Eltanexor Z-isomer (Synonyms: KPT-8602 (Z-isomer))

Name: Eltanexor Z-isomer
Brand: MedChemExpress
SKU: HY-100423A
Rating: 5.0 (2 reviews)

Cat. No.: HY-100423A Purity: 96.59%: FAQs
Data Sheet SDS COA Handling Instructions

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Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602.

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

Eltanexor Z-isomer Chemical Structure

CAS No. : 1642300-78-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 328	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 328	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 348	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 468	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1380	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 2 publication(s) in Google Scholar

Other Forms of Eltanexor Z-isomer:

Eltanexor In-stock

1 Publications Citing Use of MCE Eltanexor Z-isomer

•Biomed Pharmacother. 2023 Feb 13;160:114402. [Abstract]

Proliferation Assay

: Eltanexor Z-isomer purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Feb 13;160:114402. [Abstract]; A combination of sorafenib and KPT-8602 (30 mg/kg/day; 27 days) has a better tumor inhibition effect than sorafenib alone in xenograft tumor mice model (Fig. A-C).

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Biological Activity
Purity & Documentation
References
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Description

Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor. IC50： In Vitro: Eltanexor Z-isomer exhibits different inhibitory effects on Z138, MM15, 3T3 cell lines, with IC₅₀s of 100 nM-50 μM, < 100 nM, > 30 μM, respectively^[1]. In Vivo:

Molecular Weight

428.29

Formula

C₁₇H₁₀F₆N₆O

CAS No.

1642300-78-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N)/C(C1=CN=CN=C1)=C\N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2

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 : 50 mg/mL (116.74 mM; Need ultrasonic; 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	2.3349 mL	11.6743 mL	23.3487 mL
5 mM	0.4670 mL	2.3349 mL	4.6697 mL
10 mM	0.2335 mL	1.1674 mL	2.3349 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.75 mg/mL (6.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 96.59%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (251 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Vercruysse T et al. The second-generation exportin-1 inhibitor KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia. Clin Cancer Res. 2016 Oct 25. [Content Brief]

[2]. Hing ZA et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia. 2016 Jun 21. [Content Brief]

[3]. Etchin J et al. KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells. Leukemia. 2016 Jun 24. [Content Brief]

Complete Stock Solution Preparation Table

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

Eltanexor Z-isomer 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:

Eltanexor Z-isomer1642300-78-4KPT-8602 (Z-isomer)CRM1Chromosomal Maintenance 1Exportin 1XPO1Inhibitorinhibitorinhibit

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Eltanexor Z-isomer (Synonyms: KPT-8602 (Z-isomer))

Customer Review

Other Forms of Eltanexor Z-isomer:

Eltanexor Z-isomer Related Antibodies

1 Publications Citing Use of MCE Eltanexor Z-isomer

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Eltanexor Z-isomer Related Classifications

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