| Identification | Back Directory | [Name]
CYC-065 | [CAS]
1070790-89-4 | [Synonyms]
CDK259
CPD1574
CYC065 base
Fadraciclib
CYC065, CDK259
CYC065 free base
Fadraciclib（CYC065）
CYC065; CYC-065; CYC 065;1070790-89-4
(2R,3S)-3-((6-(((4,6-Dimethylpyridin-3-yl)methyl)amino)-9-isopropyl-9H-purin-2-yl)amino)pentan-2-ol
2-Pentanol, 3-[[6-[[(4,6-dimethyl-3-pyridinyl)methyl]amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-, (2R,3S)- | [Molecular Formula]
C21H31N7O | [MDL Number]
MFCD31693062 | [MOL File]
1070790-89-4.mol | [Molecular Weight]
397.52 |
| Chemical Properties | Back Directory | [Boiling point ]
618.3±65.0 °C(Predicted) | [density ]
1.25±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:100.0(Max Conc. mg/mL);251.55(Max Conc. mM) | [form ]
A solid | [pka]
14.62±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases[1] with IC50s of 5 and 26 nM, respectively[2]. | [in vivo]
To evaluate the therapeutic potential of Fadraciclib as a single agent, USC-ARK-2-derived xenografts are treated daily with Fadraciclib (22.5 mg/kg) for a 3-week period. Tumor size and mouse weight are recorded two times a week. The daily administration of Fadraciclib results in a significant reduction of tumor growth compared with the vehicle-treated mice (P=0.012 starting at day 9 of the treatment). No significant weight loss is reported during the entire treatment period[1]. | [IC 50]
CDK2; CDK9 | [References]
[1] Cocco E, et al. Dual CCNE1/PIK3CA targeting is synergistic in CCNE1-amplified/PIK3CA-mutated uterine serous carcinomas in vitro and in vivo. Br J Cancer. 2016 Jul 26;115(3):303-11. DOI:10.1038/bjc.2016.198
[2] Sumana Devata, et al. Molecular markers and venous thromboembolism (VTE) in acute myelogenous leukemia (AML) |
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