• Palbociclib, also known as PD 0332991, is an inhibitor of cyclin-dependent kinases (CDK)4 and CDK6. It inhibited CDK4 and CDK6 with IC50 values of 11 nM and 16 nM, respectively. It inhibited the proliferation of retinoblastoma (Rb)-positive tumor cells in vitro with IC50 values ranging from 40 to 400 nM and induced a G1 arrest with a concomitant reduction of phospho-Ser780/Ser795 on the Rb protein. It also had antitumor activity against a panel of advanced stage human tumor xenografts in vivo. Fry D.W., et al. \"Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts.\" Mol. Cancer Ther. 3: 1427-1438 (2004).
• This research compound is the free base form of palbociclib. We also offer the isethionate salt, hydrochloride salt, and dihydrochloride salt forms; please see Palbociclib, Isethionate Salt, Cat. No. [P-7766], Palbociclib, Hydrochloride Salt, Cat. No. [P-7788], and Palbociclib, Dihydrochloride Salt, Cat. No. [P-7722].
• Palbociclib potently inhibited the phosphorylation of the Rb protein and cell cycle progression through G1 in primary 5T33MM cells in vivo and ex vivo. It induced tumor suppression and a significant improvement in survival of 5T33MM diseased mice. Palbociclib sensitized 5T33MM tumor cells to killing by bortezomib in vitro and prolonged survival in vivo. Menu E., et al. \"A novel therapeutic combination using PD 0332991 and bortezomib: study in the 5T33MM myeloma model.\" Cancer Res. 68: 5519-5523 (2008).
• CDK4/6 inhibition by palbociclib induced a cooperative cytostatic effect in combination with doxorubicin in triple-negative breast cancer (TNBC) cells but ultimately antagonized cytotoxicity. However, palbociclib did not modify the sensitivity of Rb-deficient TNBC cells to doxorubicin-mediated cytotoxic chemotherapy. Palbociclib antagonized doxorubicin-mediated cytotoxicity in vivo in an Rb-dependent manner and allowed tumor cell outgrowth following doxorubicin treatment. McClendon A.K., et al. \"CDK4/6 inhibition antagonizes the cytotoxic response to anthracycline therapy.\" Cell Cycle 11: 2747-2755 (2012).
• This palbociclib product is the free base form, whose CAS number is given above. The CAS number of the isethionate salt form is 827022-33-3, the CAS number of the 1:1.8 hydrochloride salt form is 571189-11-2, the CAS number of the hydrochloride salt form is 827022-32-2, and the CAS number of the dihydrochloride salt form has not been reported as of October 30, 2014.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
• Not available in some countries; not available to some institutions; not available for some uses.

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