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MedChemExpress - Model Atiratecan -867063-97-6
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].MCE products for research use only. We do not sell to patients.
Atiratecan
MCE China:Atiratecan
Brand:MedChemExpress (MCE)
Cat. No.HY-14833
CAS:867063-97-6
Synonyms:TP300
Storage:Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping:Room temperature in continental US; may vary elsewhere.
Description: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.
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].
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].
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References:
[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]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas;
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects;
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services;
• It has a professional experimental center and strict quality control and verification system;
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products;
• The biological activity of the products has been verified by the experiments of customers in various countries;
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers;
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world;
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。
