Protein Inhibitors - Olverembatinib dimesylate (CAS: 1421783-64-3)

Olverembatinib dimesylate (CAS: 1421783-64-3)

Catalog #：EBC51164

Biological Activity

Synonyms

GZD824 dimesylate; HQP1351 dimesylate

Chemical Name

3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide dimethanesulfonate

Application

Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor.

CAS Number

1421783-64-3

Purity

≥99.0%

Molecular Weight

724.77

Molecular Formula

C31H35F3N6O7S2

SMILES

CC1=CC=C(C(NC2=CC=C(CN3CCN(C)CC3)C(C(F)(F)F)=C2)=O)C=C1C#CC4=CN=C5C(C=NN5)=C4.CS(=O)(O)=O.CS(=O)(O)=O

Target & IC50

Bcr-AblT315I : IC50=0.68 nM

Shipping

Gel Pack

Storage

Store at -20°C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	1 mg	5 mg	10 mg
1 mM	1.3797 ml	6.8987 ml	13.7975 ml
5 mM	0.2759 ml	1.3797 ml	2.7595 ml
10 mM	0.1380 ml	0.6899 ml	1.3798 ml
50 mM	0.0276 ml	0.1380 ml	0.2760 ml

Solubility
DMSO: 125 mg/mL (172.47 mM) Water: 50 mg/mL (68.99 mM)

Product Description

Olverembatinib dimesylate also known as GZD824 is an orally bioavailable Bcr-Abl inhibitor. GZD824 exhibited high affinity with Kd values of 0.32 and 0.71 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GZD824 inhibited Bcr-Abl with IC50 values of 0.34, 0.68, 0.27, 0.71, 0.15, 0.35, 0.29 and 0.35 nM for Bcr-AblWT, Bcr-AblT315I, Bcr-AblE255K, Bcr-AblG250E, Bcr-AblQ252H, Bcr-AblH396P, Bcr-AblM351T and Bcr-AblY253F, respectively. In a competitive binding assay, GZD824 bound to the ATP-binding sites of native Abl with Kd values of 0.32 and 0.34 nM for non-phosphorylated and phosphorylated Abl. In stably transformed Ba/F3 cells, GZD824 potently inhibited cells growth with IC50 values of 1.0 and 7.1 nM for Bcr-AblWT and Bcr-AblT315I expressed cells, respectively.