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TP 064

Names

[ CAS No. ]:
2080306-20-1

[ Name ]:
TP 064

[Synonym ]:
N-Methyl-N-[(2-{1-[2-(methylamino)ethyl]-4-piperidinyl}-4-pyridinyl)methyl]-3-phenoxybenzamide
Benzamide, N-methyl-N-[[2-[1-[2-(methylamino)ethyl]-4-piperidinyl]-4-pyridinyl]methyl]-3-phenoxy-

Biological Activity

[Description]:

TP-064 is a potent, selective, and cell-active inhibitor of PRMT4 with IC50 of <10 nM and Kd of 7.1 nM, shows high selectivity (>100-fold) for PRMT4 over other PRMTs; reduces dimethylation of BAF155 (IC50=340±30 nM) and MED12 (IC50=43±10 nM) in a dose-dependent manner in cell-baed assays; inhibits the proliferation of a subset of multiple myeloma cell lines (NCI-H929, RPMI8226, Cell IC50 of 379 and 886 nM, respectively) with affected cells arrested in G1 phase of the cell cycle, but has no effect on acute myeloid leukemia, colon cancer, or lung cancer cell lines.

[References]

References 1. Nakayama K, et al. Oncotarget. 2018 Apr 6;9(26):18480-18493. View Related Products by Target Histone Methyltransferase (HMTase)

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
642.8±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C28H34N4O2

[ Molecular Weight ]:
458.595

[ Flash Point ]:
342.5±31.5 °C

[ Exact Mass ]:
458.268188

[ LogP ]:
2.56

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.588

Related Compounds