PD-0332991 isethionate

• CAT Number: I004991
• CAS Number: 827022-33-3
• Molecular Formula: C₂₄H₂₉N₇O₂.C₂H₆O₄S
• Molecular Weight: 573.66
• Purity: ≥95%
• Target: Cyclin-Dependent Kinases/Cdk4/Cdk6
• Solubility: H2O: 50 mg/mL (warmed), DMSO: < 1 mg/mL
• Storage: 3 years -20C powder
• IC50: 11 nM/16 nM (Cdk4/Cdk6)
• IUPAC Name: 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one;2-hydroxyethanesulfonic acid
• 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
• SMILES: CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.C(CS(=O)(=O)O)O

PD-0332991 isethionate (CAT: I004991) is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which play a crucial role in cell cycle regulation. By blocking the activity of CDK4/6, PD-0332991 isethionate prevents the phosphorylation of the retinoblastoma protein (Rb), leading to cell cycle arrest in the G1 phase and inhibition of cell proliferation. This compound has shown significant therapeutic potential in the treatment of various cancers, particularly hormone receptor-positive breast cancer. PD-0332991 isethionate, often referred to as palbociclib, has been approved by regulatory authorities as a targeted therapy for advanced breast cancer in combination with endocrine therapy.

Overview of Clinical Research

The phase 2 subprotocol of Palbociclib in patients with tumors harboring activating alterations in cell cycle genes is recruiting. 

Reference

 


[1]. Fry DW, 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(11), 1427-1438.


[2]. Finn RS, 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.


[3]. Katsumi Y, et al. Sensitivity of malignant rhabdoid tumor cell lines to PD 0332991 is inversely correlated with p16 expression. Biochem Biophys Res Commun, 2011, 413(1), 62-68.
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