DTS-108 is a prodrug of SN38, a topoisomerase I inhibitor. DTS-108 is a conjugate formed by linking SN38 to a human oligopeptide via an esterase-sensitive cross-linker. DTS-108 has anticancer activity against colorectal cancer, lung cancer, and breast cancer.

Physicochemical Properties

Molecular Formula	C145H233N43O33S2
Molecular Weight	3170.80
CAS #	951792-83-9
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	Top1
ln Vitro	DTS-108 (48 h) is cytotoxic to colon cancer (HCT 116, HT-29, and LS 174T), lung cancer (NCI-H460), and breast cancer (MDA-MB-231) cell lines with IC50 values of 24, 94, 2, 40, and 834 nM, respectively[1]. The half-life of DTS-108 (2.55 μM, 0-48 h) in human and dog plasma is 400 and 290 min, respectively, which is superior to that in mouse plasma (half-life is less than 3 min)[1].
ln Vivo	DTS-108 was not significantly toxic in dogs at doses of 5 or 10 mg/kg, except for a moderate, but not dose-dependent, decrease in white blood cell counts [1]. DTS-108 (32-95 mg/kg, IV, on days 3, 7, and 11) was dose-dependently antitumor in a human tumor xenograft model (HCT116), with a minimum T/C ratio of 10% (at 95 mg/kg) [1]. DTS-108 (IV) was antitumor active in nude mice implanted with colorectal, lung, and breast cancer cells (80 mg/kg, on days 3, 5, 7, 10, 12, 14, 17, 19, and 21) and in rats implanted with colorectal cancer cells (63 mg/kg, on days 14, 18, 21, 25, and 29) [1]. DTS-108 (40 mg/kg, intravenous) has antitumor effects in mice bearing human HT-29 colon cancer cells, and its efficacy is enhanced when combined with 5-FU (40 mg/kg) or bevacizumab (2 mg/kg) [1].
Animal Protocol	Animal/Disease Models: Nude mice implanted into HT-29 (1 × 107) [1] Doses: 40 mg/kg Route of 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) Experimental Results: Exhibited anti-tumor activity in colon cancer mice bearing human HT-29 cells and has increased efficacy in combination with 5-FU or bevacizumab. Animal/Disease Models: 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] Doses: 80 mg/kg (mice); 63 mg/kg (rats) Route of 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) Experimental Results: 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.
References	[1]. 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. [2]. 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.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.3154 mL	1.5769 mL	3.1538 mL
	5 mM	0.0631 mL	0.3154 mL	0.6308 mL
	10 mM	0.0315 mL	0.1577 mL	0.3154 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.