Atiratecan
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.
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- CAS No.: 867063-97-6
- Formule: C31H34N6O6
- Masse moléculaire:586.64
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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 (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.
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Animal Model:Five-week-old male athymic nude mice (CAnN.CgFoxn1nu/CrlCrlj)[1]
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Dosage:47 mg/kg (the maximum tolerated dose; MTD)
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Administration:IV; once per week for 3 weeks
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Result:Showed more than 50% of tumor growth inhibition in all models, regardless of the expression of BCRP.
Chemical Information
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CAS No. 867063-97-6
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Masse moléculaire 586.64
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Formule C31H34N6O6
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SMILES
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
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Synonyms
TP300
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Atiratecan Related Classifications
HY-14833 Related Classifications
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