PHA 767491 hydrochloride
Biological Activity
Potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. Inhibits cell proliferation in a variety of human cell lines (IC50 ~ 0.86 - 5.87 μM) and induces apoptosis in a p53-independent manner in vivo. Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2) (IC50 = 171 nM).
Compound Libraries
PHA 767491 hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 249.7 |
| Formula | C12H11N3O.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 942425-68-5 |
| PubChem ID | 11715766 |
| InChI Key | IMVNFURYBZMFDZ-UHFFFAOYSA-N |
| Smiles | O=C1NCCC2=C1C=C(C3=CC=NC=C3)N2.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.97 | 100 | |
| water | 24.97 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 249.7. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4 mL | 20.02 mL | 40.05 mL |
| 5 mM | 0.8 mL | 4 mL | 8.01 mL |
| 10 mM | 0.4 mL | 2 mL | 4 mL |
| 50 mM | 0.08 mL | 0.4 mL | 0.8 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Anderson et al (2007) Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J.Med.Chem. 50 2647 PMID: 17480064
Jackson (2008) Stopping replication, at the beginning. Nature Chem.Biol. 4 331 PMID:
Montagnoli et al (2008) A cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumour activity. Nature Chem.Biol. 4 357 PMID:
If you know of a relevant reference for PHA 767491 hydrochloride, please let us know.
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Keywords: Dual cdc7/cdk9 inhibits inhibitors MK-2 mitogen-activated protein kinase-activated kinase-2 Cyclin-Dependent Protein kinases Checkpoint control PHA767491 hydrochloride MK2
2 Citations for PHA 767491 hydrochloride
Citations are publications that use Tocris products. Selected citations for PHA 767491 hydrochloride include:
Gardner et al (2011) Geminin overexpression prevents the completion of topoisomerase IIα chromosome decatenation, leading to aneuploidy in human mammary epithelial cells. Breast Cancer Res 13 R53 PMID: 21595939
FitzGerald et al (2014) A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response. PLoS One 9 e98891 PMID: 24902048
Do you know of a great paper that uses PHA 767491 hydrochloride from Tocris? If so please let us know.
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