Uses
LY3177833 (Example 4) monhydrate is an orally active CDC7 and pMCM2 inhibitor with IC50 values of 3.3 nM and 290 nM, respectively. LY3177833 monhydrate is a senescence inducer[1][2].
Biological Activity
LY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor.
in vivo
LY3177833 (Example 4; 10.4-31.2 mg/kg; oral gavage; twice a day; for 2 weeks; female athymic Balb/c nude mice with SW620 cells) treatment causes significant tumor regression in a dose-dependent manner. Also, no significant tumor growth is observed for 2 weeks after dosing cessation[1].
| Animal Model: | Female athymic Balb/c nude mice (5-6 weeks old) with SW620 cells[1] |
| Dosage: | 10.4 mg/kg, 20.8 mg/kg and 31.2 mg/kg |
| Administration: | Oral gavage; twice a day for 2 weeks |
| Result: | Showed dose dependent antitumor activity in SW620 mouse xenograft tumor model.
|
IC 50
Cdc7: 3.3 nM (IC
50); pMCM2: 290 nM (IC
50)
References
[1] Peter F. Gallagher, et al. Journal of Clinical Oncology. Volume 37, Issue 15_suppl.
