Tucatinib (Irbinitinib)

An inhibitor of HER2

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库存: 现货

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数量
2mg

￥387.00

310.00

- +
5mg

￥562.00

450.00

- +
10mg

￥987.00

790.00

- +
50mg

￥2725.00

2180.00

- +
100mg

￥4850.00

3880.00

- +

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Background

Tucatinib is an inhibitor of HER2 (IC₅₀ = 14 nM).¹ It inhibits the phosphorylation of HER2 in BT474 breast carcinoma cells (IC₅₀ = 21 nM). Tucatinib inhibits phosphorylation of AKT and induces apoptosis in BT474 cells. In vivo, tucatinib (25-100 mg/kg) inhibits tumor growth in NCI N87 gastric carcinoma and SKOV3 ovarian adenocarcinoma mouse xenograft models. Tucatinib also reduces intratumor phosphorylation of AKT and ERK and inhibits tumor growth in a BT474 mouse xenograft model.

1.Pheneger, T., Bouhana, K., Anderson, D., et al.Abstract #1795: In vitro and in vivo activity of ARRY-380: A potent, small molecule inhibitor of ErbB2AACR Cancer Res.69(9)1795(2009)

Protocol

Animal experiment:

Mice: For the SKOV-3 tumor studies, female nude mice are inoculated with cells subcutaneously in the flank. Animals received: doses of Tucatinib ranging up to 200 mg/kg/d, PO; and/or Trastuzumab at 20 mg/kg, IP, Q3D or QW; and/or RP-56976 at 10 mg/kg, IV, Q3D; and/or Bevacizumab at 10 mg/kg, IP, Q4D x3. Tumor size is measured at regular intervals and subsets of animals are monitored for up to 90 days to determine tumor-free survival[3].

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