PHA 767491 hydrochloride

Name: PHA 767491 hydrochloride
Brand: Tocris Bioscience
SKU: 3140

Tocris Bioscience, part of Bio-Techne | Catalog # 3140

Citations (9)

COA / SDS

Cdk inhibitor; potently inhibits cdk9; also inhibits MK2

Key Product Details

Description:	Cdk inhibitor; potently inhibits cdk9; also inhibits MK2
Chemical Name:	1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	249.7

View Full Technical Details for PHA 767491 hydrochloride

Technical Data
Citations

Biological Activity for PHA 767491 hydrochloride

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.

Compound Libraries for PHA 767491 hydrochloride

PHA 767491 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for PHA 767491 hydrochloride

M. Wt	249.7
Formula	C₁₂H₁₁N₃O.HCl
Storage	Desiccate at RT
Purity	≥98% (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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PHA 767491 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	24.97	100
	DMSO	24.97	100

Preparing Stock Solutions for PHA 767491 hydrochloride

The following data is based on the product molecular weight 249.7.

Batch specific molecular weights may vary from batch to batch due to the degree 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	4.00 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

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References for PHA 767491 hydrochloride

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