CYC065

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CYC065 是 seliciclib 的衍生物，是第二代 CDK 抑制剂，主要作用于 CDK2/5/9。

CYC065 is a derivative of seliciclib and second generation CDK inhibitor that is mainly active on CDK2/5/9; demonstrates cytotoxicity both in MM cell lines sensitive as well as resistant to conventional chemotherapy with IC50 of 0.06-2 uM; blocks cells in the G1 phase and inhibits cell growth specifically in CCNE1-overexpressing USCs; significantly reduces tumour growth in xenografts derived from CCNE1-amplified USCs, shows synergistic effect in vitro and in vivo combined with Taselisib .Brain Cancer Phase 1 Clinical.

Fadraciclib blocks cells in the G1 phase of the cell cycle and inhibits cell growth specifically in cyclin E1 (CCNE1)-overexpressing uterine serous carcinomas (USCs). USC cell lines expressing high CCNE1 mRNA and protein levels to be significantly more sensitive to treatment with Fadraciclib in vitro when compared with low CCNE1-expressing cell lines (IC50: mean±s.d.=124.1±57.8?nM in CCNE1-overexpressing USC cell lines vs 415±117.5?nM in CCNE1 low expressors, respectively; P=0.0003). Importantly, low concentrations of Fadraciclib (i.e., 100?nM) causes an arrest in the G1 phase of the cell cycle only in the CCNE1-overexpressing USC cell lines (i.e., USC-ARK-2, USC-ARK-7) .

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.

CYC-065 | CYC 065

Cell Cycle/DNA Damage

CDK

CDK

Cancer

Brain Cancer

1070790-89-4

397.527

C21H31N7O

>98% (HPLC)

DMSO : ≥ 100 mg/mL251.56 mM

CCC(C(C)O)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NCC3=CN=C(C=C3C)C

(2R,3S)-3-[[6-[(4,6-dimethylpyridin-3-yl)methylamino]-9-propan-2-ylpurin-2-yl]amino]pentan-2-ol

(-20℃)

With Ice Pack

≥ 2 years