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Raf

Items 1-50 of 135

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Product Name
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  1. A10001
    Sorafenib Tosylate (Nexavar)

    Raf inhibitor

    Sorafenib Tosylate (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.
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  2. A10002
    PLX-4720

    Raf inhibitor

    PLX-4720 is a potent and selective inhibitor of B-RafV600E 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-RafV600E than wild-type B-Raf.
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  3. A10250
    Regorafenib (BAY 73-4506)

    VEGFR inhibitor

    Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.
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  4. A10420
    GDC-0879

    B-Raf inhibitor

    GDC-0879 is a specific inhibitor of B-Raf kinase enzyme,targeting B-Raf (V600E) (IC50: 0.13 nM).
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  5. A10661
    NVP-BHG712

    EphB4 inhibitor

    NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.
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  6. A13226
    LGX 818 (Encorafenib)

    Selective B-RAF Inhibitor

    LGX818 is an orally available Raf kinase inhibitor with potential antineoplastic activity.
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  7. A11381
    Dabrafenib (GSK2118436A)

    Raf inhibitor

    Dabrafenib is a potent and selective inhibitor of B-RAF protein kinase carrying V600E mutation, currently in clinical trial.
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  8. A16079
    (E/Z)-Locostatin ((E/Z)-UIC-1005)

    RKIP/Raf1 inhibitor

    Locostatin is a cell permeable, potent inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration.
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  9. A10739
    PLX4032 (Vemurafenib)

    Raf inhibitor

    PLX4032 (Vemurafenib) also known as RG7204, Vemurafenib, R7204; RO5185426. PLX4032 is a B-raf inhibitor with an IC50 of 44 nM.
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  10. A13323
    TAK-632

    pan-RAF inhibitor

    TAK-632 is a potent pan-RAF inhibitor with favorable in vitro activity (BRAF(V600E) IC50, 2.4 nM; BRAF(wt), 8.3 nM; CRAF, 1.4 nM; pMEK (A375) IC50, 12 nM; pMEK (HMVII), 49 nM; V/B ratio.
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  11. A14019
    Avutometinib (RO5126766, CH5126766)

    Raf/MEK dual inhibitor

    Avutometinib (RO5126766, CH5126766), is a protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity.

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  12. A10773
    RAF265 (CHIR-265)

    RAF/VEGFR Inhibitor

    RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers.
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  13. A10774
    Raf265 derivative

    RAF/VEGFR Inhibitor

    Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM.
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  14. A10829
    SB590885

    B-Raf Inhibitor

    SB590885 is a selective small-molecule inhibitor of the B-Raf kinase and Ki app values are 0.16 and 1.72 nM for B-Raf and c-Raf respectively.
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  15. A11063
    AZ628

    Raf inhibitor

    AZ628 is a RAF inhibitor with IC50 values: ca 30 nM for BRAF V600E and wild-type CRAF and 100 nM for wild-type BRAF.
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  16. A11077
    ZM 336372

    C-Raf inhibitor

    ZM 336372 is a potent ATP-competitive inhibitor of Raf-1 in vitro (IC50 = 70 nM) with the paradoxical effect of inducing >100-fold activation of Raf-1 in whole cells.
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  17. A22641
    Raf inhibitor 2

    raf kinase inhibitor

    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.
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  18. A24661
    PROTAC B-Raf degrader 1

    PROTAC B-Raf Degrader

    PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) that facilitates the degradation of B-Raf through a Cereblon ligand. This compound demonstrates significant anti-cancer activity, making it a valuable tool for cancer research. It is particularly useful in studies investigating B-Raf-mediated signaling pathways and therapeutic strategies targeting oncogenic mutations in B-Raf.
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  19. A24696
    Tagarafdeg

    BRAFV600E Degrader

    Tagarafdeg is a CRBN-based bifunctional degradation activating compound (BiDAC) selectively targeting BRAFV600E mutations. Demonstrating potent activity with a DC50 of 14 nM in A375 cells, it effectively degrades various BRAF mutations, including G469A and G466V, as well as the p61-BRAFV600E splice variant. This reagent is suitable for applications in tumor research, contributing to the understanding of BRAF-mediated oncogenic processes.
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  20. A24708
    PROTAC BRAF-V600E degrader-1

    BRAF-V600E Degrader

    PROTAC BRAF-V600E degrader-1 is an effective degrader of the BRAF-V600E mutant, selectively targeting this oncogenic variant while sparing wild-type BRAF. With Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively, this compound facilitates degradation of BRAF-V600E through the ubiquitin-proteasome system (UPS). Its potent activity against melanoma cells makes it a valuable tool for research into targeted cancer therapies and mechanisms of drug resistance in BRAF-mutant tumors.
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  21. A24727
    SJF-0628

    RAF PROTAC Degrader

    SJF-0628 is a RAF PROTAC degrader that facilitates the targeted degradation of BRAF protein in cancer cell lines, specifically in colorectal cancer models (Colo-205, LS-411N, HT-29, RKO) and the triple-negative breast cancer line DU-4475. This compound significantly reduces levels of phosphorylated MEK and ERK in DU-4475 cells, demonstrating notable anti-tumor activity. SJF-0628 is valuable for research studies focused on the mechanisms of colorectal cancer and triple-negative breast cancer.
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  22. A24810
    Norartocarpetin

    Tyrosinase Inhibitor

    Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells.
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  23. A25316
    MO-2097

    RAF-1/HIF-1α Inhibitor

    MO-2097 is a selective RAF-1 and HIF-1α inhibitor that induces the destabilization of RAF-1, resulting in decreased levels of epithelial-mesenchymal transition (EMT) transcription factors and mesenchymal markers. Additionally, MO-2097 effectively inhibits HIF-1α protein expression mediated by hnRNPA2B1 in hypoxic conditions. This compound promotes the generation of mitochondrial reactive oxygen species (ROS), contributing to apoptosis in malignant cells. MO-2097 demonstrates significant potential in suppressing colorectal cancer metastasis by targeting the RAF/MEK/ERK signaling pathway and has shown efficacy in reducing tumor growth in HCT116 cell xenograft mouse models, thus serving as a valuable tool for colorectal cancer research.
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  24. A31172
    CCT241161

    RAF Inhibitor

    CCT241161 is a potent pan-RAF inhibitor that effectively targets multiple RAF family members with IC50 values of 3 nM for LCK, 6 nM for CRAF, 10 nM for SRC, 15 nM for V600E-BRAF, and 30 nM for BRAF. This compound demonstrates significant antiproliferative activity in BRAF and NRAS mutant melanoma cell lines, making it a valuable tool for cancer research. CCT241161 is relevant for studies focused on targeted therapies in oncogenic signaling pathways.
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  25. A25635
    Erufosine

    PI3K/Akt/Ras/Raf/MAPK Inhibitor

    Erufosine is a potent inhibitor of the PI3K/Akt and Ras/Raf/MAPK signaling pathways. It demonstrates significant cytotoxic activity against breast cancer cell lines, specifically MCF-7 and MDA-MB-231, with IC50 values of 40.95 μM and 40.8 μM, respectively. By reducing the phosphorylation levels of PI3K (p85), Akt (PKB), and cRaf, Erufosine serves as a valuable tool in the research of breast cancer and myeloid leukemia.
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  26. A26067
    PHI-501

    RAF/DDR Inhibitor

    PHI-501 is a dual inhibitor targeting RAF and DDR pathways. It demonstrates potent anti-proliferative effects in melanoma cell lines, effectively inhibiting colony formation in drug-resistant cells. PHI-501 disrupts ERK and AKT phosphorylation and downregulates key gene sets associated with TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways, as well as pathways involved in epithelial-mesenchymal transition. In vivo studies show significant anti-tumor efficacy in the SK-MEL3DR xenograft model, making PHI-501 valuable for research on drug resistance in melanoma.
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  27. A28558
    Lifirafenib maleate

    Raf/EGFR Inhibitor

    Lifirafenib maleate is a potent inhibitor of Raf kinase and EGFR, exhibiting IC50 values of 23 nM and 29 nM for recombinant BRafV600E and EGFR, respectively. This compound effectively disrupts critical signaling pathways involved in cancer cell proliferation and survival. Lifirafenib maleate is relevant for research applications in cancer biology, particularly in studies focusing on targeted therapies for tumors with BRAF mutations or EGFR dysregulation.
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  28. A28755
    EGFR/BRAF-IN-1

    EGFR/BRAF Inhibitor

    EGFR/BRAF-IN-1 is a selective inhibitor targeting both EGFR and BRAFV600E with an IC50 of 45 nM. This compound, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, effectively inhibits cancer cell proliferation with a GI50 of 35 nM. Additionally, EGFR/BRAF-IN-1 exhibits notable antioxidant properties, making it a valuable reagent for research in cancer biology and therapeutic development.
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  29. A40682
    NST-628

    RAF Molecular Glue

    NST-628 is a molecular glue targeting RAF within the MAPK signaling pathway. It disrupts RAF phosphorylation and MEK activation by preventing the formation of BRAF-CRAF and BRAF-ARAF heterodimers. NST-628 exhibits significant biological activity in inhibiting RAS- and RAF-driven cancers, particularly in tumors with mutant KRAS, NRAS, BRAF class II/III, and NF1 mutations. This compound is a valuable tool for research into targeted cancer therapies and understanding the RAS-MAPK pathway's role in oncogenesis.
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  30. A40683
    Exarafenib

    pan-RAF Inhibitor

    Exarafenib is a selective pan-RAF inhibitor that is available for oral administration. It is effective in targeting RAF-dependent cancers, specifically those with various BRAF alterations, by suppressing MAPK signaling pathways. Exarafenib has demonstrated significant anticancer activity in preclinical studies, making it a valuable tool for research in oncology and potential therapeutic applications in melanoma and other RAF-driven malignancies.
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  31. A40685
    Claturafenib

    BRAF Inhibitor

    Claturafenib is a potent, orally active pan-mutant BRAF inhibitor. It effectively inhibits phosphorylated ERK (pERK) in cells, demonstrating an IC50 value of 1.6 nM in HT29 cell lines. Claturafenib exhibits significant antitumor activity against non-small cell lung cancer (NSCLC) harboring the BRAFG469A mutation and melanoma with the BRAFK601E mutation, making it a valuable tool for cancer research focused on BRAF mutant pathways.
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  32. A40686
    Mosperafenib

    BRAF Inhibitor

    Mosperafenib is a selective BRAF inhibitor designed to target BRAF V600 mutations. It exhibits significant biological activity against BRAF-mutant solid tumors, including colorectal cancer (CRC). This reagent is used in various research applications, particularly in the study of malignancies driven by BRAF mutations, enabling investigations into disease mechanisms and therapeutic strategies.
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  33. A40687
    TBAP-001

    RAF Inhibitor

    TBAP-001 is a pan-RAF kinase inhibitor that targets the RAF signaling pathway. It exhibits potent inhibitory activity with an IC50 of 62 nM in the BRAF V600E kinase assay. This compound is utilized in research applications aimed at understanding the role of RAF kinases in cancer progression and therapeutic resistance, making it valuable for studies focused on targeted cancer therapies.
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  34. A40688
    B-Raf IN 11

    B-Raf Inhibitor

    B-Raf IN 11 is a selective inhibitor of the B-RafV600E mutant kinase, demonstrating an IC50 of 76 nM, and exhibits an IC50 of 238 nM against wild-type B-Raf kinase. This compound effectively inhibits the kinase activities of both B-RafV600E mutant and wild-type B-Raf, making it a valuable tool for investigating pathways related to colorectal cancer. Its application in research provides insight into therapeutic strategies targeting B-Raf mutations in cancer treatment.
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  35. A40689
    Flezurafenibum

    Raf Inhibitor

    Flezurafenibum is a Raf kinase inhibitor that demonstrates significant antineoplastic activity. By selectively targeting the Raf pathway, it interferes with tumor growth and proliferation. This compound is of particular interest in cancer research, especially for studies involving Raf-mediated signaling pathways and potential therapeutic applications in various malignancies.
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  36. A40690
    Uplarafenib

    BRAF Inhibitor

    Uplarafenib is a selective BRAF inhibitor with an IC50 ranging from 50 to 100 nM. This compound displays significant antitumor activity, making it a valuable tool in cancer research. Uplarafenib is primarily utilized in studies investigating BRAF mutations and their role in tumorigenesis.
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  37. A40691
    Braftide

    BRAF Inhibitor

    Braftide is an allosteric inhibitor of BRAF kinase that targets the dimer interface, effectively preventing the formation of BRAF dimers. It exhibits inhibitory activity against both wild-type BRAF and the oncogenic variant BRAFG469A, with IC50 values of 364 nM and 172 nM, respectively. By inhibiting the MAPK signaling pathway, Braftide demonstrates the ability to suppress the proliferation of KRAS mutant tumor cells, with EC50 values of 7.1 µM and 6.6 µM for HCT116 and HCT-15 cell lines, respectively. This compound is applicable in various cancer research studies.
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  38. A40692
    B-Raf IN 15

    BRAF Inhibitor

    B-Raf IN 15 is a potent BRAF inhibitor that selectively targets both BRAF wild-type and BRAF V600E variants, exhibiting IC50 values of 2.0 μM and 0.8 μM, respectively. This compound is particularly valuable in cancer research, facilitating studies on the pathways involved in tumor growth and progression. B-Raf IN 15 serves as an effective tool for evaluating therapeutic strategies and understanding the mechanisms of BRAF-related malignancies.
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  39. A40693
    PLX7922

    RAF Inhibitor

    PLX7922 is a selective RAF inhibitor that targets BRAFV600E mutations. It effectively inhibits phosphorylated ERK (pERK) in BRAFV600E cell lines, while paradoxically activating pERK in NRAS mutant cell lines. This compound is valuable for studying the signaling pathways involved in cancer, particularly in the context of RAS/RAF/MEK/ERK pathway alterations.
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  40. A40694
    RAS/RAS-RAF-IN-1

    RAS/RAS-RAF Inhibitor

    RAS/RAS-RAF-IN-1 is a potent inhibitor targeting the RAS and RAS-RAF signaling pathways. With a dissociation constant (KD) in the range of 5.0 μM to 15 μM for cyclophilin A (CYPA), this compound demonstrates significant binding affinity. RAS/RAS-RAF-IN-1 exhibits notable antitumor activity, making it a valuable tool for cancer research and therapeutic development.
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  41. A40695
    GNE-9815

    RAF Inhibitor

    GNE-9815 is a highly selective pan-RAF inhibitor that targets both CRAF and BRAF with Ki values of 0.062 nM and 0.19 nM, respectively. It demonstrates good oral bioavailability and, when used in conjunction with MEK inhibitors such as Cobimetinib, leads to synergistic modulation of the MAPK pathway. GNE-9815 is particularly useful in research focused on KRAS mutant cancers, facilitating the exploration of therapeutic strategies in this context.
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  42. A40696
    Vem-L-Cy5

    BRAF Inhibitor

    Vem-L-Cy5 is a BRAF inhibitor that incorporates the near-infrared fluorophore cyanine-5 (Cy5). This compound specifically targets the BRAFV600E mutation and effectively inhibits MEK phosphorylation. Vem-L-Cy5 demonstrates cell permeability and has been shown to inhibit the growth of various cancer cell types, making it a valuable tool for cancer research and therapeutic development.
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  43. A40697
    SHR902275

    b/cRAF Inhibitor

    SHR902275 is a selective and potent b/cRAF inhibitor, specifically designed to target RAS mutant cancers. It demonstrates impressive inhibitory activity with IC50 values of 1.6 nM for cRAF, 10 nM for bRAFwt, and 5.7 nM for the bRAFV600E mutation. In cellular assays, SHR902275 effectively inhibits growth with GI50 values of 1.5 nM and 0.17 nM for H358, as well as 0.4 nM and 0.32 nM for A375 and Calu6, and SK-MEL2 cells, respectively. This compound holds potential for research applications focused on targeted cancer therapies and understanding RAF signaling pathways.
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  44. A40699
    Belvarafenib TFA

    Raf Inhibitor

    Belvarafenib TFA is a potent pan-RAF inhibitor that targets the rapidly accelerated fibrosarcoma (RAF) family of kinases. It demonstrates impressive inhibitory activity, with IC50 values of 56 nM for B-RAF, 7 nM for B-RAFV600E, and 5 nM for C-RAF. This compound is valuable for research focusing on cancer therapeutics, particularly for the treatment of tumors driven by aberrant RAF signaling pathways.
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  45. A40700
    Brimarafenib

    Raf Inhibitor

    Brimarafenib is a selective inhibitor of Raf kinase, primarily targeting the MAPK/ERK signaling pathway. It exhibits significant antineoplastic activity, making it valuable for cancer research, specifically in the study of tumors driven by aberrant Raf signaling. Brimarafenib is utilized in preclinical models to investigate its therapeutic potential and mechanisms of action in various malignancies.
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  46. A40701
    Cyclorasin 9A5

    Ras-Raf Inhibitor

    Cyclorasin 9A5 is an 11-residue cyclic peptide that acts as an orthosteric inhibitor of the Ras-Raf protein interaction, exhibiting an IC50 of 120 nM. This compound is valuable for studying the Ras signaling pathway's involvement in various cancers and cellular processes. Its cell-permeable nature allows for effective in vitro and in vivo applications in cancer research and drug development targeting Ras-dependent pathways.
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  47. A40702
    (Z)-GW 5074

    c-Raf Inhibitor

    (Z)-GW 5074 is a selective c-Raf inhibitor that demonstrates unique interactions with mutant huntingtin protein (mHTT) and LC3, without affecting wild-type huntingtin protein. This compound effectively inhibits c-Raf signaling, playing a crucial role in cellular responses associated with neurodegenerative disorders. (Z)-GW 5074 is primarily utilized in research focused on neurodegeneration and related biochemical pathways, providing valuable insights into therapeutic strategies targeting these diseases.
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  48. A40703
    Pan-RAF kinase inhibitor 1

    Pan-RAF Kinase Inhibitor

    Pan-RAF kinase inhibitor 1 is a selective inhibitor targeting the Pan-RAF kinase family, modulating the MAPK signaling pathway. This compound effectively suppresses the proliferation of RAS-mutant tumor cells, making it a valuable tool for investigating cancer biology. Its applications include research focused on therapeutic strategies for cancer treatment, particularly in the context of RAS mutations.
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  49. A40705
    Anticancer agent 124

    RAF Inhibitor

    Anticancer Agent 124 is a potent and selective pan RAF inhibitor that acts primarily on the RAF family of kinases. It effectively suppresses MAPK signaling in tumor cells harboring BRAF V600E, NRAS, and KRAS mutations. This compound is suitable for research applications aimed at understanding the role of RAF-mediated pathways in cancer progression and therapeutic resistance.
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  50. A40706
    C-RAF kinase-IN-1

    C-RAF Kinase Inhibitor

    C-RAF kinase-IN-1 is a selective inhibitor of C-RAF kinase, demonstrating an IC50 value of 0.193 μM. As a quinoline derivative, it plays a significant role in inhibiting C-RAF-mediated signaling pathways. This compound is primarily utilized in cancer research, providing insights into therapeutic targeting and the underlying mechanisms of cancer progression.
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