化合物 T14340 T14340

Product Introduction
Bioactivity


英文名: Atiratecan

描述: Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1]. Atiratecan does not inhibit acetylcholinesterase (AChE) activities.

体外活性: Atiratecan (TP300) is stable in an acidic solution. However it is rapidly converted to CH0793076 under physiological pH conditions such as in sera[1]. Atiratecan has antiproliferative activity against camptothecin-resistant cell lines and it also has IC50s of 9.4 nM and 1.1 nM for A2780 and A2780/SN75 cells, respectively[1].

体内活性: The eVective dose range of Atiratecan is between 0.30 and 47 mg/kg (MTD/ED50=157). The toxic dose is 63 mg/kg for Atiratecan[1]. Atiratecan (24 mg/kg; IV; once per week for 6 weeks) in combination with capecitabine results in synergistic eVects in the HCT116 human colon cancer and NCI-N87 human gastric cancer xenograft models and an additive eVect in the WiDr human colon cancer xenograft model which is BCRP-positive and CPT-11-insensitive[1]. Atiratecan (TP300; 47 mg/kg; IV; once per week for 3 weeks) shows more than 50% of tumor growth inhibition in all nine models, regardless of the expression of BCRP[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: TP 300 | Atiratecan | TP-300

化合物 T14340 T14340信息由TargetMol中国为您提供，如您想了解更多关于化合物 T14340 T14340报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途