Canertinib (CI1033)
爱闪购- 卡奈替尼;CI-1033;PD-183805;CI1033;CI 1033;PD183805;PD 183805
货号: abs812013
货号-规格 | 货期 | 价格 | 数量 |
abs812013-10mg | 现货 | - + | |
abs812013-25mg | 现货 | - + | |
abs812013-50mg | 现货 | - + | |
abs812013-100mg | 现货 | - + |

产品描述 | ||
描述 | Canertinib (CI-1033) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3. | |
纯度 | >98% | |
储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. | |
基本信息 | ||
别名 | 卡奈替尼;CI-1033;PD-183805;CI1033;CI 1033;PD183805;PD 183805 | |
外观 | White powder | |
可溶性/溶解性 | DMSO : 2 mg/mL (4.11 mM) Ethanol : 9 mg/mL (18.52 mM) | |
生物活性 | ||
靶点 | EGFR;ErbB2 | |
In vitro(体外研究) | CI-1033 shows excellent potency for irreversible inhibition of erbB2 autophosphorylation in MDA-MB 453 cells. CI-1033 also shows high permeability in Caco-2 cells and inhibits secretory transport of vinblastine, which indicates that CI-1033 is a likely inhibitor of the P-gp. CI-1033 alone, significantly suppresses constitutively activated Akt and MAP kinase. In combination with gemcitabine, CI-1033 inhibits Akt and prevents increased levels of MAPK phosphorylation. CI-1033 stimulates p27 expression and p38 phosphorylation in MDA-MB-453 cells. CI-1033 is highly specific to the erbB receptor family and not sensitive to PGFR, FGFR or IR even at 50 μM. CI-1033 shows high levels of inhibition in A431 cells expressing EGFR with IC50 of 7.4 nM. CI-1033 suppresses heregulin-stimulated tyrosine phosphorylation of erbB2, erbB3 and erbB4 with IC50 of 5, 14 and 10 nM, respectively. CI-1033 also inhibits expression of pp62c-fos in response to heregulin. CI-1033 is predicted to modify Cys773 covalently within the ATP binding site of the HER2 kinase and enhances destruction of both mature and immature ErbB-2 molecules. CI-1033 induces a significant decrease in measurable phosphorylation of tyrosine residues 845 and 1068 of EGFR, which are responsible for Src and Ras/MAPK signaling respectively. The corresponding residues of Her-2, tyrosine residues 877 and 1248 are dephosphorylated significantly by CI-1033 at a concentration of 3 μM or higher. CI could block EGFR internalization and increase the rate of apoptosis in primary osteosarcoma cells in a titratable fashion. In addition, CI-1033 inhibits the proliferation of TT, TE2, TE6 and TE10 cells significantly at 0.1 nM. | |
In vivo(体内研究) | CI-1033 shows impressive activity against A431 xenografts in nude mice at 5 mg/kg of body weight. CI-1033 (20 to 80 mg/kg/d) achieves a high degree of tumor regressions in H125 xenograft models. Oral administration of CI-1033 causes a marked inhibition of growth in TT, TE6 and TE10 xenografts in nude mice, without animal death and | |
参考文献 | ||
参考文献 | [1] Smaill JB et al. J Med Chem. 2000; 43(7): 1380-1397. [2] Nelson JM et al. J Biol Chem. 2001; 276(18): 14842-14827. [3] Slichenmyer WJ et al. Semin Oncol. 2001; 28(5 Suppl 16): 80-85. [4] Citri A et al. EMBO J. 2002; 21(10): 2407-2417. [5] Hughes DP et al. Pediatr Blood Cancer. 2006; 46(5): 614-623. | |
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
- 实验方法 实验条件
共 0张,还能上传 8张 提交
- 提示: 尊敬的客户您好,如果您对我们的产品有什么疑问或想要了解的,可以点击“我要咨询”按钮填写您的疑问。
提交不成功?请联系info@absin.cn。
促销资讯 更多
订购信息
您可以从我们的授权经销商处购买absin产品或获得技术支持。若要查看您所在地区的经销商,请从以下的下拉列表中选择。