Palbociclib (PD0332991) Isethionate

SKU: orb1223927

Description

Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

Key Properties

• CAS Number: 827022-33-3
• MW: 573.66
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₉N₇O₂·C₂H₆O₄S
• SMILES: OCCS(O)(=O)=O.CC(=O)C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N3CCNCC3)N=C2N(C2CCCC2)C1=O
• Target: CDK
• Solubility: Water: 50 mg/mL warmed (87.15 mM)

Bioactivity

• In Vivo:
  Animal model: Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted). Dosage: 75, 150 mg/kg, daily for 14 days. Administration: Oral adminstration. Result: Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days. Animal model: Tumor-free female FVB mice. Dosage: 90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 days. Administration: Oral adminstration. Result: Reduced total thymic mass and immature CD4+ and CD8+ double-positive thymocytes, and increased the fractions of CD4+ and CD8+ single-positive thymocytes. Animal model: Genetically engineered mosaic mouse model of liver cancer (Myc; p53-sgRNA). Dosage: 100 mg/kg, daily for 1 week. Administration: Oral adminstration. Result: Decreased the luminescence signal in liver and delayed tumour growth.
• In Vitro:
  Cell Cycle Analysis Cell line: MDA-MB-453 cells. Concentration: 0-1 μM. Incubation time: 24 h. Result: Arrested MDA-MB-453 cells in G1.Cell Proliferation Assay Cell line: ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc. ) Concentration: 0-10 μM. Incubation time: 6 days. Result: Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

CDK