P-7890 Purvalanol A, Free Base, >99%

PRV-101

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• Purvalanol A is a cell-permeable, potent, and selective cyclin-dependent kinase (CDK) inhibitor. It inhibited CDK kinases with IC50 values of 4 nM for CDC2/cyclin B, 70 nM for CDK2/cyclin A, 35 nM for CDK2/cyclin E, 75 nM for CDK5/p35, and 850 nM for CDK4/cyclin D1. Gray N.S., et al. “Exploiting chemical libraries, structure and genomics in the search for kinase inhibitors.” Science 281: 533-538 (1998).
• Purvalanol A inhibited radiation-induced CDC2 kinase activity and induced apoptosis by increasing the levels of active fragments of caspase 3. Lizuka D., et al. “Purvalanol A enhances cell killing by inhibiting up-regulation of CDC2 kinase activity in tumor cells irradiated with high doses of X rays.” Radiat. Res. 167: 563-571 (2007).
• Purvalanol A prevented hippocampal proliferation in a time- and concentration -dependent manner. Mackowiak M., et al. “Purvalanol A, inhibitor of cyclin-dependent kinases attenuates proliferation of cells in the dentate gyrus of the adult rat hippocampus.” Pharmacol. Rep. 57: 845-849 (2005)
• Purvalanol A arrested cells at the G(2)-M phase and induced apoptosis in a concentration-dependent manner. It also concomitantly down-regulated the antiapoptotic protein survivin, a member of the inhibitors of apoptosis protein family. Pennati M., et al. “Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation.” Mol. Cancer Ther. 4: 1328-1337 (2005).
• In synchronized cells, purvalanol A arrested cells in the G1 and G2 phases, but did not prevent DNA synthesis in S-phase cells. After mouse fibroblasts and human cancer cell lines were incubated with purvalanol A for 24 hr, inhibition of cell proliferation and cell death were observed. Villerbu N., et al. “Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities.” Int. J. Cancer 97: 761-769 (2002).
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• 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.
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