Selinexor, Inhibitor of the nuclear export receptor CRM1/XPO1 (TBI4011)

Description

Product Details

Formal Name: (Z)-3-[3-[3,5-Bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N’-pyrazin-2-ylprop-2-enehydrazide

Alternate Names: KPT-330

Molecular Formula: C₁₇H₁₁F₆N₇O

Formula Weight: 443.30

CAS Number: 1393477-72-9

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Inhibitor of the nuclear export receptor CRM1/XPO1

Functions

Selinexor is a first-in-class chemotherapeutic, functioning by binding to Exportin-1 (XPO1, CRM1), a nuclear membrane-associated protein that aids transport of proteins into the cytoplasm. It also helps maintain chromosome structure. Inhibition of these functions in cancer cells results in sensitization to DNA damaging agents, cell cycle arrest, and apoptosis. For example, it suppresses growth of T-cell acute lymphoblastic leukemia (T-ALL) cells (IC50 = 34-203 nM), and pancreatic cancer cells (IC50 ~ 150 nM). Currently in clinical trials for COVID-19 because of its ability to reduce inflammation.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.