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Canertinib dihydrochloride

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Chemical Structure| 289499-45-2 同义名 : 卡奈替尼二盐酸盐 ;CI-1033 dihydrochloride;PD-183805 dihydrochloride;PD 183805;CI-1033;Canertinib (hydrochloride)
CAS号 : 289499-45-2
货号 : A239262
分子式 : C24H27Cl3FN5O3
纯度 : 98%
分子量 : 558.86
MDL号 : MFCD09954112
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(107.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 25 mg/mL(44.73 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • EGFR/ErbB1

    EGFR, IC50:7.4 nM

  • HER2/ErbB2

    ErbB2, IC50:9 nM
描述 Epidermal growth factor receptor (EGFR) is a tyrosine kinase associated with tumorigenesis. Canertinib dihydrochloride is a potent EGFR inhibitor that inhibits autophosphorylation of EGFR and ErbB2 with IC50 values of 7.4 and 9.0nM, respectively[3]. Canertinib at a concentration of 2–10µM inhibits proliferation of melanoma cells (RaH3 and RaH5) after 72 hours of treatment. Treatment with canertinib at 1 and 10µM for 24 hours inhibits melanoma cell cycle progression and induces apoptosis, respectively. Incubation of melanoma cells with 1µM canertinib for 30 minutes inhibits ErbB1, ErbB2, and ErbB3 receptor phosphorylation. In mice bearing human malignant melanoma xenografts, i.p. injection of canertinib (40 mg/kg/day) significantly inhibits melanoma growth within 18 days of treatment[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00051051 Breast Neoplasms Phase 2 Completed - -
NCT00174356 Carcinoma, Non-Small Cell Lung Phase 1 Completed - United States, Florida ... 展开 >> Pfizer Investigational Site Tampa, Florida, United States, 33612 United States, Illinois Pfizer Investigational Site Park Ridge, Illinois, United States, 60068 Pfizer Investigational Site Skokie, Illinois, United States, 60076 United States, Kentucky Pfizer Investigational Site Louisville, Kentucky, United States, 40202 Pfizer Investigational Site Louisville, Kentucky, United States, 40207 United States, Texas Pfizer Investigational Site Houston, Texas, United States, 77030 Canada, Ontario Pfizer Investigational Site Hamilton, Ontario, Canada, L8V 5C2 收起 <<
NCT00050830 Lung Neoplasms Phase 2 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.79mL

0.36mL

0.18mL

8.95mL

1.79mL

0.89mL

17.89mL

3.58mL

1.79mL
参考文献

[1]Ako E, Yamashita Y, et al. The pan-erbB tyrosine kinase inhibitor CI-1033 inhibits human esophageal cancer cells in vitro and in vivo. Oncol Rep. 2007 Apr;17(4):887-93.

[2]Smaill JB, Rewcastle GW, et al. Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d] pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem. 2000; 43(7): 1380-1397.

[3]Smaill JB, Rewcastle GW, Loo JA, et al. Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem. 2000;43(7):1380-1397.

[4]Djerf Severinsson EA, Trinks C, Gréen H, et al. The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo. Biochem Biophys Res Commun. 2011;414(3):563-568.