For research use only. Not for therapeutic Use.
PD-0332991 isethionate (Cat No.: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.
| Catalog Number | I004991 |
| CAS Number | 827022-33-3 |
| Synonyms | 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one;2-hydroxyethanesulfonic acid |
| Molecular Formula | C₂₄H₂₉N₇O₂.C₂H₆O₄S |
| Purity | ≥95% |
| Target | Cyclin-Dependent Kinases/Cdk4/Cdk6 |
| Solubility | H2O: 50 mg/mL (warmed), DMSO: < 1 mg/mL |
| Storage | 3 years -20C powder |
| Overview of Clinical Research | The phase 2 subprotocol of Palbociclib in patients with tumors harboring activating alterations in cell cycle genes is recruiting. |
| 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 |
| Reference | <p style=”/line-height:25px/”> |
