For research use only. Not for therapeutic Use.
Purvalanol A（Cat No.:I002639）is a potent and selective inhibitor of cyclin-dependent kinases (CDKs), particularly CDK2, CDK1, and CDK4, which are crucial for regulating cell cycle progression. By inhibiting these CDKs, Purvalanol A induces cell cycle arrest, mainly at the G1 phase, leading to the suppression of cancer cell proliferation. It has been extensively studied in cancer research for its ability to induce apoptosis and enhance the effectiveness of other chemotherapeutic agents. Purvalanol A is valuable in exploring novel cancer therapies targeting cell cycle dysregulation in various malignancies.
| Catalog Number | I002639 |
| CAS Number | 212844-53-6 |
| Synonyms | (R)-2-((6-((3-chlorophenyl)amino)-9-isopropyl-9H-purin-2-yl)amino)-3-methylbutan-1-ol |
| Molecular Formula | C19H25ClN6O |
| Purity | ≥95% |
| Target | Cyclin-Dependent Kinases |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| IUPAC Name | (2R)-2-[[6-(3-chloroanilino)-9-propan-2-ylpurin-2-yl]amino]-3-methylbutan-1-ol |
| InChI | InChI=1S/C19H25ClN6O/c1-11(2)15(9-27)23-19-24-17(22-14-7-5-6-13(20)8-14)16-18(25-19)26(10-21-16)12(3)4/h5-8,10-12,15,27H,9H2,1-4H3,(H2,22,23,24,25)/t15-/m0/s1 |
| InChIKey | PMXCMJLOPOFPBT-HNNXBMFYSA-N |
| SMILES | CC(C)[C@H](CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NC3=CC(=CC=C3)Cl |
| Reference | </br>1:Placental passage of olomoucine II, but not purvalanol A, is affected by p-glycoprotein (ABCB1), breast cancer resistance protein (ABCG2) and multidrug resistance-associated proteins (ABCCs). Hofman J, Kučera R, Neumanova Z, Klimes J, Ceckova M, Staud F.Xenobiotica. 2016;46(5):416-23. doi: 10.3109/00498254.2015.1086039. Epub 2015 Sep 12. PMID: 26364927 </br>2:Purvalanol A, olomoucine II and roscovitine inhibit ABCB1 transporter and synergistically potentiate cytotoxic effects of daunorubicin in vitro. Cihalova D, Hofman J, Ceckova M, Staud F.PLoS One. 2013 Dec 23;8(12):e83467. doi: 10.1371/journal.pone.0083467. eCollection 2013. PMID: 24376706 Free PMC Article</br>3:Purvalanol A is a strong apoptotic inducer via activating polyamine catabolic pathway in MCF-7 estrogen receptor positive breast cancer cells. Obakan P, Arısan ED, Özfiliz P, Çoker-Gürkan A, Palavan-Ünsal N.Mol Biol Rep. 2014 Jan;41(1):145-54. doi: 10.1007/s11033-013-2847-1. Epub 2013 Nov 5. PMID: 24190492 </br>4:Olomoucine II, but not purvalanol A, is transported by breast cancer resistance protein (ABCG2) and P-glycoprotein (ABCB1). Hofman J, Kučera R, Cihalova D, Klimes J, Ceckova M, Staud F.PLoS One. 2013 Oct 8;8(10):e75520. doi: 10.1371/journal.pone.0075520. eCollection 2013. PMID: 24116053 Free PMC Article</br>5:Olomoucine II and purvalanol A inhibit ABCG2 transporter in vitro and in situ and synergistically potentiate cytostatic effect of mitoxantrone. Hofman J, Ahmadimoghaddam D, Hahnova L, Pavek P, Ceckova M, Staud F.Pharmacol Res. 2012 Mar;65(3):312-9. doi: 10.1016/j.phrs.2011.11.017. Epub 2011 Dec 6. PMID: 22173067 </br>6:Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src. Hikita T, Oneyama C, Okada M.Genes Cells. 2010 Oct;15(10):1051-62. doi: 10.1111/j.1365-2443.2010.01439.x. Epub 2010 Sep 5. PMID: 20825494 Free Article</br>7:Two specific drugs, BMS-345541 and purvalanol A induce apoptosis of HTLV-1 infected cells through inhibition of the NF-kappaB and cell cycle pathways. Agbottah E, Yeh WI, Berro R, Klase Z, Pedati C, Kehn-Hall K, Wu W, Kashanchi F.AIDS Res Ther. 2008 Jun 10;5:12. doi: 10.1186/1742-6405-5-12. PMID: 18544167 Free PMC Article</br>8:Purvalanol A induces apoptosis and downregulation of antiapoptotic proteins through abrogation of phosphorylation of JAK2/STAT3 and RNA polymerase II. Iizuka D, Ogura A, Kuwabara M, Inanami O.Anticancer Drugs. 2008 Jul;19(6):565-72. doi: 10.1097/CAD.0b013e3282fe330e. PMID: 18525315 </br>9:Purvalanol A enhances cell killing by inhibiting up-regulation of CDC2 kinase activity in tumor cells irradiated with high doses of X rays. Iizuka D, Inanami O, Kashiwakura I, Kuwabara M.Radiat Res. 2007 May;167(5):563-71. PMID: 17474786 </br>10:Purvalanol A, inhibitor of cyclin-dependent kinases attenuates proliferation of cells in the dentate gyrus of the adult rat hippocampus. Maćkowiak M, Kolasiewicz W, Markowicz-Kula K, Wedzony K.Pharmacol Rep. 2005 Nov-Dec;57(6):845-9. PMID: 16382206 Free Article |
