CYC065
CYC065 is an orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9) with potential antineoplastic and chemoprotective activities. CYC065 selectively binds to and inhibits the activity of CDK2, 5 and 9, which leads to inhibition of CDK2, 5 and 9-dependent cellular pathways, downregulation of genes involved in the pro-survival pathway, prevention of the activation of DNA double-strand break repair pathways, and induction of both cell cycle arrest and apoptosis. This inhibits the proliferation of CDK2/5/9-overexpressing tumor cells. In addition, CYC065 protects hematopoietic stem and progenitor cells (HSPCs), prevents myelosuppression, and preserves the function of the bone marrow.
Note: structure was from Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy Miniperspective Yogesh A. Sonawane, Margaret A. Taylor, John Victor Napoleon, Sandeep Rana, Jacob I. Contreras, and Amarnath Natarajan*
| Chemical | |
|---|---|
| CAS Num | 1070790-89-4 (free base); 1315571-38-0 (HCl) |
| Chemical Formula | C21H31N7O |
| Molecular Weight | 397.527 |
| IUPAC Chemical Name | (2R,3S)-3-((6-(((4,6-dimethylpyridin-3-yl)methyl)amino)-9-isopropyl-9H-purin-2-yl)amino)pentan-2-ol |
| Exact Mass | 397.259 |
| Elemental Analysis | C, 63.45; H, 7.86; N, 24.66; O, 4.02 |
| Synonym | CYC065; CYC-065; CYC 065. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | C[C@@H](O)[C@@H](NC1=NC(NCC2=C(C)C=C(C)N=C2)=C3N=CN(C(C)C)C3=N1)CC |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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