GZD824 Dimesylate

SKU: orb1223310

Description

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

Key Properties

• CAS Number: 1421783-64-3
• MW: 724.77
• Purity: >98% (HPLC)
• Formula: C₂₉H₂₇F₃N₆O·2CH₄O₃S
• SMILES: 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
• Target: Serine Protease
• Solubility: In Vitro: DMSO : 125 mg/mL (172.47 mM)

Bioactivity

• In Vivo:
  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).
• In Vitro:
  Western blot analysis. Cell line: K562 cells. Concentration: 1 nM, 2 nM, 5 nM, 10 nM, 20 nM. Incubation time: 4.0 hours Result: Inhibited Bcr-Abl signaling in K562 cell lines.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Serine Protease