444825 Menin-MLL Interaction Inhibitor, MI-2-2 - Calbiochem

444825
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444825-10MG
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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable thienopyrimidine compound that competes against MLL (Mixed Lineage Leukemia) for menin binding (IC50 = 46 and 520 nM, respectively, against MBM1 sequence MLL4-15 and MLL4-43 containing both MBM1 & MBM2) by targeting menin MLL-binding pocket with high affinity (KD = 22 nM), effectively disrupting cellular menin and MLL-AF9 fusion interaction (by >90% at 12 µM in MLL-AF9-expressing HEK293 cells). Shown to inhibit the oncogenic proliferation of four MLL translocation-harboring human leukemia cell lines (by >95% in 12 d at 6 µM), but not non-MLL leukemia Kasumi-1 and HAL-01 lines (≤16% inhibition at 12 µM), by downregulating MLL target genes expression via simultaneous hematopoietic differentiation induction and killing of non-differentiated population.
      Catalogue Number444825
      Brand Family Calbiochem®
      Synonyms4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine, HCl, MI22
      References
      ReferencesShi, A., et al. 2012. Blood120, 4461.
      Product Information
      FormOff-white powder
      Hill FormulaC₁₇H₂₀F₃N₅S₂ • HCl
      Chemical formulaC₁₇H₂₀F₃N₅S₂ • HCl
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetMenin
      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 Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      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

      Menin-MLL Interaction Inhibitor, MI-2-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      444825

      References

      Reference overview
      Shi, A., et al. 2012. Blood120, 4461.
      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.

      Revision31-October-2013 JSW
      Synonyms4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine, HCl, MI22
      DescriptionA cell-permeable thienopyrimidine compound that competes against MLL (Mixed Lineage Leukemia) for menin binding (IC50 = 46 and 520 nM, respectively, against MBM1 sequence MLL4-15 and MLL4-43 containing both MBM1 & MBM2) by targeting menin MLL-binding pocket with high affinity (KD = 22 nM by ITC), effectively disrupting cellular menin and MLL-AF9 fusion interaction (by >90% at 12 µM in MLL-AF9-expressing HEK293 cells). Shown to inhibit the oncogenic proliferation of four MLL translocation-harboring human leukemia cell lines (by >95% in 12 d cultures with 6 µM MI-2-2), including MV4;11 (MLL-AF4), ML-2 (MLL-AF6), MOLM-13 (MLL-AF9), and KOPN-8 (MLL-ENL), but not non-MLL leukemia Kasumi-1 and HAL-01 lines (≤16% inhibition with 12 µM MI-2-2), by downregulating MLL target genes expression (36% and 31% of DMSO control Hoxa9 and Meis1 mRNA level, respectively, in 4 d 6 µM MI-2-2-treated MV4;11), via simultaneous hematopoietic differentiation induction (5% and 41% CD11b population, respectively, in 10 d MV4;11 culture with DMSO or 6 µM MI-2-2) and killing of non-differentiated population (81% and 63% viability in 2 d MV4;11 culture with DMSO or 6 µM MI-2-2).
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₇H₂₀F₃N₅S₂ • HCl
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      Hygroscopic
      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
      ReferencesShi, A., et al. 2012. Blood120, 4461.