An inhibitor of XPO1/CRM1
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KPT-276

Item No. 29158

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-1-(3,3-difluoro-1-azetidinyl)-2-propen-1-one
CAS Number
1421919-75-6
Molecular Formula
C16H10F8N4O
Formula Weight
426.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMF:PBS (pH 7.2) (1:2): 0.3mg/mLDMSO: 2mg/mLEthanol: 1mg/mL
λmax
268 nm
SMILES
O=C(N1CC(F)(F)C1)/C=C\N2C=NC(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=N2
InChi Code
InChI=1S/C16H10F8N4O/c17-14(18)6-27(7-14)12(29)1-2-28-8-25-13(26-28)9-3-10(15(19,20)21)5-11(4-9)16(22,23)24/h1-5,8H,6-7H2/b2-1-
InChi Key
JCHAWRDHMUSLMM-UPHRSURJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $75

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    10 mg

    $120

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    25 mg

    $222

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    50 mg

    $295

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    Cayman Chemical
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    Product Description

    KPT-276 is an orally bioavailable inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity.1 In vivo, KPT-276 (150 mg/kg) increases survival and reduces spleen weight and white blood cell count in an MV4-11 acute myeloid leukemia (AML) mouse xenograft model. It also reduces tumor volume and increases survival in a BT 145 glioblastoma mouse xenograft model when administered at a dose of 75 mg/kg.2

    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. Green, A.L., Ramkissoon, S.H., McCauley, D., et al. Preclinical antitumor efficacy of selective exportin 1 inhibitors in glioblastoma. Neuro. Oncol. 17(5), 697-707 (2015).