GZD824 Dimesylate

Research use only, not for human use.

GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I).

GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I).

Western Blot Analysis Cell Line:K562 cells Concentration:1 nM, 2 nM, 5 nM, 10 nM, 20nM Incubation Time:4.0 hours Result:Inhibited Bcr-Abl signaling in K562 cell lines.

Animal Model:SCID nude mice, bearing allografted Ba/F3 cells expressing Bcr-AblT315I Dosage:1 mg/kg, 2 mg/kg, 5.0 mg/kg, 10 mg/kg, 20 mg/kg Administration:Oral gavage, daily, for 10 days Result:Efficiently prolonged animal survival in an allograft leukemia tumor model.Animal Model:Rats Dosage:5 mg/kg for i.v.; 25 mg/kg for oral (Pharmacokinetic Analysis)Administration:Intravenous injection and oral administration Result:Oral bioavailability (48.7%), Cmax (390.5 μg/L), T1/2 (5.6 h).

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Proteasome/Ubiquitin

Serine Protease

Abl| Abl (E255K)| Abl (H396P)| Abl (M351T)| Abl (Q252H)

Cancer

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1421783-64-3

724.77

C29H27F3N6O·2CH4O3S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (172.47 mM)

CS(=O)(=O)O.CS(=O)(=O)O.CN1CCN(Cc2c(cc(NC(=O)c3cc(C#Cc4cc5c([nH]nc5)nc4)c(C)cc3)cc2)C(F)(F)F)CC1

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(-20℃)

With Ice Pack

≥ 2 years