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KPT-276
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KPT-276图片
CAS NO:1421919-75-6
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)426.26
FormulaC16H10F8N4O
CAS No.1421919-75-6
Storage-20℃ for 3 years in powder form
-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
SynonymsKPT-276; KPT 276; KPT276
实验参考方法
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 modelHuman leukemia (MV4-11) xenografts are established in mice.
Formulation & DosageDissolved 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.