Bulk Inquiry
Palbociclib isethionate
- PD0332991 isethionate
- Parent CAS: 571190-30-2
- Soluble in water and DMSO
- MF: C24H29N7O2.C2H6O4S
- MW: 573.66
Description
Palbociclib isethionate is an orally active, selective CDK4/CDK6 inhibitor. It blocks cyclin D-dependent phosphorylation of retinoblastoma protein, leading to G1 cell-cycle arrest in susceptible tumor cells.
CDK4/6 signaling is a central driver of hormone receptor-positive breast cancer and other proliferative diseases. Palbociclib is useful for studying Rb-dependent cell-cycle control, senescence and CDK4/6 inhibitor response mechanisms.
Key Features
- Selective CDK4/CDK6 inhibitor
- Blocks Rb phosphorylation and G1 progression
- Orally active pharmacological profile
- Relevant to breast cancer cell-cycle research
Applications
- CDK4/6 kinase assays
- Rb pathway studies
- Cancer cell-cycle arrest models
- Breast cancer drug-response profiling
Note: Another salt form, PD0332991 hydrochloride (Axon 1505) is also available.
More Information
| Parent CAS No. | 571190-30-2 |
|---|---|
| Chemical Name | 6-acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one 2-hydroxyethanesulfonate |
| extra_info | . |
| SMILES | C1(NC2=NC=C(N3CCNCC3)C=C2)=NC=C2C(C)=C(C(C)=O)C(=O)N(C3CCCC3)C2=N1.C(O)CS(O)(=O)=O |
| MFCD | MFCD11840850 |
| InChi | InChI=1S/C24H29N7O2.C2H6O4S/c1-15-19-14-27-24(28-20-8-7-18(13-26-20)30-11-9-25-10-12-30)29-22(19)31(17-5-3-4-6-17)23(33)21(15)16(2)32;3-1-2-7(4,5)6/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29);3H,1-2H2,(H,4,5,6) |
| InChiKey | LYYVFHRFIJKPOV-UHFFFAOYSA-N |
| CID | 11478676 |
| Short Description | CDK 4/6 inhibitor |
References
- Malini Guha. Blockbuster dreams for Pfizer's CDK inhibitor. Nature Biotech. 2013, 31, 187.
- RL Sutherland and EA Musgrove. CDK inhibitors as potential breast cancer therapeutics: new evidence for enhanced efficacy in ER+ disease. Breast Cancer Res. 2009, 11(6), 112-113.
- RS Finn et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009, 11(5), R77.
- DW Fry et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol. Cancer Ther. 2004, 3, 1427-1438.
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