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Product Details:

  • Product Name: Palbociclib
  • CAS #: 571190-30-2
  • Mode of Action:

    Palbociclib works as a highly potent and selective inhibitor of CDK4 and -6 in patients with advanced estrogen receptor positive, HER-2 negative breast cancer. When used in conjunction with anticancer therapy Letrozole, Palbociclib has proven to significantly promote progression-free survival in patients. Studies have determined that In vitro, Palbociclib reduced cellular proliferation of ER-positive breast cancer cells by effectively blocking the progression of the cell from the G1 into S phase of the cell cycle.

  • Pharmacodynamics:

    Regarding Cardiac Electrophysiology Palbociclib elicited no substantial change in the QTc interval in studies of patients diagnosed with metastatic estrogen receptor positive, HER-2 negative breast cancer. The binding of Palbociclib to plasma proteins in vitro was valued at 85 percent, with no concentration dependence over the expected range of 500 ng/mL to 5000 ng/mL.

  • Metabolism:

    Palbociclib is metabolized both in vitro and in vivo via hepatic metabolism in humans. Post oral administration of a one-time dose of 125 milligrams of Palbociclib the primary metabolic pathways have been observed to involve both oxidation and sulfonation, along with with glucuronidation and acylation as contributing minor pathways.

  • Toxicity:

    The toxicity of Palbociclib alongside Letrozole was found to be acceptable in extensive and comprehensive studies. Adverse events noted included anemia, neutropenia and fatigue.

  • IUPAC: 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2, 3-d]pyrimidin-7(8H)-one
  • PubChem: 5330286
  • Formula: C24H29N7O2
  • Molecular Mass: 447.5328
  • Synonyms: 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-ylpyridin-2-ylamino)-8H-pyrido(2,3-d)pyrimidin-7-one; OTAVA-BB 1115529; PD-0332991; Palbociclib
  • InChl: InChI=1/C24H29N7O2/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/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29)
  • General Reference:

    Weinberg RA. The Biology of Cancer. 2nd ed. New York: Garland Science; 2014.https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4128689/

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