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^[1][2].

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 is not significantly toxic at 5 or 10 mg/kg, except for a moderate but not dose-dependent decrease in white blood cell counts in dogs^[1].
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.

3170.80

C₁₄₅H₂₃₃N₄₃O₃₃S₂

951792-83-9

Room temperature in continental US; may vary elsewhere.

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

• [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]