Name: Eltanexor (KPT-8602)
Brand: Selleck Chemicals
SKU: S8397
Availability: InStock
Rating: 5 (18 reviews)

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Quality Control

Batch: Purity: 99.66%

99.66

Related Targets	CFTR CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Other CRM1 Inhibitors	KPT-185 Verdinexor (KPT-335) KPT-276 Leptomycin B (LMB)

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (198.46 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.150mg/ml (5.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 43 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	428.29	Formula	C₁₇H₁₀F₆N₆O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1642300-52-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ONO-7706，ATG-016			Smiles	C1=C(C=C(C=C1C(F)(F)F)C(F)(F)F)C2=NN(C=N2)C=C(C3=CN=CN=C3)C(=O)N

Mechanism of Action

Targets/IC₅₀/Ki	XPO1
In vitro	Eltanexor (KPT-8602) is a potent inhibitor of AML cells in cell-based viability assays. It inhibits XPO1/cargo interactions and nuclear export, induces apoptosis of primary CLL cells and significantly inhibits proliferation of diffuse large B-cell lymphoma cell lines
In vivo	Eltanexor (KPT-8602) is orally bioavailable and has similar pharmacokinetic properties to selinexor, but exhibits markedly reduced (approximately 30-fold less) penetration across the blood−brain barrier. Toxicology studies in rats and monkeys indicate that this compound has a substantially better tolerability profile, probably due to its inability to penetrate into the CNS, with reduced anorexia, malaise and weight loss compared to selinexor. It also shows superior anti-leukemic activity and better tolerability in the AML PDX models tested, with nearly complete elimination of human AML cells in the AML-CN model. It is minimally toxic to normal hematopoietic stem and progenitor cells. Furthermore, it does not accumulate in plasma after repetitive dosing and prolongs survival in a human leukemia xenograft model of AML.
References	[1] https://pubmed.ncbi.nlm.nih.gov/27211268/ [2] https://pubmed.ncbi.nlm.nih.gov/27323910/

Applications

Methods	Biomarkers	Images	PMID
Western blot	XPO1		26654943
Immunofluorescence	p53 / NPM1 p62 / p53		27323910

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05918055	Recruiting	Myelodysplastic Syndromes	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	November 14 2023	Phase 1\|Phase 2
NCT02649790	Active not recruiting	Relapsed/Refractory Multiple Myeloma (RRMM)\|Metastatic Colorectal Cancer (mCRC)\|Metastatic Castration-Resistant Prostate Cancer (mCRPC)\|Higher-Risk Myelodysplastic Syndrome (HR-MDS)\|Acute Myeloid Leukemia (AML)\|Newly Diagnosed Intermediate/High-Risk MDS	Karyopharm Therapeutics Inc	January 2016	Phase 1\|Phase 2

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Handling Instructions

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Eltanexor (KPT-8602) CRM1 inhibitor

Chemical Structure

Molecular Weight: 428.29