GZD856|CAS 1257628-64-0|DC Chemicals

Cas No.:	1257628-64-0
Chemical Name:	GZD856
Synonyms:	GZD856;4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamide;CID 51037822;GZD856,GZD-856;Benzamide, 4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)-
SMILES:	FC(C1C=C(C=CC=1CN1CCN(C)CC1)NC(C1C=CC(C)=C(C#CC2C=NC3=CC=NN3C=2)C=1)=O)(F)F
Formula:	C₂₉H₂₇F₃N₆O
M.Wt:	532.559496164322
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

In Vitro GZD856 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells. GZD856 shows dose-dependent inhibition of PDGFRα and PDGFRβ phosphorylation in H1703 and A549 cells, respectively. The activation of downstream AKT (phosphorylation of S473 but not T308), ERK1/2 and STAT3 is also observed after exposure to GZD856, with no obvious effects on total protein levels. GZD856 induces dose-dependent G0/G1 phase arrest and apoptosis in H1703 cells but not in A549 cells. GZD856 strongly suppresses the proliferation of K562, K562R (Q252H) and murine Ba/F3 cells ectopically expressing Bcr-AblWT and Bcr-AblT315I, with IC50s of 2.2, 67.0, 0.64 and 10.8 nM, respectively. In Vivo GZD856 (10 and 30 mg/kg/day, 16 days) displays good in vivo antitumor activity in both H1703 and A549 lung cancer models. A 25-mg/kg oral dose of GZD856 exhibits a long half-life of 22.2 h, optimal plasma exposure (Cmax, 899.5 μg/L) and a good oral bioavailability of 78%. GZD856 (10 mg/kg/day, 8 days, oral) potently suppresses tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-AblT315I

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