2. Membrane Transporter/Ion Channel Apoptosis
  3. CRM1 Apoptosis
  4. 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.

For research use only. We do not sell to patients.

KPT-251 Chemical Structure

KPT-251 Chemical Structure

CAS No. : 1388841-50-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 640 In-stock
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10 mM * 1 mL in DMSO USD 640 In-stock
Solid
1 mg USD 155 In-stock
5 mg USD 400 In-stock
10 mg USD 640 In-stock
25 mg USD 1280 In-stock
50 mg USD 2050 In-stock
100 mg USD 3280 In-stock
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Based on 1 publication(s) in Google Scholar

KPT-251 Related Antibodies

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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.

KPT-251 Related Antibodies

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

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)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (266.50 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6650 mL 13.3252 mL 26.6503 mL
5 mM 0.5330 mL 2.6650 mL 5.3301 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.92%

SDS (252 KB)

COA (253 KB) HNMR (141 KB) RP-HPLC (194 KB) LCMS (317 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6650 mL 13.3252 mL 26.6503 mL 66.6258 mL
5 mM 0.5330 mL 2.6650 mL 5.3301 mL 13.3252 mL
10 mM 0.2665 mL 1.3325 mL 2.6650 mL 6.6626 mL
15 mM 0.1777 mL 0.8883 mL 1.7767 mL 4.4417 mL
20 mM 0.1333 mL 0.6663 mL 1.3325 mL 3.3313 mL
25 mM 0.1066 mL 0.5330 mL 1.0660 mL 2.6650 mL
30 mM 0.0888 mL 0.4442 mL 0.8883 mL 2.2209 mL
40 mM 0.0666 mL 0.3331 mL 0.6663 mL 1.6656 mL
50 mM 0.0533 mL 0.2665 mL 0.5330 mL 1.3325 mL
60 mM 0.0444 mL 0.2221 mL 0.4442 mL 1.1104 mL
80 mM 0.0333 mL 0.1666 mL 0.3331 mL 0.8328 mL
100 mM 0.0267 mL 0.1333 mL 0.2665 mL 0.6663 mL
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KPT-251 Related Classifications

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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