Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

A-966492

🥰Excellent
Catalog No. T6366Cas No. 934162-61-5

A-96649 is a new-type and effective inhibitor. The Ki of A-966492 for PARP1 and PARP2 is 1 nM and 1.5 nM, respectively.

A-966492

A-966492

🥰Excellent
Purity: 99.27%
Catalog No. T6366Cas No. 934162-61-5
A-96649 is a new-type and effective inhibitor. The Ki of A-966492 for PARP1 and PARP2 is 1 nM and 1.5 nM, respectively.
Pack SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$46In Stock
10 mg$91In Stock
25 mg$175In Stock
50 mg$290In Stock
100 mg$415In Stock
200 mg$589In Stock
1 mL x 10 mM (in DMSO)$51In Stock
Bulk & Custom
Add to Cart
Questions
View More

Related Compound Libraries of "A-966492"

Select Batch
Purity:99.27%
Contact us for more batch information
Resource Download
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Product Introduction

Bioactivity
Description
A-96649 is a new-type and effective inhibitor. The Ki of A-966492 for PARP1 and PARP2 is 1 nM and 1.5 nM, respectively.
Targets&IC50
PARP2:1.5 nM(Ki), PARP1:1 nM(ki)
In vitro
A-966492 stands out as a highly potent inhibitor of PARP, demonstrating exceptional efficacy against the PARP-1 enzyme with a Kiof 1 nM and an EC50 of 1 nM in whole-cell assays. It markedly boosts the effectiveness of TMZ in a dose-dependent fashion. Additionally, A-966492 exhibits oral bioavailability in various species, can traverse the blood−brain barrier, and seems to infiltrate tumor tissues effectively. Representing a promising benzimidazole analogue with structural diversity, A-966492 is currently undergoing further preclinical characterization. [1]
In vivo
A-966492 exhibits robust in vivo efficacy, particularly when used in combination with temozolomide (TMZ) in a B16F10 subcutaneous murine melanoma model and carboplatin in an MX-1 breast cancer xenograft model, alongside demonstrating effectiveness as a single agent in a BRCA1-deficient MX-1 tumor model. This compound also showcases excellent pharmaceutical properties, achieving oral bioavailabilities between 34−72% and half-lives of 1.7−1.9 hours in Sprague−Dawley rats, beagle dogs, and cynomolgus monkeys. Furthermore, A-966492 significantly enhances the efficacy of TMZ in a murine B16F10 syngeneic melanoma model, with combination therapy groups showing superior efficacy.
Kinase Assay
PARP Enzyme Assay: The enzyme assay is conducted in buffer containing 50 mM Tris, pH 8.0, 1 mM dithiothreitol(DTT), and 4 mM MgCl2. PARP reactions contains 1.5 μM [3H]-NAD+ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Autoreactions utilizing SPA bead-based detection are carried out in 100 μL volumes in white 96-well plates. Reactions are initiated by adding 50 μL of 2X NAD+ substrate mixture to 50 μL of 2× enzyme mixture containing PARP and DNA. These reactions are terminated by the addition of 150 μL of 1.5 mM benzamide (~1 × 103-fold over its IC50). A 170 μL amount of the stopped reaction mixtures is transferred to streptavidin-coated Flash Plates, incubated for 1 hour, and counted using a TopCount microplate scintillation counter. Ki data are determined from inhibition curves at various substrate concentrations.
Cell Research
C41 cells are treated with A-966492 for 30 minutes in a 96-well plate. PARP are activated by damaging DNA with 1 mM Water2 for 10 minutes. Cells are washed with ice-cold phosphate-buffered saline (PBS) once and fixed with prechilled methanol/acetone (7:3) at -20 °C for 10 minutes. After they are air-dried, plates are rehydrated with PBS and blocked using 5% nonfat dry milk in PBS-Tween(0.05%) (blocking solution) for 30 minutes at room temperature. Cells are incubated with anti-PAR antibody 10H (1:50) in blocking solution at room temperature for 60 minutes followed by washing with PBS-Tween20 five times, and incubation with goat antimouse fluorescein 5(6)-isothiocyanate (FITC)-coupled antibody (1:50) and 1 μg/mL 40,6-diamidino-2-phenylindole (DAPI) in blocking solution at room temperature for 60 minutes. After washing with PBS-Tween20 5 times, analysis is performed using an fmax Fluorescence Microplate Reader set at the excitation and emission wavelength for FITC or the excitation and emission wavelength for DAPI. PARP activity (FITC signal) is normalized with cell numbers (DAPI).(Only for Reference)
Chemical Properties
Molecular Weight324.35
FormulaC18H17FN4O
Cas No.934162-61-5
SmilesNC(=O)c1cccc2[nH]c(nc12)-c1ccc(cc1F)[C@@H]1CCCN1
Relative Density.1.335 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 8.13 mg/mL (25.05 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.0831 mL15.4154 mL30.8309 mL154.1545 mL
5 mM0.6166 mL3.0831 mL6.1662 mL30.8309 mL
10 mM0.3083 mL1.5415 mL3.0831 mL15.4154 mL
20 mM0.1542 mL0.7708 mL1.5415 mL7.7077 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
%Tween 80
%ddH2O

Dose Conversion

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

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

Related Tags: buy A-966492 | purchase A-966492 | A-966492 cost | order A-966492 | A-966492 chemical structure | A-966492 in vivo | A-966492 in vitro | A-966492 formula | A-966492 molecular weight