LY3177833 (C09-1142-600)

LY3177833 (Example 4) is an orally active CDC7 and pMCM2 inhibitor with IC 50 values of 3.3 nM and 290 nM, respectively. LY3177833 is a senescence inducerIn VitroLY3177833 (10 μM; 4 days) increases SA-β-gal content in Hep3B cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Hep3B cells Concentration: 10 μM Incubation Time: 4 days Result: Increased the expression of human SA-β-gal.In VivoLY3177833 (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female athymic Balb/c nude mice (5-6 weeks old) with SW620 cells 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.Form:SolidIC50& Target:Cdc7 3.3 nM (IC 50 ) pMCM2 290 nM (IC 50 ). Specification: 0.99 Molecular Formula: C16H12FN5O Molecular Weight: 309.3 PubChem CID: 81689696 Isomeric SMILES: C[C@@]1(C2=C(C=C(C=C2)C3=CNN=C3)C(=O)N1)C4=NC=NC=C4F