ICG1035-Canertinib, Canertinib, Dihydrochloride Salt
- 型号：ICG1035-Canertinib,
- 供应商：上海翊圣生物科技有限公司
- 供应商报价：面议
- 标签：Canertinib, Dihydrochloride Salt,-1,上海翊圣生物科技有限公司
产品库
ICG1035-Canertinib, Dihydrochloride Salt
Canertinib, Dihydrochloride Salt，>98%
【英文同义名】：CI-1033, 289499-45-2, Canertinib HCl, PD-183805, Canertinib dihydrochloride [USAN], PD-0183805, CI1033, AC1L4G5O
【中文同义名】：卡奈替尼二*酸*
订购信息：（原装进口，常备现货）
品 Pai | 产品名称 | 产品货号 | 规 格 | 目录价（元） |
Gene Operation | ICG1035-0010MG | 10 mg | ¥569.00 | |
ICG1035-0025MG | 25 mg | ¥1,259.00 | ||
ICG1035-0050MG | 50 mg | ¥2,159.00 | ||
ICG1035-0100MG | 100 mg | ¥3,839.00 |
产品描述是Canertinib的二*酸*，是一种可以口服的、不可逆的广谱ErbBYZ剂，能够有效YZEGFR和ErbB2，其IC50分别为1.5 nM和9.0 nM，但对PDGFR, FGFR, InsR, PKC和CDK1/2/4等无YZ活性 [1]。Canertinib能显著YZMDA-MB453细胞ErbB2自体磷酸化 [1]。Canertinib不仅能够YZErbB2自磷酸化，同时也能增强ErbB2的泛素化以及加速内吞作用及随后的ErbB2的细胞内降解 [2]。Canertinib能通过YZ酪氨酸激酶信号通路，阻止细胞生长，YZ细胞G(1)期，促进P53的表达，并诱导细胞凋亡增强放射治LX果 [3]。Canertinib显著YZ黑色素瘤细胞RaH3和RaH5的增殖，并能YZ这两种细胞的裸鼠移植瘤的生长 [4]。Canertinib已经进入三期临床试验用于ZL未分类的成人实体肿瘤及其皮肤科并发症。
靶点
靶点 | EGFR | ErbB2 |
IC50（半数有效浓度） | 1.5 nM | 9.0 nM [1] |
化学特性
Cas No.: 289499-45-2 | M. Wt.: 558.86 |
Formula: C24H27Cl3FN5O3 | Purity: >98% |
Synonym: CI-1033, 289499-45-2, Canertinib HCl, PD-183805, Canertinib dihydrochloride [USAN], PD-0183805, CI1033, AC1L4G5O | |
Chemical Name: N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide;dihydrochloride | |
Appearance: white powder | |
Solubility: Soluble in DMSO (up to 100 mg/mL) | |
Storage：Store powder at -20 ºC for the stability of three years | |
储存液 (1 ml DMSO体系) | 1 mM | 5 mM | 10 mM | 25 mM | 50 mM | 100 mM |
质量(mg) | 0.5589 | 2.7943 | 5.5886 | 13.9715 | 27.9430 | 55.8860 |
使用浓度(仅作参考)Canertinib的具体使用浓度请参考相关文献，并根据自身实验条件（如实验目的，细胞种类，培养特性等）进行摸索和优化。
参考文献[1] Smaill, J. B. 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. Journal of medicinal chemistry 43, 1380-1397 (2000).
[2] Citri, A. et al. Drug-induced ubiquitylation and degradation of ErbB receptor tyrosine kinases: implications for cancer therapy. The EMBO journal 21, 2407-2417 (2002).
[3] Nyati, M. K. et al. Radiosensitization by pan ErbB inhibitor CI-1033 in vitro and in vivo. Clinical cancer research : an official journal of the American Association for Cancer Research 10, 691-700 (2004).
[4] Djerf Severinsson, E. A. et al. The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo. Biochemical and biophysical research communications 414, 563-568 (2011).
