Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GZD856 is an orally bioavailable PDGFRα/β inhibitor (IC50s: 68.6 and 136.6 nM) with anti-lung cancer activities.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | GZD856 is an orally bioavailable PDGFRα/β inhibitor (IC50s: 68.6 and 136.6 nM) with anti-lung cancer activities. |
Targets&IC50 | PDGFRβ:136.6 nM, PDGFRα:68.6 nM, BCR-ABL (T315I):19.9 nM, BCR-ABL:15.4 nM |
In vitro | 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 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells. |
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%. |
Molecular Weight | 532.56 |
Formula | C29H27F3N6O |
CAS No. | 1257628-64-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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GZD856 1257628-64-0 Angiogenesis Tyrosine Kinase/Adaptors PDGFR GZD 856 GZD-856 inhibitor inhibit