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500505 CRM1 Inhibitor IV, KPT-251 - Calbiochem

CRM1 Inhibitor IV, KPT-251 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: XPO1
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₄H₇F₆N₅O
Description
OverviewA 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 <500 nM) 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 (1 µM; up to 72 h). Reported to prolong the survival of SCID mice (75 mg/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.
Catalogue Number500505
Brand Family Calbiochem®
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
References
ReferencesEtchin, J., et al. 2013. Leukemia. 27, 66.
Lapalombella, R., et al. 2012. Blood. 120, 4621.
Product Information
FormWhite solid
Hill FormulaC₁₄H₇F₆N₅O
Chemical formulaC₁₄H₇F₆N₅O
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetXPO1
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
500505 0

Documentation

CRM1 Inhibitor IV, KPT-251 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Etchin, J., et al. 2013. Leukemia. 27, 66.
Lapalombella, R., et al. 2012. Blood. 120, 4621.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision17-May-2013 JSW
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
DescriptionA cell-permeable, irreversible, triazole-containing heterotricyclic CRM1 inhibitor that effectively blocks CRM1-mediated nuclear export (complete HIV-1 Rev nuclear retention after 4 h 1µM incubation in RevGFP-expressing U2OS cells) via covalent interaction with Cys528 (numbering based on human sequence) in the CRM1 NES- (nuclear export signal) binding groove, while being ineffective against CRM1C528S-Rev interaction in RevBFP-expressing HeLa cells. Exhibits antileukemic activity in primary human CD19+ CLL (chronic lymphocytic leukemia) cultures (IC50 <500 nM) 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 (1 µM; up to 72 h). KPT-251 is orally available in mice (tmax = 0.5 h; t1/2 = 3.83 h; Cmax = 439 ng/mL; AUCINF = 1590 h·ng/mL; 10 mg/kg p.o.) and reported to prolong the survival of SCID mice (75 mg/kg p.o.) engrafted with murine Eμ-TCL1 (mean survival time = 130.5 d vs. 72 d, respectively, with or without treatment) and human MV4-11 leukemia (62% survival rate on d 60 vs. 24% on d 34, respectively, with or without treatment) in vivo.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₄H₇F₆N₅O
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (25 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesEtchin, J., et al. 2013. Leukemia. 27, 66.
Lapalombella, R., et al. 2012. Blood. 120, 4621.