產品描述: SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations |
靶點:
ERK2:1 nM (IC50);ERK1:4 nM (IC50);ERK;?MEK |
體內研究:
SCH772984 (12.5-50 mg/kg; i.p.; twice daily for 14 days) leads to 98% tumor regression. Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss。 |
參考文獻:
1. Morris EJ, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013 Jul;3(7):742-50. |
溶解性:
DMSO : 48 mg/mL (81.68 mM; Need ultrasonic) |
保存條件:
-20℃ |
配置溶液濃度參考:
|
1mg |
5mg |
10mg |
1 mM |
1.702 ml |
8.508 ml |
17.016 ml |
5 mM |
0.34 ml |
1.702 ml |
3.403 ml |
10 mM |
0.17 ml |
0.851 ml |
1.702 ml |
50 mM |
0.034 ml |
0.17 ml |
0.34 ml |
|
注意: |
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