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KPT-251
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-251图片
CAS NO:1388841-50-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 inducescancercellapoptosisand shows antileukemic activity[1][2].

体外研究
(In Vitro)

KPT-251 binds in the NES-binding groove, which is located on the central, convex side of the CRM1 ring[1].
KPT-251 (72 h) suppresses melanoma cell proliferation[2].
KPT-251 (1 μM; 0-48 h) modulates levels of p53, pRb, survivin, and ERK phosphorylation[2].
KPT-251 (0.1 and 1 μM; 0-72 h) induces cell-cycle arrest and apoptosis[2].

Western Blot Analysis[2]

Cell Line:Melanoma BRAF WT (Mewo) and mutant cells (A375)
Concentration:1 μM
Incubation Time:4, 8, 24 and 48 h
Result:Prevented cytoplasmic p53 degradation, decreased survivin levels, increased ERK phosphorylation in both BRAF WT and mutant and reduced pRb and p-pRb levels.

Cell Cycle Analysis[2]

Cell Line:Mewo and A375 cells
Concentration:1 μM
Incubation Time:24, 48 and 72 h
Result:Reduced S-phase, both G1 and/or G2 cell-cycle arrest can be observed.

Apoptosis Analysis[2]

Cell Line:Mel-Juso, SK-MEL-28, SK-MEL-5 and A375 cells
Concentration:0.1 and 1 μM
Incubation Time:24, 48 and 72 h
Result:Increased caspase-3 and -7 activity in the tested melanoma cell lines in a dose- and time-related manner.
体内研究
(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[1].
KPT-251 (50 mg/kg; p.o.; every other day for 21 days) suppresses tumor growth in mice melanoma xenograft models[2].

Animal Model:7-weekold female NOD-SCID-IL2Rcγnull(NSG) mice, introduced 2 × 106luciferase-expressing MV4-11 cells via tail-vein injections[1]
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[2]
Dosage:50 mg/kg
Administration:Oral, every other day for 21 days
Result:Suppressed tumor growth, increased cleaved caspase-3 and decreased Ki67.
分子量

375.23

Formula

C14H7F6N5O

CAS 号

1388841-50-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.