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KPT-276

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InvivoChem Cat #: V1683

CAS #: 1421919-75-6Purity ≥98%

Description: This product has been discontinued. KPT-276 (KPT276; KPT 276) is a potent, orally bioavailable, and selective inhibitor of CRM1 (Chromosomal Maintenance 1, also known as Exportin 1 or XPO1). KPT-276 rreversibly binds to CRM1 and blocks CRM1-mediated nuclear export. In human multiple myeloma (MM) cell lines (HMCLs), KPT-276 irreversibly and specifically inhibited the nuclear export of XPO1, which encoded CRM1 and significantly reduced the viability of HMCLs. In bone marrow cells isolated from MM patients, KPT-276 induced apoptosis. Also, KPT-276 downregulated the expression of c-MYC, CDC25A and BRD4, which caused G1/S phase arrest.

References: Blood. 2012 Aug 30;120(9):1765-73; Exp Hematol. 2013 Jan;41(1):67-78.e4.

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Molecular Weight (MW)	426.26
Formula	C16H10F8N4O
CAS No.	1421919-75-6
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 20 mg/mL (46.9 mM)
	Water: <1 mg/mL
	Ethanol:<1 mg/mL
Solubility (In vivo)	30% PEG400+0.5% Tween80+5% Propylene glycol: 5 mg/mL
Synonyms	KPT-276; KPT 276; KPT276

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In Vitro	In vitro activity: 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. Cell Assay: KPT-276 is an orally bioavailable and selective CRM1 inhibitor that irreversibly binds to CRM1 and blocks CRM1-mediated nuclear export. In human multiple myeloma (MM) cell lines (HMCLs), KPT-276 irreversibly and specifically inhibited the nuclear export of XPO1, which encoded CRM1 and significantly reduced the viability of HMCLs. In bone marrow cells isolated from MM patients, KPT-276 induced apoptosis. Also, KPT-276 downregulated the expression of c-MYC, CDC25A and BRD4, which caused G1/S phase arrest.
In Vivo	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.
Animal model	Human leukemia (MV4-11) xenografts are established in mice.
Formulation & Dosage	Dissolved in DMSO; ~150 mg/kg; Oral administration
References	Blood. 2012 Aug 30;120(9):1765-73; Exp Hematol. 2013 Jan;41(1):67-78.e4.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Purity ≥98%
COA
MSDS

CRM1 inhibitor increases survival in a human leukemia xenograft model. Blood. 2012 Aug 30; 120(9): 1765–1773.

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