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KPT-276 1421919-75-6

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Synonyms
Appearance
Chemical Formula
C16H10F8N4O
Solubility
Molecular Weight
426.26
Storage and Stability
in stock
CAS No.
1421919-75-6
Purity
98%+
Introduction
KPT-276 is an orally bioavailable selective CRM1 inhibitor.

Superior oral bioavailability and PK profile relative to KPT-185 in vivo. Potential for use in hematological malignancies such as AML and multiple myeloma.

KPT-276 results in significant growth inhibition and apoptosis induction in MCL cells. KPT-276 specifically and irreversibly inhibits the nuclear export function of XPO1, and reduces the viability of 12 HMCLs. KPT-276 also actively induces apoptosis in primary MM patient samples. 

KPT-276 significantly prolongs survival of leukemic mice and reduces leukemic burden in a xenograft AML mouse model. KPT-276 significantly suppresses tumor growth in an MCL-bearing severe combined immunodeficient mouse model without severe toxicity.  KPT-276 reduces monoclonal spikes in the Vk*MYC transgenic MM mouse model, and inhibits tumor growth in a xenograft MM mouse model. 

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