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217290 CRM1 Inhibitor IV, KPT-251 (KPT251, (Z)-2-(2-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)vinyl)-1,3,4-oxadiazole, Exportin 1 Inhibitor IV, Chromosome Region Maintenance 1 Protein Inhibitor IV, CRM1 Inhibitor IV, XPO1 Inhibitor IV) CAS:

Specifications
Grade
Highly Purified
Molecular Formula
C₁₄H₇F₆N₅O
Molecular Weight
375.23
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
-20°C

A cell-permeable, irreversible, triazole-containing heterotricyclic CRM1 inhibitor that effectively blocks CRM1-mediated nuclear export (4h 1uM 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 (1uM; up to 72h). Reported to prolong the survival of SCID mice (75mg/kg p.o.) engrafted with murine E-mu-TCL1 or human MV4-11 leukemia in vivo.

Synonyms: (Z)-2-(2-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)vinyl)-1,3,4-oxadiazole, Exportin 1 Inhibitor IV, Chromosome Region Maintenance 1 Protein Inhibitor IV, CRM1 Inhibitor IV, XPO1 Inhibitor IV, KPT251
Molecular Formula
C₁₄H₇F₆N₅O
Solubility
DMSO
Primary Target
XPO1
Molar Mass
375.23
Storage and Stability
Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Purity
~99% (HPLC)
Concentration
Not determined
Form
Supplied as a white solid.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
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