Fadraciclib, also known as 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.
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Name | Fadraciclib free base |
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Iupac Chemical Name | (2R,3S)-3-((6-(((4,6-dimethylpyridin-3-yl)methyl)amino)-9-isopropyl-9H-purin-2-yl)amino)pentan-2-ol InChi Key: DLPIYBKBHMZCJI-WBVHZDCISA-N |
Synonyms | CYC065; CYC-065; CYC 065; Fadraciclib |
Molecular Formula | C21H31N7O |
Molecular Weight | 397.52 |
Smile | C[C@@H](O)[C@@H](NC1=NC(NCC2=C(C)C=C(C)N=C2)=C3N=CN(C(C)C)C3=N1)CC |
InChiKey | DLPIYBKBHMZCJI-WBVHZDCISA-N |
InChi | InChI=1S/C21H31N7O/c1-7-17(15(6)29)25-21-26-19(18-20(27-21)28(11-24-18)12(2)3)23-10-16-9-22-14(5)8-13(16)4/h8-9,11-12,15,17,29H,7,10H2,1-6H3,(H2,23,25,26,27)/t15-,17+/m1/s1 |
CAS Number | 1070790-89-4 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Bulk | Enquiry | Enquiry | Enquiry |
Formulation | Solid powder |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | |
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. |
HS Code |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
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*