Datelliptium chloride is a DNA-intercalating agent derived from ellipticine, with anti-tumor activities.

Datelliptium (100 μM) shows significantly cytotoxic effects after 2 hr of treatment in suspension and primary cultures of rat hepatocytes. Datelliptium mobilizes glycogen in both rat systems in vitro concentration dependently. The half-maximal effect is 14.3 μM in isolated hepatocytes, whereas in cultured rat hepatocytes it is 5.9 μM. Datelliptium also leads to a concentration-dependent decrease in gluconeogenesis from lactate in cells^[1]. Datelliptium acetate is selectively cytotoxic for solid tumors over leukemia L1210. Human tumors H-125 and HCT-116 demonstrates less sensitivity to datelliptium acetate^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Upon intravenous administration, datelliptium acetate shows potent inhibitory activities in vivo against a variety of murine solid tumors. Datelliptium acetate is highly active against early-stage colon #38 with highest non-toxic dose (HNTD) of 170 mg/kg TD, and weight loss of 10%, T/C of 0%^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

397.94

C₂₃H₂₈ClN₃O

105118-14-7

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

In Vitro: 

H₂O : 41.67 mg/mL (104.71 mM; Need ultrasonic)

DMSO : 5 mg/mL (12.56 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

• [1]. Donato MT, et al. Toxicity of the antitumoral drug datelliptium in hepatic cells: Use of models in vitro for the prediction of toxicity in vivo. Toxicol In Vitro. 1992 Jul;6(4):295-302.

  [2]. Mucci-LoRusso P, et al. Activity of datelliptium acetate (NSC 311152; SR 95156A) against solid tumors of mice. Invest New Drugs. 1990 Aug;8(3):253-61.

Cytotoxicity is estimated after short-term exposure (2 hr) to datelliptium using suspended and cultured rat hepatocytes. When cytotoxicity is evaluated after longer-term exposure, using human and rat monolayers and hepatoma cell lines, the compound is added 1 hr after cell plating and incubated for 23 hr. The loss of intracellular LDH and the MTT test are the endpoints evaluated in cultured cells. The intracellular LDH is measured in the microwell culture plates by a colorimetric method. The MTT test, reduction of the tetrazolium salt MTT to formazan by mitochondrial succinate dehydrogenase, is performed as described. Cytotoxicity in the hepatocyte suspension is evaluated by LDH leakage to the medium after a 2-hr treatment with the drug.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Donato MT, et al. Toxicity of the antitumoral drug datelliptium in hepatic cells: Use of models in vitro for the prediction of toxicity in vivo. Toxicol In Vitro. 1992 Jul;6(4):295-302.

  [2]. Mucci-LoRusso P, et al. Activity of datelliptium acetate (NSC 311152; SR 95156A) against solid tumors of mice. Invest New Drugs. 1990 Aug;8(3):253-61.