GZD824 dimesylate - CAS# 1421783-64-3

GZD824 dimesylate (HQP1351 dimesylate) is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 dimesylate strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 dimesylate has antitumor activity.

Product information

CAS Number: 1421783-64-3

Molecular Weight: 724.77

Formula: C31H35F3N6O7S2

Chemical Name: 4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-3-(2-{1H-pyrazolo[3,4-b]pyridin-5-yl}ethynyl)benzamide; bis(methanesulfonic acid)

Smiles: CN1CCN(CC2=CC=C(C=C2C(F)(F)F)NC(=O)C2C=C(C#CC3=CN=C4NN=CC4=C3)C(C)=CC=2)CC1.CS(O)(=O)=O.CS(O)(=O)=O

InChiKey: LEVIGHXVOVROGW-UHFFFAOYSA-N

InChi: InChI=1S/C29H27F3N6O.2CH4O3S/c1-19-3-5-22(14-21(19)6-4-20-13-24-17-34-36-27(24)33-16-20)28(39)35-25-8-7-23(26(15-25)29(30,31)32)18-38-11-9-37(2)10-12-38;2*1-5(2,3)4/h3,5,7-8,13-17H,9-12,18H2,1-2H3,(H,35,39)(H,33,34,36);2*1H3,(H,2,3,4)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 125 mg/mL (172.47 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

GZD824 dimesylate shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants. GZD824 dimesylate selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells. GZD824 dimesylate inhibits Bcr-Abl signaling in K562 (1-20 nM; 4.0 hours) and Ba/F3 stable cell lines expressing native Bcr-Abl (0.1-100 nM; 4.0 hours) or Bcr-AblT315I(0.1-100 nM; 4.0 hours).

In Vivo:

GZD824 dimesylate suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl WT. GZD824 dimesylate (1-20 mg/kg; i.g.; daily; for 10 days) significantly increases the median survival of the mice bearing allografted Ba/F3 cells expressing Bcr-AblT315I. GZD824 dimesylate exhibits a good oral bioavailability (rat 48.7%) and Cmax (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg). GZD824 dimesylate exhibits terminal elimination half-lives (rat 5.6 h) due to high plasma clearance (rat 1.7 L/h/kg) following intravenous administration (rat 5 mg/kg).

Products are for research use only. Not for human use.