Name: TAK-632
Price: 220.00 USD

- Overview
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    Background
    
    TAK-632 is a selective inhibitor of BRAF, CRAF and BRAF-V600E kinase with IC50 value of 8.3 nM, 1.4 nM and 2.4 nM [1].RAF kinases are a family of three serine/threonine-specific protein kinases and play an important role in the RAS-RAF-MEK-ERK signal transduction cascade, as well as the mitogen-activated protein kinase (MAPK) cascade [2].TAK-632 is a potent pan-RAF kinase inhibitor and has a higher selectivity compared with the reported pan-RAF kinase inhibitor vemurafenib. When tested with SK-MEL-2 cells, TAK-632 showed induction on the BRAF-CRAF dimmers formation in a dose-dependent manner. In melanoma cell lines A375 and SK-MEL-2, TAK-632 exhibited significant antiproliferative effects with GI50 value of 6 nom/L and 11 nom/L, respectively [1].In mouse model with SK-MEL-2 subcutaneous xenograft, oral administration of TAK-632 caused significant reduction of phosphorylated ERK and tumor growth at the dose of 60 or 120 mg/kg/d once daily for 21 days without severe toxicity [1].It is also reported that TAK-632 is a potent inhibitor of pERK with IC50 value of 25 nM [1].
    
    [1]. Nakamura, A., et al., Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma. Cancer Res, 2013. 73(23): p. 7043-55.
    [2]. Korkut, A., et al., Perturbation biology nominates upstream-downstream drug combinations in RAF inhibitor resistant melanoma cells. Elife, 2015. 4.
- Properties
  - Alternative Name
    
    N-[7-cyano-6-[4-fluoro-3-[[2-[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide
    
    CAS Number
    
    1228591-30-7
    
    Molecular Formula
    
    C27H18F4N4O3S
    
    Molecular Weight
    
    554.52
    
    Appearance
    
    A solid
    
    Purity
    
    99.01%
    
    Solubility
    
    ≥27.75 mg/mL in DMSO; insoluble in H2O; ≥2.23 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758

TAK-632

TAK-632

Background

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