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

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: MI22, 4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine, HCl

444825
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Overview

Replacement Information

Products

Catalog NumberPackaging Qty/Pack
444825-10MG Glass bottle 10 mg
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®
SynonymsMI22, 4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine, HCl
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
Global Trade Item Number
Catalog Number GTIN
444825-10MG 04055977186178

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
SynonymsMI22, 4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine, HCl
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 Protect from light
+2°C to +8°C
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.
Toxicity Standard Handling
ReferencesShi, A., et al. 2012. Blood120, 4461.