenibum
  • HY-126298

    Raf Cancer
    RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAF V600E and B-RAF WT, respectively .
    RAF mutant-IN-1
  • HY-15198

    Raf PDGFR FLT3 c-Kit Cancer
    KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities .
    KG5
  • HY-159508

    Raf Cancer
    Brimarafenib is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor wtih antineoplastic effect .
    Brimarafenib
  • HY-14177A
    Raf inhibitor 1 dihydrochloride
    3 Publications Verification

    Raf Cancer
    B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
    Raf inhibitor 1 dihydrochloride
  • HY-W013411

    (E/Z)-UIC-1005

    Raf Cancer
    (E/Z)-Locostatin ((E/Z)-UIC-1005) is a racemic of Locostatin. Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .
    (E/Z)-Locostatin
  • HY-14660S

    GSK2118436A-d9; GSK2118436-d9

    Isotope-Labeled Compounds Raf Cancer
    Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively .
    Dabrafenib-d9
  • HY-164492

    Raf Cancer
    LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation .
    LSN3074753
  • HY-19343

    BMS-908662

    Raf Cancer
    XL-281 (BMS-908662) is an orally active inhibitor for RAF kinase, with IC50s of 2.6, 4.5 and 6 nM, for CRAF, B-RAF, and B-RAFV600E, respectively. XL-281 exhibits antitumor activity .
    XL-281

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