Adarotene-(ST1926)-Apoptosis-Activator-MedChemExpress

Adarotene

体内研究Adarotene (15, 20 mg/kg, p.o.) causes a significant tumor growth inhibition in a human ovarian carcinoma, A2780/DX, and in a human melanoma, MeWo, growing in nude mice[1]. Adarotene (30, 40 mg/kg, p.o.) results in a significant and

dose-dependent increase in the life span of NB4-bearing SCID mice without overt toxicity[2].

PROTOCOL

Cell Assay [2]Briefly, cells (1×107/mL) are loaded with 1 μM FURA-2 at 37°C in the dark for 30 minutes, washed twice, resuspended in phosphate-buffered saline (PBS) containing 1.26 mM CaCl2 at 106 cells/mL and then used for the experiments.

Dual excitation, alternating at 340 nm and 380 nm, is provided by a spectrophotofluorometer equipped with 2

excitation monochromators, and emission is fixed at 480 nm. The temperature is set at 37°C±1°C. In some

experiments, to eliminate extracellular calcium, cells preloaded with FURA-2 are resuspended in PBS without Ca2+,

and 0.5 mM EGTA (ethylene glycol tetraacetic acid) is added to each sample prior to addition of the appropriate

stimulus.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration [2]NB4 cells (3×106) are intraperitoneally inoculated in SCID mice (8 mice/group). ST1926 is dissolved in

cremophor/ethanol 1:1 solution, and diluted 1:10 in PBS at the concentration of 50 mg/kg; the doses of 30 mg/kg and 40 mg/kg are then prepared by appropriate dilutions in the same vehicle. ATRA is dissolved in the dark in Cremophor EL and kept magnetically stirred; the solution is then diluted 1:10 in PBS at the final concentration of 40 mg/kg. Both compounds are administered intraperitoneally and orally twice per day for 3 weeks starting from the day after cell inoculation, in a volume of 10 mL/kg. During treatments body weight and lethality are registered. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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REFERENCES

[1]. Cincinelli R, et al. A novel atypical retinoid endowed with proapoptotic and antitumor activity. J Med Chem. 2003 Mar 13;46(6):909-12.

[2]. Garattini E, et al. ST1926, a novel and orally active retinoid-related molecule inducing apoptosis in myeloid leukemia cells: modulation of intracellular calcium homeostasis. Blood. 2004 Jan 1;103(1):194-207.

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Caution: Product has not been fully validated for medical applications. For research use only.

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? Cell Physiol Biochem. 2017 Jan 30;41(2):519-529.