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

444825
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Descripción

Products

Número de referenciaEmbalaje Cant./Env.
444825-10MG Frasco de vidrio 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®
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
Biological Information
Primary TargetMenin
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
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
Global Trade Item Number
Número de referencia GTIN
444825-10MG 04055977186178