An Hsp90 inhibitor
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TAS 116

Item No. 33779

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-ethyl-4-[3-(1-methylethyl)-4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-1H-pyrazolo[3,4-b]pyridin-1-yl]-benzamide
CAS Number
1260533-36-5
Molecular Formula
C25H26N8O
Formula Weight
454.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
SMILES
O=C(C1=CC=C(N2N=C(C(C)C)C3=C(N4C=NC(C5=CN(C)N=C5)=C4)C=CN=C32)C(CC)=C1)N
InChi Code
InChI=1S/C25H26N8O/c1-5-16-10-17(24(26)34)6-7-20(16)33-25-22(23(30-33)15(2)3)21(8-9-27-25)32-13-19(28-14-32)18-11-29-31(4)12-18/h6-15H,5H2,1-4H3,(H2,26,34)
InChi Key
NVVPMZUGELHVMH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    10 mg

    $183

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    25 mg

    $303

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    Cayman Chemical
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    Product Description

    TAS 116 is a heat shock protein 90 (Hsp90) inhibitor.1 It selectively binds to Hsp90α and Hsp90β (Kis = 34.7 and 21.3 nM, respectively) over glucose-regulated protein 94 (GRP94) and TGF-β receptor-associated protein 1 (TRAP1; Kis = 50,000 nM for both). TAS 116 (3.6, 7.1, and 14 mg/kg) reduces intratumoral protein levels of HER2, HER3, and Akt, as well as reduces tumor growth in a HER2-expressing NCI N87 gastric cancer mouse xenograft model and does not induce photoreceptor injury in rats when administered at a dose of 12 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ohkubo, S., Kodama, Y., Muraoka, H., et al. TAS-116, a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models. Mol. Cancer Ther. 14(1), 14-22 (2015).