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

KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity.

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KPT-251 Chemical Structure

KPT-251 Chemical Structure

CAS No. : 1388841-50-6

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Based on 1 publication(s) in Google Scholar

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Description

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].

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].

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

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.
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].

MedChemExpress (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.
Molecular Weight

375.23

Formula

C14H7F6N5O

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

FC(C1=CC(C(F)(F)F)=CC(C2=NN(/C=C\C3=NN=CO3)C=N2)=C1)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Purity & Documentation
References
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  • 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.

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Product Name:
KPT-251
Cat. No.:
HY-117996
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