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Atiratecan

CAS No. : 867063-97-6

MCE 站：Atiratecan

产品活性：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。

研究领域：Others

作用靶点：Others

In Vitro: Atiratecan (TP300) is stable in an acidic solution but is rapidly converted to CH0793076 under physiological pH conditions such as in sera.
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.

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.
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.
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.

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