KPT276

SKU: orb1301097

Description

KPT276 is an orally active, selective inhibitor of nuclear export (SINE) that covalently and irreversibly binds to CRM1. It is used in preclinical research to study CRM1 inhibition in cancer models, demonstrating activity in both in vitro cell assays and in vivo xenograft studies.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1421919-75-6
• MW: 426.26
• Purity: 99.84%
• Formula: C₁₆H₁₀F₈N₄O
• SMILES: FC(F)(F)c1cc(cc(c1)C(F)(F)F)-c1ncn(C=CC(=O)N2CC(F)(F)C2)n1
• Target: CRM1
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:11 mg/mL (25.81 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.69 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• In Vivo:
  KPT-276 significantly prolongs survival of leukemic mice and reduces leukemic burden in a xenograft AML mouse model. KPT-276 significantly suppresses tumor growth in an MCL-bearing severe combined immunodeficient mouse model without severe toxicity. KPT-276 reduces monoclonal spikes in the Vk*MYC transgenic MM mouse model, and inhibits tumor growth in a xenograft MM mouse model.
• In Vitro:
  KPT-276 results in significant growth inhibition and apoptosis induction in MCL cells. KPT-276 specifically and irreversibly inhibits the nuclear export function of XPO1, and reduces the viability of 12 HMCLs. KPT-276 also actively induces apoptosis in primary MM patient samples.

Storage & Handling

• Storage: 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, KPT276, KPT-276, KPT 276

Compound Identifiers

PubChem CID

77992924