Product Name

Palbociclib Isethionate

General description

Palbociclib Isethionate is the isethionate salt form of palbociclib, an orally available CDK inhibitor with potential antineoplastic activity.

Synonym

6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one; 2-hydroxyethanesulfonic acid; PD0332991 Isethionate

Purity

≥98.0%(HPLC)

CAS Number

827022-33-3

Formula

C²⁴H²⁹N⁷O²·C²H⁶O⁴S

Molecular Weight

573.66

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

Solid

Solubility(25℃)

DMSO

Insoluble

Ethanol

Insoluble

Water

≥5mg/mL(warmed)

l  Biological Information

Biochem/Physiol  Actions

Palbociclib Isethionate is the isethionate salt form of palbociclib, an orally available CDK inhibitor with potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation early in the G1 phase leading to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of cell cycle progression. Palbociclib Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc.

l  Storage

Storage temp.

-20℃

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