Atiratecan  (Synonyms: TP300)

Atiratecan (TP300) is a proagent 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].

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].

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

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].

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

586.64

C₃₁H₃₄N₆O₆

867063-97-6

O=C(O[C@](C(C=C12)=C(CO3)C(N1CC(C2=N4)=C5N(CCCCC)C=NC6=C5C4=CC=C6)=O)(CC)C3=O)CN(C(CN)=O)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Endo M, et al. A water soluble prodrug of a novel camptothecin analog is efficacious against breast cancerresistance protein-expressing tumor xenografts. Cancer Chemother Pharmacol. 2010 Jan;65(2):363-71.  [Content Brief]