Product Name

Milciclib

General description

Milciclib is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7.

Synonym

PHA-848125; N,1,4,4-tetramethyl-8-[4-(4-methylpiperazin-1-yl)anilino]-5H-pyrazolo[4,3-h]quinazoline-3-carboxamide

Purity

≥98.0%(HPLC)

CAS Number

802539-81-7

Formula

C²⁵H³²N⁸O

Molecular Weight

460.586

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

Solid

Solubility(25°C)

DMSO

≥50mg/mL

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Milciclib is an orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and tropomyosin receptor kinase A (TRKA), with potential antineoplastic activity. CDK2/TRKA inhibitor PHA-848125 AC potently inhibits cyclin-dependent kinase 2 (CDK2) and exhibits activity against other CDKs including CDK1 and CDK4, in addition to TRKA. Inhibition of these kinases may result in cell cycle arrest and apoptosis of tumor cells that express these kinases. CDKs are serine/threonine kinases involved in regulation of the cell cycle and may be overexpressed in some cancer cell types. The neurotrophin receptor TRKA is mutated in a variety of cancer cell types.

l  Storage

Storage temp.

-20°C

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov