Selinexor

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

Neuroscience

Key Properties

• CAS Number: 1393477-72-9
• MW: 443.3
• Purity: >98%
• Formula: C₁₇H₁₁F₆N₇O
• SMILES: FC(F)(F)c1cc(cc(c1)C(F)(F)F)-c1ncn(\C=C/C(=O)NNc2cnccn2)n1
• Target: CRM1,PANoptosis
• Solubility: Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)

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
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• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KPT-330

Compound Identifiers

PubChem CID

71481097