产品
编 号：F098402
分子式：C29H27F3N6O
分子量：532.56
分子式：C29H27F3N6O
分子量：532.56
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CAS No: 1257628-64-0
产品详情
生物活性：
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4?nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
体内研究：
GZD856 (10-30 mg/kg, p.o. once daily for 16 d) displays good antitumor activity in both H1703 and A549 lung cancer models and is well tolerated. GZD856 inhibits brain and liver metastasis of lung cancer cells in an A549-Luc orthotopic model.GZD856 (10?mg/kg; p.o. once daily for 8 d) potently inhibits tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-AblT315I.GZD856 (5 mg/kg; a single i.v.) exhibits a long half-life (T1/2=19.97 h), optimal plasma exposure (Cmax=934.38 μg/L) and a AUC0-∞ (8165.8 μg/L?h) in rats.GZD856 (25 mg/kg; a single p.o.) exhibits a long half-life (T1/2=22.2 h), optimal plasma exposure (Cmax=899.5 μg/L) and a good oral bioavailability (BA=78%) in rats.Animal Model:Male CB17-SCID mice implanted with H1703 and A549 cancer cells
Dosage:10, 30 mg/kg
Administration:Oral gavage once daily for 16 days
Result:Displayed antitumor effects in H1703-xenograft mice, with tumor growth inhibition (TGI) values of 20.8% and 74.1% at dosages of 10 and 30 mg/kg, respectively.Displayed antitumor effects in A549-xenograft mice, with a TGI value of 51.1% at 30 mg/kg.Was well tolerated in all of the tested groups, with no mortality or significant loss of body weight.
Animal Model:Sprague-Dawley (SD) rats (180-220?g)
Dosage:5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:A single intravenous injection and oral administration
Result:I.v.: T1/2=19.97 h; Cmax=934.38 μg/L; AUC0-∞=8165.8 μg/L?h.P.o.: T1/2=22.2 h; Cmax=899.5 μg/L; BA=78%.
体外研究：
GZD856 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells.GZD856 (0.3-3 μM; 24-28 h) induces a dose-dependent G0/G1 phase arrest and apoptosis in H1703 but not A549 cells.GZD856 (0.1-10 μM; 6 h) dose-dependently inhibits the PDGFRα/β phosphorylation and downstream signaling in H1703 and A549 cells.GZD856 inhibits 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.
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4?nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
体内研究：
GZD856 (10-30 mg/kg, p.o. once daily for 16 d) displays good antitumor activity in both H1703 and A549 lung cancer models and is well tolerated. GZD856 inhibits brain and liver metastasis of lung cancer cells in an A549-Luc orthotopic model.GZD856 (10?mg/kg; p.o. once daily for 8 d) potently inhibits tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-AblT315I.GZD856 (5 mg/kg; a single i.v.) exhibits a long half-life (T1/2=19.97 h), optimal plasma exposure (Cmax=934.38 μg/L) and a AUC0-∞ (8165.8 μg/L?h) in rats.GZD856 (25 mg/kg; a single p.o.) exhibits a long half-life (T1/2=22.2 h), optimal plasma exposure (Cmax=899.5 μg/L) and a good oral bioavailability (BA=78%) in rats.Animal Model:Male CB17-SCID mice implanted with H1703 and A549 cancer cells
Dosage:10, 30 mg/kg
Administration:Oral gavage once daily for 16 days
Result:Displayed antitumor effects in H1703-xenograft mice, with tumor growth inhibition (TGI) values of 20.8% and 74.1% at dosages of 10 and 30 mg/kg, respectively.Displayed antitumor effects in A549-xenograft mice, with a TGI value of 51.1% at 30 mg/kg.Was well tolerated in all of the tested groups, with no mortality or significant loss of body weight.
Animal Model:Sprague-Dawley (SD) rats (180-220?g)
Dosage:5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:A single intravenous injection and oral administration
Result:I.v.: T1/2=19.97 h; Cmax=934.38 μg/L; AUC0-∞=8165.8 μg/L?h.P.o.: T1/2=22.2 h; Cmax=899.5 μg/L; BA=78%.
体外研究：
GZD856 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells.GZD856 (0.3-3 μM; 24-28 h) induces a dose-dependent G0/G1 phase arrest and apoptosis in H1703 but not A549 cells.GZD856 (0.1-10 μM; 6 h) dose-dependently inhibits the PDGFRα/β phosphorylation and downstream signaling in H1703 and A549 cells.GZD856 inhibits 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.
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