产品
编 号：F146975
分子式：C14H7F6N5O
分子量：375.23
分子式：C14H7F6N5O
分子量：375.23
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 1388841-50-6
产品详情
生物活性：
KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity.
体内研究：
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.Animal Model:7-weekold female NOD-SCID-IL2Rcγnull (NSG) mice, introduced 2 × 106 luciferase-expressing MV4-11 cells via tail-vein injections
Dosage:75 mg/kg/day
Administration:Gavage, three times per week for 5 weeks
Result:Exhibited significantly increased survival with leukemia progression occurring only after cessation of treatment, prevented infiltration of leukemia cells into mouse bone marrow and spleen, and spared normal hematopoietic cells.
Animal Model:Athymic nude mice Nu/Nu, melanoma xenograft models
Dosage:50 mg/kg
Administration:Oral, every other day for 21 days
Result:Suppressed tumor growth, increased cleaved caspase-3 and decreased Ki67.
体外研究：
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.
KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity.
体内研究：
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.Animal Model:7-weekold female NOD-SCID-IL2Rcγnull (NSG) mice, introduced 2 × 106 luciferase-expressing MV4-11 cells via tail-vein injections
Dosage:75 mg/kg/day
Administration:Gavage, three times per week for 5 weeks
Result:Exhibited significantly increased survival with leukemia progression occurring only after cessation of treatment, prevented infiltration of leukemia cells into mouse bone marrow and spleen, and spared normal hematopoietic cells.
Animal Model:Athymic nude mice Nu/Nu, melanoma xenograft models
Dosage:50 mg/kg
Administration:Oral, every other day for 21 days
Result:Suppressed tumor growth, increased cleaved caspase-3 and decreased Ki67.
体外研究：
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.
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