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 |
Molarity Calculator
Reconstitution Calculator
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.
Dilution Calculator
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.
View Related Products by Target
View Related Products by Product Action
Keywords: PHA 767491 hydrochloride, supplier, Dual, cdc7/cdk9, inhibits, inhibitors, MK-2, mitogen-activated, protein, kinase-activated, kinase-2, Cyclin-Dependent, Protein, kinases, Checkpoint, control, PHA767491, hydrochloride, MK2, Tocris Bioscience
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.
Literature in this Area
Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Immunology Product Listing
A collection of over 190 products for immunology research, the guide includes research tools for the study of:
- Chemokine and Cytokine Signaling
- Chemotaxis
- Complement System
- Immune Cell Signaling
- Inflammation
Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
- Receptor Tyrosine Kinases
- Protein Kinases A, C, D and G
- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
- Receptor Serine/Threonine Kinases
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
