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

Eltanexor  (Synonyms: KPT-8602)

Cat. No.: HY-100423 Purity: 99.84%
COA Handling Instructions

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Eltanexor (KPT-8602) is a second-generation, highly specific and orally active exportin-1 (XPO1) inhibitor with potent anti-leukemic activity. Eltanexor (KPT-8602) inhibits XPO1-dependent nuclear export (EC50=60.9 nM) by directly targeting XPO1. Eltanexor (KPT-8602) induces Caspase-dependent apoptosis in a panel of leukemic cell lines.

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

Eltanexor Chemical Structure

Eltanexor Chemical Structure

CAS No. : 1642300-52-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 271 In-stock
Solution
10 mM * 1 mL in DMSO USD 271 In-stock
Solid
1 mg USD 75 In-stock
5 mg USD 288 In-stock
10 mg USD 340 In-stock
50 mg USD 800 In-stock
100 mg USD 1160 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Eltanexor:

Eltanexor Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Eltanexor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Eltanexor (KPT-8602) is a second-generation, highly specific and orally active exportin-1 (XPO1) inhibitor with potent anti-leukemic activity. Eltanexor (KPT-8602) inhibits XPO1-dependent nuclear export (EC50=60.9 nM) by directly targeting XPO1. Eltanexor (KPT-8602) induces Caspase-dependent apoptosis in a panel of leukemic cell lines[1].

IC50 & Target

XPO1[1]
In Vitro

KPT-8602 (2-6 nM; 72 hours) reduces cell viability in leukemia cell lines with EC50s ranging from 25 to 145 nM[1].
KPT-8602 (1 nM; 16 hours) induces apoptosis in leukemia cell lines[1].

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

Eltanexor Related Antibodies

Cell Viability Assay[1]

Cell Line: T-ALL cells (Jurkat, MOLT-4, ALL-SIL, DND41, and HPB-ALL), B-ALL cells (BV173, EHEB, and REH), AML cells (MV4-11, MOLM13, K-562, and HL-60)
Concentration: 2, 4, 6 nM
Incubation Time: 72 hours
Result: Cell viability was reduced with EC50 values ranging from 25 to 145 nM.

Western Blot Analysis[1]

Cell Line: T-ALL, B-ALL, AML cells
Concentration: 1 μM
Incubation Time: 16 hours
Result: Appearance of cleaved caspase-3 substrate PARP as early as 6 hours.
In Vivo

KPT-8602 (15 mg/kg; oral gavage; daily for 12 days) shows potent anti-lymphoblastic leukemia activity[1].

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

Animal Model: Female BALB/c mice (model with the JAK3 (M511I) mutation)[1]
Dosage: 15 mg/kg
Administration: Oral gavage; daily for 12 days
Result: Showed a marked reduction in total white blood cell (WBC) counts after 2 days of treatment compared to placebo-treated animals and the WBC counts continued to drop until they reached normal levels (<10,000 cells/μL) by day 12.
Clinical Trial
Molecular Weight

428.29

Formula

C17H10F6N6O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC(F)(F)C1=CC(C(F)(F)F)=CC(C2=NN(/C=C(C3=CN=CN=C3)/C(N)=O)C=N2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (233.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3349 mL 11.6743 mL 23.3487 mL
5 mM 0.4670 mL 2.3349 mL 4.6697 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.84 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (5.84 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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

Dosage

mg/kg

Animal weight
(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:
%
DMSO +
% 
+
%
Tween-80 +
%
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).
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: 99.84%

COA (252 KB) LCMS (266 KB) Elemental Analysis Report (110 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3349 mL 11.6743 mL 23.3487 mL 58.3717 mL
5 mM 0.4670 mL 2.3349 mL 4.6697 mL 11.6743 mL
10 mM 0.2335 mL 1.1674 mL 2.3349 mL 5.8372 mL
15 mM 0.1557 mL 0.7783 mL 1.5566 mL 3.8914 mL
20 mM 0.1167 mL 0.5837 mL 1.1674 mL 2.9186 mL
25 mM 0.0934 mL 0.4670 mL 0.9339 mL 2.3349 mL
30 mM 0.0778 mL 0.3891 mL 0.7783 mL 1.9457 mL
40 mM 0.0584 mL 0.2919 mL 0.5837 mL 1.4593 mL
50 mM 0.0467 mL 0.2335 mL 0.4670 mL 1.1674 mL
60 mM 0.0389 mL 0.1946 mL 0.3891 mL 0.9729 mL
80 mM 0.0292 mL 0.1459 mL 0.2919 mL 0.7296 mL
100 mM 0.0233 mL 0.1167 mL 0.2335 mL 0.5837 mL
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Eltanexor 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:

Eltanexor1642300-52-4KPT-8602KPT8602KPT 8602CRM1Chromosomal Maintenance 1Exportin 1XPO1Inhibitorinhibitorinhibit

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