CAS NO: | 1421919-75-6 |
规格: | ≥98% |
包装 | 价格(元) |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 426.26 |
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Formula | C16H10F8N4O |
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 |
Synonyms | KPT-276; KPT 276; KPT276 |
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. |
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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. |