PALBOCICLIB (PD-0332991) (HCL SALT)

Background Information:

Palbociclib (PD-0332991) is an orally bioavailable, potent and highly selective cyclindependent kinase 4 and 6 (CDK 4/6) with IC₅₀ at 11 and 16 nM, respectively.

Reference:

1. Rivadeneira, Dayana B.; Mayhew, Christopher N.; Thangavel,
Chellappagounder; Sotillo, Elena; Reed, Christopher A.; Grana, Xavier;
Knudsen, Erik S. Proliferative suppression by CDK4/6 inhibition: complex
function of the retinoblastoma pathway in liver tissue and hepatoma
cells. Gastroenterology (2010), 138(5), 1920-1930.
2. Dean, J. L.; Thangavel, C.; McClendon, A. K.; Reed, C. A.; Knudsen,
E. S. Therapeutic CDK4/6 inhibition in breast cancer: key mechanisms of
response and failure. Oncogene No pp. yet given. CODEN: ONCNES
ISSN:0950-9232. AN 2010:612647.
3. Michaud, Karine; Solomon, David A.; Oermann, Eric; Kim, Jung-Sik;
Zhong, Wei-Zhu; Prados, Michael D.; Ozawa, Tomoko; James, C. David;
Waldman, Todd. Pharmacologic Inhibition of Cyclin-Dependent Kinases 4
and 6 Arrests the Growth of Glioblastoma Multiforme Intracranial
Xenografts. Cancer Research (2010), 70(8), 3228-3238.

APIM050217: PALBOCICLIB (PD-0332991) (HCL SALT)

CAS No.: 827022-32-2
Molecular Formula: C₂₄H₂₉N₇O₂ ? HCl.
Molecular Weight: 484.0 (or refer to Certificate of Analysis).
Purity: >99.5% (HPLC at 214 and 254 nm).
QC: HPLC, ¹HNMR.
Solubility: Soluble in DMSO and water.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.