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MI-2-2

Names

[ CAS No. ]:
1454920-20-7

[ Name ]:
MI-2-2

[Synonym ]:
Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-(2,2,2-trifluoroethyl)-
4-[4-(5,5-Dimethyl-4,5-Dihydro-1,3-Thiazol-2-Yl)piperazin-1-Yl]-6-(2,2,2-Trifluoroethyl)thieno[2,3-D]pyrimidine
4-[4-(5,5-Dimethyl-4,5-dihydro-1,3-thiazol-2-yl)-1-piperazinyl]-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine
MFCD29044864

Biological Activity

[Description]:

MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[In Vitro]

MI-2-2 is capable of inhibiting both the interaction of menin with MBM1 (IC50= 46 nM) and with the bivalent fragment of MLL that comprises both MBM1 and MBM2 (IC50=520 nM). MI-2-2 exhibits very pronounced activities at low micromolar concentrations in BMCs transformed with MLL-AF9 and in MV4;11, a human leukemia cell line harboring the MLL-AF4 translocation[1].

[References]

[1]. Shi A, et al. Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia. Blood. 2012;120(23):4461-4469.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
515.1±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C17H20F3N5S2

[ Molecular Weight ]:
415.499

[ Flash Point ]:
265.3±32.9 °C

[ Exact Mass ]:
415.111206

[ LogP ]:
2.22

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.680

[ Storage condition ]:
2-8°C

Related Compounds