An inhibitor of XPO1/CRM1
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KPT-185

Item No. 26074

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2Z-propenoic acid, 1-methylethyl ester
CAS Number
1333151-73-7
Molecular Formula
C16H16F3N3O3
Formula Weight
355.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 15 mg/ml
λmax
233, 278 nm
SMILES
COC1=CC(C2=NN(/C=C\C(OC(C)C)=O)C=N2)=CC(C(F)(F)F)=C1
InChi Code
InChI=1S/C16H16F3N3O3/c1-10(2)25-14(23)4-5-22-9-20-15(21-22)11-6-12(16(17,18)19)8-13(7-11)24-3/h4-10H,1-3H3/b5-4-
InChi Key
NLNGWFLRRRYNIL-PLNGDYQASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $127

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    25 mg

    $297

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    Cayman Chemical
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    Product Description

    KPT-185 is an inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity.1,2 It reduces proliferation in a panel of patient-derived acute myeloid leukemia cells (IC50s = 100-500 nM).1 KPT-185 induces cell cycle arrest in the G1 phase and apoptosis in MOLT-4 T cell acute lymphoblastic leukemia cells and in a panel of six non-small cell lung cancer (NSCLC) cell lines in a time- and dose-dependent manner.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ranganathan, P., Yu, X., Na, C., et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood 120(9), 1765-1773 (2012).

    2. Etchin, J., Sanda, T., Mansour, M.R., et al. KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia. Br. J. Haematol. 161(1), 117-127 (2013).

    3. Wang, S., Han, X., Wang, J., et al. Antitumor effects of a novel chromosome region maintenance 1 (CRM1) inhibitor on non-small cell lung cancer cells in vitro and in mouse tumor xenografts. PLoS One 9(3), e89848 (2014).