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• 產(chǎn)品描述： Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

• 靶點(diǎn)： HER2;EGFR;?HER

• 體內(nèi)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.

• 參考文獻(xiàn)：
  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)

• 保存條件： 2-8℃

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *