Art. -Nr.: HY-100423

Eltanexor

(Synonyms: KPT-8602)

3 Cited Publications

Kundenbewertung

Based on 3 publication(s) in Google Scholar

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.

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Reinheit: 99.79%
CAS. Nr.: 1642300-52-4
Formel: C₁₇H₁₀F₆N₆O
Molecular Weight:428.29

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Eltanexor Chemical Structure

CAS. Nr.: 1642300-52-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

XPO1^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
H9	IC₅₀	139.4 nM Compound: KPT-8602	Antiproliferative activity against human H9 cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human H9 cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
MM1.S	IC₅₀	64 nM Compound: KPT-8602	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
NAMALVA	IC₅₀	93.8 nM Compound: KPT-8602	Antiproliferative activity against human NAMALVA cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human NAMALVA cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]
YT	IC₅₀	103.1 nM Compound: KPT-8602	Antiproliferative activity against human YT cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay Antiproliferative activity against human YT cells assessed as inhibition of cell growth incubated for 4 hrs by CCK-8 assay	[PMID: 35367710]

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1642300-52-4
Appearance Solid
Molecular Weight 428.29
Formel C₁₇H₁₀F₆N₆O
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
Synonyms

KPT-8602
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

All WBCell Proliferation/Viability AssayRT-PCRIF

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Journal Impact Factor

Front Microbiol

The Second-Generation XPO1 Inhibitor Eltanexor Inhibits Human Cytomegalovirus (HCMV) Replication and Promotes Type I Interferon Response. [Abstract]

2021 May 3:12:675112. PMID: 34012430

Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112. [Abstract]

Eltanexor (0.05-0.8 μM) inhibited the expression of IE2/86 (encoded by UL122), early protein pp52 (UL44), and late proteins pp71 and pp65 (UL82 and UL83) in a dose-dependent manner in HFFs infected with HCMV.

Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112. [Abstract]

Eltanexor (0.05-0.8 μM) inhibited the production of HCMV progeny virions in a dose-dependent manner.

Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112. [Abstract]

Eltanexor (0.4 μM; 36-96 h) increaseed the transcript levels of UL36, and reduced the transcript levels of UL122, E (UL44) and L (UL82, UL83, UL99, and UL75) genes in HFFs infected with HCMV.

Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112. [Abstract]

Eltanexor (0.4 μM; 6-96 h) significantly reduced IE2, and suppressesed the protein levels of E protein pp52 (encoded by UL44), pp65 (UL83), pp71 (UL82), and L protein pp28 (UL99) after 36 hpi in HFFs infected with HCMV.

Eltanexor purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2021 May 3:12:675112. [Abstract]

Eltanexor (0.4 μM) inhibited the nuclear export of the viral tegument protein pp65 in HFFs infected with HCMV.
Exp Cell Res

KPT-8602 combined with IFN-γ released ZBP1-PANoptosome to inhibit the progression of primary central nervous system lymphoma. [Abstract]

2026 Feb 18;457(2):114946. PMID: 41720446
BMC Cancer

Targeting EP300 in diffuse large b-cell lymphoma: efficacy of A485 and synergistic effects with XPO1 inhibition. [Abstract]

2025 May 28;25(1):955. PMID: 40437414

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.84 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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Eltanexor

3 Cited Publications

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Eltanexor

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

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Publications Citing Use of MedChemExpress (MCE) Eltanexor

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Eltanexor

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Rare Diseases Drug Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Eltanexor

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Eltanexor Related Classifications

Art. -Nr.: HY-100423