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XMU-MP-2

Names

[ CAS No. ]:
2031152-10-8

[ Name ]:
XMU-MP-2

[Synonym ]:
Benzamide, N-[3-[1,4-dihydro-7-[[6-(4-hydroxy-1-piperidinyl)-3-pyridinyl]amino]-1-methylpyrimido[4,5-d]pyrimidin-3(2H)-yl]-4-methylphenyl]-3-(trifluoromethyl)-
N-{3-[7-{[6-(4-Hydroxy-1-piperidinyl)-3-pyridinyl]amino}-1-methyl-1,4-dihydropyrimido[4,5-d]pyrimidin-3(2H)-yl]-4-methylphenyl}-3-(trifluoromethyl)benzamide

Biological Activity

[Description]:

XMU-MP-2 is a potent and selective BRK/PTK6 (breast tumor kinase) inhibitor with biochemical IC50 of 3.2 nM; inhibits the autophosphorylation of BRK Y342 in dose-dependent manner (maximum inhibition at 500 nM), abolishes phosphorylation levels of STAT3 Y705 and STAT5 Y694; blocks proliferation and survival of BRK-transformed Ba/F3 cells with IC50 of 29.7 nM; cooperates strongly with HER2 inhibitor or ER blockade to block breast cancer cell proliferation in vitro and in vivo.

[References]

References 1. Jiang J, et al. Cancer Res. 2017 Jan 1;77(1):175-186. View Related Products by Target Breast Tumor Kinase (BRK;PTK6)

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C32H33F3N8O2

[ Molecular Weight ]:
618.652

[ Exact Mass ]:
618.267883

[ LogP ]:
3.16

[ Index of Refraction ]:
1.659

Related Compounds