KPT-251

SKU: orb1305499

Description

KPT-251 is a small molecule that potently and selectively inhibits nuclear export. It is utilized in cancer research, particularly in studies of leukemia and solid tumors, to investigate the biological consequences of XPO1 inhibition in both cellular and animal models.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1388841-50-6
• MW: 375.23
• Purity: 98.54% (May vary between batches)
• Formula: C₁₄H₇F₆N₅O
• SMILES: C(F)(F)(F)C=1C=C(C=C(C(F)(F)F)C1)C2=NN(/C=C\C3=NN=CO3)C=N2
• Target: Apoptosis,CRM1,Others
• Solubility: DMSO:65 mg/mL (173.23 mM)

Bioactivity

• In Vivo:
  In a systemic metastasis model, following intracardiac injection of PCb2 cells, 80% (8/10) of controls, 10% (1/10) Selinexor- and 20% (2/10) KPT-251-treated animals developed radiographic evidence of lytic bone lesions. Similarly, after intra-tibial injection, the lytic areas were higher in controls than in Selinexor and KPT-251 groups. Analogously, the serum levels of osteoclast markers (mTRAP and type I collagen fragment, CTX), were significantly higher in controls than in Selinexor- and KPT-251-treated animals. Importantly, overall survival and disease-free survival were significantly higher in Selinexor- and KPT-251-treated animals when compared to controls.
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• In Vitro:
  Treatment of Glioblastoma neurosphere cultures with KPT-251 revealed dose-responsive growth inhibition in seven patient-derived GBM lines.

Storage & Handling

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

Alternative Names

A375, antileukemic activity, Apoptosis, CRM1, Chromosomal Maintenance 1, KPT 251, KPT251, KPT-251, myeloid leukemia, inhibit, nuclear export, Inhibitor, melanoma, Exportin 1, XPO1

Compound Identifiers

PubChem CID

57519758