500505 | CRM1 Inhibitor IV, KPT-251 - Calbiochem

500505
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₄H₇F₆N₅O

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00505.0001
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          Glass bottle 5 mg
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          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
          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

          Documentation

          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 -20°C
          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.
          Toxicity Standard Handling
          ReferencesEtchin, J., et al. 2013. Leukemia. 27, 66.
          Lapalombella, R., et al. 2012. Blood. 120, 4621.