PHA 767491 hydrochloride

Product Description

PHA 767491 hydrochloride is an ATP-competitive cyclin-dependent kinase (cdk) inhibitor (reported IC₅₀ values are 0.034 - 0.75, 0.24 - 1.2, 0.25 - 1.1 and 0.46 - 1 μM for cdk9, cdk2, cdk1 and cdk5, respectively). Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2; IC₅₀ = 171 nM). Prevents initiation of DNA replication. Inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo.

Solubility

Preparing Stock Solutions for PHA 767491 hydrochloride

The following data is based on the product molecular weight 249.70

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

3 2 1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	4.00 mL	20.02 mL	40.05 mL
5 mM	0.80 mL	4.00 mL	8.01 mL
10 mM	0.40 mL	2.00 mL	4.00 mL
50 mM	0.08 mL	0.40 mL	0.80 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Jorda How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases? J.Med.Chem. 2018 PMID: 30234987
• Jackson Stopping replication, at the beginning. Nature Chem.Biol. 2008 PMID: 18488006
• Montagnoli A cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumour activity. Nature Chem.Biol. 2008 PMID: 18469809
• Anderson Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J.Med.Chem. 2007 PMID: 17480064