2031152-10-8

2031152-10-8 structure

Name: XMU-MP-2
Chemical Name: 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
CAS Number: 2031152-10-8
Molecular Formula: C₃₂H₃₃F₃N₈O₂
Molecular Weight: 618.652
Create Date: 2020-01-20 10:40:55
Modify Date: 2024-04-01 20:45:57
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.

Name	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
Synonyms	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

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)