MilliporeSigma™ Calbiochem™ CRM1 Inhibitor IV, KPT-251

A cell-permeable, irreversible, triazole-containing heterotricyclic CRM1 inhibitor that effectively blocks CRM1-mediated nuclear export (4 h 1μM in U2OS cells) via covalent interaction with CRM1 NES- (nuclear export signal) binding groove cysteine (Cys528 in human)

Supplier:  MilliporeSigma™ 5.00505.0001

Catalog No. 50-050-50001

Description

A cell-permeable, irreversible, triazole-containing heterotricyclic CRM1 inhibitor that effectively blocks CRM1-mediated nuclear export (4 h 1μM in U2OS cells) via covalent interaction with CRM1 NES- (nuclear export signal) binding groove cysteine (Cys528 in human). Exhibits antileukemic activity against primary human CD19⁺ CLL (IC₅₀ <500nM) via apoptosis induction even in the presence of stroma cells or other known CLL survival stimuli, while exhibiting little cytotoxicity toward CD56⁺ NK cells from healthy donors (1μM; up to 72 h). Reported to prolong the survival of SCID mice (75mg/kg p.o.) engrafted with murine Eμ-TCL1 or human MV4-11 leukemia in vivo .

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Specifications

• Form: Solid
• Quantity: 5 mg
• Description: 99% by HPLC
• Molecular Formula: C₁₄H₇F₆N₅O
• Solubility: DMSO

• Content And Storage: Protect from light
• Color: White
• Target Proteins: XPO1
• Formula Weight: 375.23g/mol