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MI-538

Chemical Structure : MI-538

CAS No.: 1857417-10-7

MI-538 (MI538;MI 538)

Catalog No.: PC-45727Not For Human Use, Lab Use Only.

MI-538 is potent and selective menin-MLL interaction inhibitor (IC50=21 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MI-538 is potent and selective menin-MLL interaction inhibitor (IC50=21 nM).
MI-538 shows the most potent binding affinity to menin (Kd = 6.5 nM) obtained for small molecule menin–MLL inhibitor reported to date.
MI-538 exhibits significantly increased activity, selectivity, polarity and pharmacokinetic profile over MI-136 and demonstrates a pronounced effect in a mouse model of MLL leukemia.

Physicochemical Properties

M.Wt 566.6006
Formula C27H25F3N8OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO; Need ultrasonic and warming

Chemical Name/SMILES

1H-Indole-2-carbonitrile, 6-hydroxy-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-

References

1. Borkin D, et al. J Med Chem. 2016 Feb 11;59(3):892-913.

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