2. Membrane Transporter/Ion Channel Apoptosis
  3. CRM1 Apoptosis
  4. KPT-251

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。

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KPT-251 Chemical Structure

KPT-251 Chemical Structure

CAS No. : 1388841-50-6

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1 mg ￥2210
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KPT-251 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

KPT-251 相关抗体:

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 7-weekold female NOD-SCID-IL2Rcγnull (NSG) mice, introduced 2 × 106 luciferase-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
性状

固体

颜色

Off-white to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

纯度 & 产品资料
参考文献

KPT-251 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KPT-2511388841-50-6KPT251KPT 251CRM1ApoptosisChromosomal Maintenance 1Exportin 1XPO1myeloid leukemiaantileukemic activitymelanomaA375Inhibitorinhibitorinhibit

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