Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-5-thiazolecarboxamide
Purity: ≥98%
Formula Markup: C30H31F3N8O3S
Formula Weight: 640.680469
CAS Number: 903564-48-7
Notes: UM-164 is an inhibitor of Src and p38 MAPK kinases (Kds = 2.7, 2.2, and 5.5 nM for c-Src, p38α, and p38β, respectively).{48199} It also inhibits Fyn, Yes, Lyn, Abl, Arg, Ack, Csk, EphB2, EphB4, and Zak by greater than 75% in a kinome profiling assay using MDA-MB-231 cell lysates when used at a concentration of 500 nM. UM-164 inhibits cell growth in a panel of triple-negative breast cancer (TNBC) cell lines (IC50s = 6.1-260 nM) and in a patient-derived TNBC cell line (IC50 = 320 nM). In MDA-MB-231 and SUM149 cells, UM-164 (1 μM) induces cell cycle arrest at the G1/S phase and inhibits cell motility and invasion when used at concentrations greater than or equal to 50 nM. UM-164 (≥10 mg/kg) reduces tumor growth in SUM149 and MDA-MB-231 mouse xenograft models.
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