DTS-108
DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer.
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- CAS No.: 951792-83-9
- Formule: C145H233N43O33S2
- Masse moléculaire:3170.80
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Stockage:
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Chemical Information
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Activité biologique
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DTS-108 (48 h) is shown to be cytotoxic in a panel of colon (HCT 116, HT-29, and LS 174T), lung (NCI-H460), and breast (MDA-MB-231) cancer cell lines, with IC50 of 24, 94, 2, 40, and 834 nM, respectively[1].
DTS-108 (2.55 μM, 0-48 h) has a half-life of 400 and 290 min in human and dog plasma, respectively, preferable to that in mouse plasma (half-life of <3 min)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DTS-108 (32-95 mg/kg, i.v., on days 3, 7, and 11) shows dose-dependent antitumor activity in a human tumor xenograft model (HCT116), with a minimal T/C ratio of 10% (at 95 mg/kg)[1].
DTS-108 (i.v.) exhibits anti-tumor activity in nude mice (80 mg/kg, on days 3, 5, 7, 10, 12, 14, 17, 19, and 21) implanted with colorectal, lung, and breast cancer cells and rats (63 mg/kg, on days 14, 18, 21, 25, and 29) implanted with colorectal cancer cells[1].
DTS-108 (40 mg/kg, i.v.) shows antitumor activity in colon cancer mice bearing human HT-29 cells and has increased efficacy in combination with 5-FU (HY-90006) (40 mg/kg) or Bevacizumab (HY-P9906) (2 mg/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice implanted into HT-29 (1 × 107) [1]
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Dosage:40 mg/kg
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Administration:Intravenous injection (i.v.), on days 3, 6, 10, 13, 17, and 20 (with 5-FU); on days 3, 7, 11, 17, 21, and 25 (with bevacizumab)
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Result:Exhibited anti-tumor activity in colon cancer mice bearing human HT-29 cells and has increased efficacy in combination with 5-FU or bevacizumab.
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Animal Model:7-wk-old female nude mice implanted into HCT 116 (1 × 107), NCI-H460 (3 × 106), MDA-MB-231 (3 × 106); Rh rnu/rnu nude rats implanted into LS 174T (2 × 107)[1]
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Dosage:80 mg/kg (mice); 63 mg/kg (rats)
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Administration:Intravenous injection (i.v.), on days 3, 5, 7, 10, 12, 14, 17, 19, and 21 (mice); on days 14, 18, 21, 25, and 29 (rats)
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Result:Exhibited anti-tumor activity in nude mice implanted with HCT 116, NCI-H460, and MDA-MB-231 cells, with minimum T/C ratios of 3%, 23%, and 29%, respectively.
Exhibited antitumoral efficacy (with a minimal T/C ratio of 44%) in rats bearing LS 174T.
Chemical Information
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CAS No. 951792-83-9
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Masse moléculaire 3170.80
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Formule C145H233N43O33S2
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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
[1]. Meyer-Losic, et al. DTS-108, a novel peptidic prodrug of SN38: in vivo efficacy and toxicokinetic studies. Clinical cancer research : an official journal of the American Association for Cancer Research. 2008, 14(7), 2145–2153. [Content Brief]
[2]. Coriat, et al. Pharmacokinetics and safety of DTS-108, a human oligopeptide bound to SN-38 with an esterase-sensitive cross-linker in patients with advanced malignancies: a Phase I study. International journal of nanomedicine. 2016, 11, 6207–6216. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DTS-108 Related Classifications
HY-P10765 Related Classifications
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