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Atiratecan (Synonyms: TP300)

Cat. No.: HY-14833
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Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models.

For research use only. We do not sell to patients.

Atiratecan Chemical Structure

Atiratecan Chemical Structure

CAS No. : 867063-97-6

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Description

Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

586.64

Formula

C31H34N6O6

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Atiratecan
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HY-14833
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