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CAN508

Catalog No. T8796   CAS 140651-18-9

CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. It is also a competitive inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 and 20 μM, respectively.CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.

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CAN508 Chemical Structure
CAN508, CAS 140651-18-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 32.00
5 mg In stock $ 72.00
10 mg In stock $ 138.00
25 mg In stock $ 233.00
50 mg In stock $ 346.00
100 mg In stock $ 513.00
1 mL * 10 mM (in DMSO) In stock $ 81.00
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Purity: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. It is also a competitive inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 and 20 μM, respectively.CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.
Targets&IC50 CDK9-CyclinT1:0.35 μM
In vitro The most potent inhibitor,CAN508, reduced the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays.?Further observed cellular effects included decreased phosphorylation of the retinoblastoma protein and the C-terminal domain of RNA polymerase II, inhibition of mRNA synthesis, and induction of the tumor suppressor protein p53, all of which are consistent with inhibition of CDK9.
Molecular Weight 218.22
Formula C9H10N6O
CAS No. 140651-18-9

Storage

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

Solubility Information

DMSO: 250 mg/mL (1145.63 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Krystof V, et al. 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006;49(22):6500-6509. 2. Tong Z, et al. Antitumor effects of cyclin dependent kinase 9 inhibition in esophageal adenocarcinoma. Oncotarget. 2017;8(17):28696-28710.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Inhibitor Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max Anti-Pancreatic Cancer Compound Library Bioactive Compound Library Cell Cycle Compound Library

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Keywords

CAN508 140651-18-9 Cell Cycle/Checkpoint CDK inhibit CAN-508 ATP-competitive Cyclin dependent kinase esophageal cells Inhibitor adenocarcinoma HT-29 CAN 508 inhibitor

 

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