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PHA-767491

Catalog No. T6206   CAS 845714-00-3
Synonyms: CAY10572, PHA767491, PHA 767491

PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
PHA-767491 Chemical Structure
PHA-767491, CAS 845714-00-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 30.00
5 mg In stock $ 45.00
10 mg In stock $ 63.00
25 mg In stock $ 135.00
50 mg In stock $ 236.00
100 mg In stock $ 426.00
1 mL * 10 mM (in DMSO) In stock $ 45.00
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Purity: 100.00%
Purity: 99.49%
Purity: 99.42%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.
Targets&IC50 Cdc7:10 nM, CDK9:34 nM
Kinase Assay 20 ng of purified human DDK, together with increasing concentrations of each DDK inhibitor is pre-incubated for 5 min. Then 10 μCi (γ)-32P ATP and 1.5 μM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. DDK kinase activity is indicated by Auto-phosphorylation of DDK. 32P-labeled bands are quantified using ImageJ and the IC50 values are calculated using GraphPad.
Cell Research For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC50 values are calculated using the GraphPad software. For assays in six well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 μL of this suspension is mixed with 30 μL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader.
Synonyms CAY10572, PHA767491, PHA 767491
Molecular Weight 213.24
Formula C12H11N3O
CAS No. 845714-00-3

Storage

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

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 24 mg/mL (112.54 mM)

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

TargetMolReferences and Literature

1. Montagnoli A, et al. Nat Chem Biol, 2008, 4(6), 357-365. 2. Yecies D, et al. Blood, 2010, 115(16), 3304-3313. 3. Natoni A, et al. Mol Cancer Ther, 2011, 10(9), 1624-1634.

TargetMolCitations

1. Yu Z, Deng P, Chen Y, et al. Inhibition of the PLK1‐Coupled Cell Cycle Machinery Overcomes Resistance to Oxaliplatin in Colorectal Cancer. Advanced Science. 2021: 2100759. 2. Shan X, Jiang R, Gou D, et al.Identification of a diketopiperazine‐based O‐GlcNAc transferase inhibitor sensitizing hepatocellular carcinoma to CDK9 inhibition.The FEBS Journal.2023

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Ovarian Cancer Compound Library Anti-Liver Cancer Compound Library Antidepressant Compound Library Anti-Cancer Metabolism Compound Library Anti-Lung Cancer Compound Library Glycolysis Compound Library Neuronal Differentiation Compound Library

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Keywords

PHA-767491 845714-00-3 Cell Cycle/Checkpoint GPCR/G Protein PI3K/Akt/mTOR signaling Stem Cells cholecystokinin GSK-3 CDK CAY10572 PHA767491 Cyclin dependent kinase CAY-10572 CAY 10572 inhibit Inhibitor PHA 767491 inhibitor

 

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