Atiratecan (TP300) 是喜树碱类似物 CH0793076 (HY-107096) 的前药。Atiratecan 不抑制乙酰胆碱酯酶 (AChE) 活性。Atiratecan 在小鼠异种移植模型中显示出对乳腺癌抗性蛋白 (BCRP) 阳性和阴性异种移植物的抗肿瘤活性。
| 生物活性 | Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breastcancerresistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1]. |
体外研究
(In Vitro) | Atiratecan (TP300) is stable in an acidic solution but is rapidly converted to CH0793076 under physiological pH conditions such as in sera[1].
Atiratecan has antiproliferative activity against camptothecin-resistant cell lines. Atiratecan has IC50s of 9.4 nM and 1.1 nM for A2780 and A2780/SN75 cells, respectively[1].
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体内研究
(In Vivo) | 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].
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].
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].
| Animal Model: | Five-week-old male athymic nude mice (CAnN.CgFoxn1nu/CrlCrlj)[1] | | Dosage: | 47 mg/kg (the maximum tolerated dose; MTD) | | Administration: | IV; once per week for 3 weeks | | Result: | Showed more than 50% of tumor growth inhibition in all models, regardless of the expression of BCRP. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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