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KPT-276

Chemical Structure : KPT-276

CAS No.: 1421919-75-6

KPT-276 (KPT276)

Catalog No.: PC-49222Not For Human Use, Lab Use Only.

KPT-276 (KPT276) is an orally bioavailable selective inhibitor of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of this protein, shows antileukemic activity in vitro and in vivo in acute myeloid leukemia (AML).

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Biological Activity

KPT-276 (KPT276) is an orally bioavailable selective inhibitor of nuclear export (SINE) that irreversibly bind to CRM1 and block the function of this protein, shows antileukemic activity in vitro and in vivo in acute myeloid leukemia (AML).
KPT-276 inhibits a panel of AML cell lines proliferation (MV4-11, Kasumi-1, OCI/AML3, MOLM-13, KG1a, and THP-1) with IC50 of 100-500 nM.
KPT-276 decreases CRM1 protein level and accumulates CRM1 cargo proteins in the nucleus.
KPT-276 induces differentiation of AML cell lines.
KPT-276 (150 mg/kg) increases survival in a human leukemia xenograft model.

Physicochemical Properties

M.Wt 426.270
Formula C16H10F8N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

1. Ranganathan P, et al. Blood. 2012 Aug 30;120(9):1765-73.

2. Zhang K, et al. Exp Hematol. 2013 Jan;41(1):67-78.e4.

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