S81131 |
ARRY-380 |
源叶(MedMol) | 99% |
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- 产品描述: Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
- 靶点: HER2;EGFR; HER
- 体内研究:
Tucatinib (ONT-380, 200 mg/kg/d) shows a survival benefit when each drug is dosed at the maximum-tolerated dose. Tucatinib and its active metabolite causes a significant reduction in brain pErbB2 (80%). Tucatinib (ARRY-380) demonstrates significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size) at the higher dose level in 9/12 animals. Tucatinib (50 mg/kg/d) in combination with trastuzumab shows a 98% TGI with complete regressions in 9/12 animals and two partial regressions.
- 参考文献:
1. Moulder-Thompson S, et al. Phase 1 Study of ONT-380, a HER2 Inhibitor, in Patients with HER2+ Advanced Solid Tumors, with an Expansion Cohort in HER2+ Metastatic Breast Cancer (MBC). Clin Cancer Res. 2017 Jan 4. pii: clincanres.1496.2016. 2. Abstract: In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 852. doi:1538-7445.AM2012-852 3. P. Lee, et al. In Vivo Activity of ARRY-380, a Potent, Small Molecule Inhibitor of ErbB2 in Combination with RP-56976. Cancer Research
- 溶解性: DMSO : 41.67 mg/mL (86.72 mM; ultrasonic and warming and heat to 60°C)
- 保存条件: 2-8℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.081 ml 10.405 ml 20.811 ml 5 mM 0.416 ml 2.081 ml 4.162 ml 10 mM 0.208 ml 1.041 ml 2.081 ml 50 mM 0.042 ml 0.208 ml 0.416 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)