[CAS NO. 1393477-72-9]  Selinexor (KPT-330)

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PRODUCTS SPECIFICATIONS [1393477-72-9]

Store
Catalog
SLK-S7252
Brand
Selleck
CAS
1393477-72-9

DESCRIPTION [1393477-72-9]

Overview

MDL-
Molecular Weight443.31
Molecular FormulaC17H11F6N7O
SMILESC(F)(F)(F)C=1C=C(C=C(C(F)(F)F)C1)C2=NN(/C=C\C(NNC=3C=NC=CN3)=O)C=N2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.2558 mL11.2788 mL22.5576 mL
5 mM0.4512 mL2.2558 mL4.5115 mL
10 mM0.2256 mL1.1279 mL2.2558 mL
50 mM0.0451 mL0.2256 mL0.4512 mL

Description

Selinexor (KPT-330, ATG-010) is an orally bioavailable selective inhibitor. Phase 2.

Targets

CRM1 [1]
(Cell-free assay)

In 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.

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. 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.


Synonyms

2-Propenoic acid, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-, 2-(2-pyrazinyl)hydrazide, (2Z)-
KPT 330
Selinexor
Xpovio