Selinexor (KPT-330)

SKU: orb1301068

Description

Selinexor (KPT-330) is an orally bioavailable, selective inhibitor of Exportin 1 (XPO1/CRM1). It induces cell cycle arrest and apoptosis, demonstrating antitumor activity in preclinical models of multiple myeloma, including both in vitro cell studies and in vivo xenograft experiments.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1393477-72-9
• MW: 443.31
• Purity: >99.99% (May vary between batches)
• Formula: C₁₇H₁₁F₆N₇O
• SMILES: FC(F)(F)c1cc(cc(c1)C(F)(F)F)-c1ncn(\C=C/C(=O)NNc2cnccn2)n1
• Target: CRM1
• Solubility: Ethanol:38 mg/mL (85.72 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:8.2 mg/mL (18.5 mM);DMSO:247.5 mg/mL (558.3 mM)

Bioactivity

• Target IC50:
  Jurkat cells:34 - 203 nM|HBP-ALL cells:34-203 nM|ATC cell:150–500 nM|SKW-3 cells:34-203 nM|DND-41 cells:34-203 nM|MOLT-4 cells:34-203 nM|KOPTK-1 cells:34-203 nM|T-ALL cells:34-203 nM
• In Vivo:
  METHODS: To assay antitumor activity in vivo, Selinexor (20-25 mg/kg) was administered by gavage to NSG mice harboring the human T-ALL tumor MOLT-4 three times per week for thirty-six days. RESULTS: Selinexor-treated mice exhibited significant inhibition of leukemia cell growth with significant survival benefit. METHODS: To assay anti-tumor activity in vivo, Selinexor (20 mg/kg) was administered by gavage three times per week for four weeks to an NSG mouse model of primary AML in patients. RESULTS: Selinexor was cytotoxic to primary AML cells transplanted into mice.
• In Vitro:
  METHODS: Six T-ALL cells, MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3 and DND-41, were treated with Selinexor (0-1000 µM) for 72 h. Cell growth inhibition was detected using Cell Titer Glo assay. RESULTS: Selinexor treatment inhibited T-ALL cell growth with IC50 values of 34-203 nM. METHODS: Multiple myeloma cells MM1S were treated with Selinexor (100 nM) for 8 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Selinexor treatment resulted in the accumulation of p53, IκB, p21 and p27 in the nucleus of MM1S cells.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CRM1, KPT 330, KPT330, KPT-330, Selinexor, Selinexor (KPT 330), Selinexor (KPT330)

Compound Identifiers

PubChem CID

71481097