| 产品描述: | LY3177833 (Example 4) is an orally active CDC7 and pMCM2 inhibitor with IC50 values of 3.3 nM and 290 nM, respectively. LY3177833 is a senescence inducer |
| 靶点: |
Cdc7:3.3 nM (IC50);pMCM2:290 nM (IC50);CDK |
| 体外研究: |
LY3177833 (10 μM; 4 days) increases SA-β-gal content in Hep3B cells. Western Blot Analysis Cell Line: Hep3B cells Concentration: 10 μM Incubation Time: 4 days Result: Increased the expression of human SA-β-gal. |
| 体内研究: |
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. 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. |
| 参考文献: |
1. Robert Dean Dally, et al. CDC7 Inhibitors. Patent WO2014143601A1. 2. Li X, et al. First-generation species-selective chemical probes for fluorescence imaging of human senescence-associated β-galactosidase. Chem Sci. 2020 Jun 17;11(28):7292-7301. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.233 ml |
16.166 ml |
32.331 ml |
| 5 mM |
0.647 ml |
3.233 ml |
6.466 ml |
| 10 mM |
0.323 ml |
1.617 ml |
3.233 ml |
| 50 mM |
0.065 ml |
0.323 ml |
0.647 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |