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MI-503

Chemical Structure : MI-503

CAS No.: 1857417-13-0

MI-503 (MI 503;MI503)

Catalog No.: PC-45092Not For Human Use, Lab Use Only.

MI-503 (MI 503) is a highly potent and orally bioavailable small-molecule inhibitor of Menin-MLL interaction with Kd of 9.3 nM.

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Biological Activity

MI-503 (MI 503) is a highly potent and orally bioavailable small-molecule inhibitor of Menin-MLL interaction with Kd of 9.3 nM.
MI-503 effectively induces differentiation of MLL leukemia cells and and substantially increases expression of CD11b, also reduces expression of Hoxa9 and Meis1.
MI-503 induces marked anti-proliferative effects in MV4;11 cells with GI50 of 200 nM.
MI-503 blocks hematologic tumors in vivo and reduces MLL leukemia tumor burden in mouse models.

Physicochemical Properties

M.Wt 564.6278
Formula C28H27F3N8S
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

10 mM in DMSO

Chemical Name/SMILES

1-((1H-pyrazol-4-yl)methyl)-4-methyl-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile

References

1. Borkin D, et al. Cancer Cell. 2015 Apr 13;27(4):589-602.

2. Svoboda LK, et al. Oncotarget. 2017 Jan 3;8(1):458-471.

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