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KPT-251

CAS No. : 1388841-50-6

MCE 国际站：KPT-251

产品活性：KPT-251 是一种具有口服活性的染色体区域维持1蛋白 (CRM1) 抑制剂。 KPT-251 诱导癌细胞凋亡 (apoptosis)，具有抗白血病活性。

研究领域：Membrane Transporter/Ion Channel  |  Apoptosis

作用靶点：CRM1  |  Apoptosis

In Vitro: KPT-251 binds in the NES-binding groove, which is located on the central, convex side of the CRM1 ring.
KPT-251 (72 h) suppresses melanoma cell proliferation.
KPT-251 (1 μM; 0-48 h) modulates levels of p53, pRb, survivin, and ERK phosphorylation.
KPT-251 (0.1 and 1 μM; 0-72 h) induces cell-cycle arrest and apoptosis.

In Vivo: KPT-251 (75 mg/kg/day; i.g.; three times per week for 5 weeks) effectively suppresses the growth of MV4-11 cells engrafted into NSG mice and provides a significant survival benefit.
KPT-251 (50 mg/kg; p.o.; every other day for 21 days) suppresses tumor growth in mice melanoma xenograft models.

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