GZD856 formic 是一种有效的和具有口服活性的 PDGFRα/β 抑制剂，IC₅₀ 值分别为 68.6 和 136.6 nM。GZD856 formic 也是 Bcr-Abl^T315I 的抑制剂，对天然 Bcr-Abl 和 T315I 突变型的 IC₅₀ 值分别为 19.9 和 15.4 nM。GZD856 formic 具有抗肿瘤活性。

GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC 50 s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl inhibitor, with IC 50 s of 19.9 and 15.4?nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.

Solid

PDGFRα 68.6 nM (IC50) PDGFRβ 136.6 nM (IC

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-Abl and Bcr-Abl, with IC50s of 2.2, 67.0, 0.64 and 10.8?nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

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-Abl.
GZD856 (5 mg/kg; a single i.v.) exhibits a long half-life (T 1/2 =19.97 h), optimal plasma exposure (C max =934.38 μg/L) and a AUC 0-∞ (8165.8 μg/L?h) in rats.
GZD856 (25 mg/kg; a single p.o.) exhibits a long half-life (T 1/2 =22.2 h), optimal plasma exposure (C max =899.5 μg/L) and a good oral bioavailability (BA=78%) in rats. has not independently confirmed the accuracy of these metho

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Zhang Z, et, al. GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo. Cancer Lett. 2016 May 28;375(1):172-178.
[2]. Lu X, et, al. Synthesis and identification of GZD856 as an orally bioavailable Bcr-Abl T315I inhibitor overcoming acquired imatinib resistance. J Enzyme Inhib Med Chem. 2017 Dec;32(1):331-336.

In Vitro: DMSO : 100 mg/mL (172.84 mM; Need ultrasonic)配制储备液