Home Tools
Log in
Cart

Olverembatinib dimesylate

Catalog No. T2429   CAS 1421783-64-3
Synonyms: GZD824 Dimesylate, HQP1351

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Olverembatinib dimesylate Chemical Structure
Olverembatinib dimesylate, CAS 1421783-64-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 33.00
2 mg In stock $ 47.00
5 mg In stock $ 76.00
10 mg In stock $ 122.00
25 mg In stock $ 240.00
50 mg In stock $ 335.00
100 mg In stock $ 498.00
1 mL * 10 mM (in DMSO) In stock $ 123.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 100%
Purity: 99.81%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Olverembatinib dimesylate (GZD824 Dimesylate) is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I).
Targets&IC50 Abl (M351T):0.29 nM, Abl (H396P):0.35 nM, Abl:0.34 nM, Abl (Q252H):0.15 nM, Abl (E255K):0.27 nM
In vitro Administering 20 mg/kg of GZD824 daily inhibits tumor growth in syngeneic transplantation mice bearing Ba/F3 cells expressing Bcr-AblWT and BCR-AblT315I. Daily doses of 5 and 10 mg/kg GZD824 show a dose-dependent inhibition of tumor growth in xenograft models of K562 and KU812 tumors, without causing mortality or weight loss.
In vivo GZD824 effectively inhibits the activation of Bcr-Abl and its downstream targets, Crk1 and STAT5, in leukemia cells in a concentration-dependent manner. Its efficacy in inhibiting the proliferation of Ba/F3 cells expressing the Bcr-Abl T315I mutation and another 14 Bcr-Abl mutations associated with resistance aligns closely with results from biochemical kinase inhibition and protein binding affinity experiments.
Kinase Assay FRET-Based Z′-Lyte Assay Detecting Peptide Substrate Phosphorylation: The kinases ABL1, ABL1(E255K), ABL1 (G250E), ABL1(T315I), and ABL1(Y253F) are P3049, PV3864, PV3865, PV3866, and PV3863 are full-length human recombinant protein expressed in insect cells and histidine-tagged. Inhibition activities of inhibitors against Abl1 and its mutants are performed in 384-well plates using the FRET-based Z′-Lyte assay system. Briefly, the kinase substrate is diluted into 5 μL of kinase reaction buffer; and the kinase is added. Compounds (10 nL) with indicated concentrations are then delivered to the reaction by using Echo liquid handler, and the mixture is incubated for 30 min at room temperature. Then 5 μL of 2X ATP solution is added to initiate the reaction, and the mixture is further incubated for 2 h at room temperature. The resulting reactions contains 10 μM (for wild-type Abl1, and mutants Y253F, Q252H, M351T, and H396P) or 5 μM (for mutants E255K, G250E, T315I) of ATP, 2 μM of Tyr2 Peptide substrate in 50 mM HEPES (PH 7.5), 0.01% BRIJ-35, 10 mM MgCl2, 1 mM EGTA, 0.0247 μg/mL Abl1, and inhibitors as appropriate. Then, 5 μL of development reagent is added, and the mixture is incubated for 2 h at room temperature before 5 μL of stop solution is added. Fluorescence signal ratio of 445 nm (Coumarin)/520 nm (fluorescin) is examined on an EnVision Multilabel Reader. The data are analyzed using Graphpad Prism5. The data are the mean value of three experiments.
Cell Research Cells in the logarithmic phase are plated in 96-well culture dishes. Twenty-four hours later, cells are treated with the corresponding compounds or vehicle control at the indicated concentration for 72 h. CCK-8 is added into the 96-well plates (10 μL/well) and incubated with the cells for 3 h. OD450 and OD650 are determined by a microplate reader. Absorbance rate (A) for each well is calculated as OD450 – OD650. The cell viability rate for each well is calculated as V% = (As – Ac)/(Ab – Ac) × 100%, and the data were further analyzed using Graphpad Prism5. The data are the mean value of the three experiments. As is the absorbance rate of the test compound well, Ac is the absorbance rate of the well without either cell or test compound, and Ab is the absorbance rate of the well with cell and vehicle control.(Only for Reference)
Synonyms GZD824 Dimesylate, HQP1351
Molecular Weight 724.77
Formula C29H27F3N6O·2CH4O3S
CAS No. 1421783-64-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: 92 mg/mL (126.9 mM)

DMSO: 93 mg/mL (128.3 mM)

TargetMolReferences and Literature

1. Ren X, et al. J Med Chem. 2013, 56(3), 879-894.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Angiogenesis related Compound Library Fluorochemical Library NO PAINS Compound Library Clinical Compound Library Anti-Cancer Metabolism Compound Library

Related Products

Related compounds with same targets
Olverembatinib AEE788 Radotinib BCR-ABL-IN-8 c-ABL-IN-5 SKLB 1028 Ponatinib Bosutinib

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Olverembatinib dimesylate 1421783-64-3 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl region-Abelson phosphorylated imatinib GZD824 Dimesylate inhibit linase Inhibitor HQP-1351 nonphosphorylated breakpoint resistance GZD-824 Dimesylate HQP 1351 HQP1351 dimesylate Olverembatinib Dimesylate GZD 824 Dimesylate GZD-824 GZD824 Bcr-Abl(T315I) GZD 824 HQP1351 cluster Olverembatinib inhibitor

 

TargetMol