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Medchemexpress LLC 1H-Indole-2-carbonitrile, 6-hydroxy-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluor... | 1857417-10-7 | 98.2% | 566.60 | 1 MG
Supplier: Medchemexpress LLC HY198101MG
MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM. It is for research use only and not sold to patients.
- Inhibits the proliferation of MLL leukemia cells with a GI50 of 83 nM.
- Shows selectivity towards MLL fusion protein transformed cells.
- Binds to menin with a Kd of 6.5 nM.
- Leads to strong down-regulation of Hoxa9 and Meis1 gene expression.
- Reduces tumor volume in mice xenografts.
- Improved exposure and Cmax in blood plasma.
- Low clearance and a half-life of about 1.6 hours.
- High oral bioavailability (~50%).
- Soluble in DMSO.
- Soluble in various in vivo protocols, including 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline.
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