ELTANEXOR, (Z)-

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H10F6N6O
Molecular Weight	428.2913
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

NC(=O)C(=C/N1C=NC(=N1)C2=CC(=CC(=C2)C(F)(F)F)C(F)(F)F)\C3=CN=CN=C3

InChI

InChIKey=JFBAVWVBLRIWHM-MLPAPPSSSA-N

InChI=1S/C17H10F6N6O/c18-16(19,20)11-1-9(2-12(3-11)17(21,22)23)15-27-8-29(28-15)6-13(14(24)30)10-4-25-7-26-5-10/h1-8H,(H2,24,30)/b13-6-

HIDE SMILES / InChI

Description
Sources: https://www.karyopharm.com/pipeline/oral-eltanexor/ | https://adisinsight.springer.com/drugs/800044323

Eltanexor (KPT-8602) is an investigational second-generation Selective Inhibitor of Nuclear Export (SINE) compound that is designed to selectively block the nuclear export protein XPO1. Most of the key tumor suppressor proteins (TSPs), are cargos of XPO1 and inhibition of XPO1 by eltanexor is believed to sequester TSPs in the nucleus where they can carry out their normal functions. Karyopharm Therapeutics is developing eltanexor for the treatment of relapsed/refractory cancers.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Exportin-1 8 Target ID: CHEMBL5661 Sources: https://worldwide.espacenet.com/publicationDetails/biblio?DB=EPODOC&II=0&ND=3&adjacent=true&locale=en_EP&FT=D&date=20141224&CC=WO&NR=2014205389A1&KC=A1	Inhibitor 8297

PubMed

Title	Date	PubMed
KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells.	2017 Jan	27211268
Down-regulation of AR splice variants through XPO1 suppression contributes to the inhibition of prostate cancer progression.	2018 Oct 19	30450161
Nuclear-Cytoplasmic Transport Is a Therapeutic Target in Myelofibrosis.	2019 Apr 1	30563936

Sample Use Guides

In Vivo Use Guide

In Phase 1/2 study in patients with refractory multiple myeloma, using a 3+3 dose escalation design, eltanexor is dosed orally (QDx5 or QoDx3 weekly) for a 28-day cycle with a starting dose of 5 mg.

Route of Administration: Oral

Name

Type

Language

ELTANEXOR, (Z)-

Common Name

English

5-PYRIMIDINEACETAMIDE, .ALPHA.-((3-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-1H-1,2,4-TRIAZOL-1-YL)METHYLENE)-, (.ALPHA.Z)-

Systematic Name

English

(2Z)-3-(3-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-1H-1,2,4-TRIAZOL-1-YL)-2-(PYRIMIDIN-5-YL)PROP-2-ENAMIDE

Systematic Name

English

Code System Code Type Description

PUBCHEM

117763569

Created by admin on Sat Dec 16 13:19:38 GMT 2023 , Edited by admin on Sat Dec 16 13:19:38 GMT 2023

PRIMARY

EPA CompTox

DTXSID301112738

Created by admin on Sat Dec 16 13:19:38 GMT 2023 , Edited by admin on Sat Dec 16 13:19:38 GMT 2023

PRIMARY

FDA UNII

6T69TU098I

Created by admin on Sat Dec 16 13:19:38 GMT 2023 , Edited by admin on Sat Dec 16 13:19:38 GMT 2023

PRIMARY

CAS

1642300-78-4

Created by admin on Sat Dec 16 13:19:38 GMT 2023 , Edited by admin on Sat Dec 16 13:19:38 GMT 2023

PRIMARY

SUBSTANCE RECORD


					6T69TU098I

ELTANEXOR, (Z)-

Details

SMILES

InChI

DescriptionSources: https://www.karyopharm.com/pipeline/oral-eltanexor/ | https://adisinsight.springer.com/drugs/800044323

CNS Activity

Originator

Approval Year

Targets

PubMed

Sample Use Guides

Description
Sources: https://www.karyopharm.com/pipeline/oral-eltanexor/ | https://adisinsight.springer.com/drugs/800044323