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

444825
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      444825-10MG
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      Stocked 
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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
          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

          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.