DC Chemicals · Product datasheet

KPT-330(Selinexor) — Datasheet

CAT. NO. DC7067

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ParameterValue
Chemical NameSelinexor free base
CAS No.1393477-72-9
SynonymsKPT-330;(S)-1-(3-Ethoxy-4-methoxyphenyl)-2-（methylsulfonyl）ethylamine N-acetyl-L -leucine salt;(Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N'-pyrazin-2-ylprop-2-enehydrazide;ABT-199;KPT 330;Selinexor;Selinexor (KPT-330);(2Z)-3-[3-[3,5-Bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2-propenoic acid 2-(2-pyrazinyl)hydrazide;31TZ62FO8F;(Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide;2-Propenoic acid, 3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-, 2-(2-pyrazinyl)hydrazide, (2Z)-;2-Propenoic acid, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-, 2-(2-pyrazinyl)hydrazide, (2Z)-;Selinexor [USAN:INN];KPT330;Selinexor;Tube706
FormulaC17H11F6N7O
M.Wt443.31
SMILESFC(C1C([H])=C(C(F)(F)F)C([H])=C(C2N=C([H])N(/C(/[H])=C(/[H])\C(N([H])N([H])C3C([H])=NC([H])=C([H])N=3)=O)N=2)C=1[H])(F)F
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

KPT-330, analog of KPT-185, is an orally bioavailable selective CRM1 inhibitor.IC50 value: Target: CRM1in vitro: As the clinical candidate analog of KPT-185, KPT-330 exhibits similar effects on the viability of T-ALL cells and elicits rapid apoptotic response. KPT-330 also reduces cell growth in MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines, with IC50 values of 34-203 nM [1]. in vivo: KPT-330 dramatically suppresses the growth of T-ALL cells (MOLT-4) and AML cells (MV4–11) in vivo, with little toxicity to normal haematopoietic cells [1]. In SCID mice with diffuse human MM bone lesions, KPT-330 inhibits MM-induced bone lysis and prolongs survival. Moreover, KPT-330 directly impairs osteoclastogenesis and bone resorption by blocking RANKL-induced NF-κB and NFATc1, with minimal impact on osteoblasts and BMSCs [2].

In Vitro

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In Vivo

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References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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