MI-503( MI 503 | MI503 )

Catalog No. M12868 CAS No. 1857417-13-0

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Product Name

MI-503
Note

Research use only, not for human use.
Brief Description

A highly potent and orally bioavailable small-molecule inhibitor of Menin-MLL interaction with Kd of 9.3 nM.
Description

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

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In Vivo

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Synonyms

MI 503 | MI503
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

Cancer
Indication

Blood cancer

CAS Number

1857417-13-0
Formula Weight

564.6278
Molecular Formula

C28H27F3N8S
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

N#CC(N1CC2=CNN=C2)=CC3=C1C=CC(CN4CCC(NC5=C(C=C(CC(F)(F)F)S6)C6=NC=N5)CC4)=C3C
Chemical Name

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

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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