A selective pan-Raf inhibitor
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TAK-632

Item No. 16285

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-[[7-cyano-2-[(cyclopropylcarbonyl)amino]-6-benzothiazolyl]oxy]-2-fluorophenyl]-3-(trifluoromethyl)-benzeneacetamide
CAS Number
1228591-30-7
Molecular Formula
C27H18F4N4O3S
Formula Weight
554.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mlEthanol: 0.5 mg/ml
λmax
238, 260, 282, 326 nm
SMILES
O=C(NC1=C(F)C=CC(OC2=CC=C(N=C(NC(C3CC3)=O)S4)C4=C2C#N)=C1)CC5=CC(C(F)(F)F)=CC=C5
InChi Code
InChI=1S/C27H18F4N4O3S/c28-19-7-6-17(12-21(19)33-23(36)11-14-2-1-3-16(10-14)27(29,30)31)38-22-9-8-20-24(18(22)13-32)39-26(34-20)35-25(37)15-4-5-15/h1-3,6-10,12,15H,4-5,11H2,(H,33,36)(H,34,35,37)
InChi Key
OJFKUJDRGJSAQB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $186

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    50 mg

    $835

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    Product Description

    TAK-632 is a slow off-rate inhibitor of Raf kinases (IC50s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively).1 It demonstrates 14-1,200-fold selectivity for Raf over a panel of 26 different kinases.1 TAK-632 shows significant antiproliferative activity against mutated B-Raf or mutated N-Ras cancer cell lines and xenograft models, inhibiting MEK phosphorylation with an IC50 value of 12 nM and downstream ERK phosphorylation with an IC50 value of 16 nM.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Okaniwa, M., Hirose, M., Arita, T., et al. Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: Design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. J. Med. Chem. 56(16), 6478-6494 (2013).

    2. Nakamura, A., Arita, T., Tsuchiya, S., et al. Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma. Cancer Res. 73(23), 7043-7055 (2013).