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Adarotene Sale

(Synonyms: (2E)-3-(4'-羟基-3'-金刚烷-1-基[1,1'-联苯]-4-基)-2-丙烯酸,ST 1926;ST-1926;ST1926) 目录号 : GC13959

An atypical retinoid

Adarotene Chemical Structure

Cas No.:496868-77-0

规格 价格 库存 购买数量
5mg
¥586.00
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10mg
¥1,088.00
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50mg
¥3,432.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

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.

Animal experiment:

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.

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.

产品描述

Retinoid-related molecules are derivatives of retinoic acid and promising antileukemic agents with a mechanism of action different from that of other common chemotherapeutics. Adarotene is a novel atypical retinoid endowed with proapoptotic and antitumor activity.
In vitro: The novel atypical retinoid adarotene exhibited potent antiproliferative activity on a large panel of human tumor cells. It was found that although almost complete loss of ability to activate RARs, adarotene was performing as an effective apoptosis inducer and surprisingly produced DNA damage, which likely contributed to its proapoptotic activity [1].
In vivo: Following oral administration, adarotene was well tolerated and caused tumor growth inhibition in the ovarian carcinoma (A2780/DX) and the human melanoma (MeWo) exnographt in nude mice, supporting the therapeutic interest of this novel agent [1].
Clinical trial: Adarotene is currently only in the preclinical developlent stage and no clinical data are available.
Reference:
[1] Cincinelli R, Dallavalle S, Merlini L, Penco S, Pisano C, Carminati P, Giannini G, Vesci L, Gaetano C, Illy B, Zuco V, Supino R, Zunino F. A novel atypical retinoid endowed with proapoptotic and antitumor activity. J Med Chem. 2003;46(6):909-12.

Chemical Properties

Cas No. 496868-77-0 SDF
别名 (2E)-3-(4'-羟基-3'-金刚烷-1-基[1,1'-联苯]-4-基)-2-丙烯酸,ST 1926;ST-1926;ST1926
化学名 (E)-3-[4-[3-(1-adamantyl)-4-hydroxyphenyl]phenyl]prop-2-enoic acid
Canonical SMILES C1C2CC3CC1CC(C2)(C3)C4=C(C=CC(=C4)C5=CC=C(C=C5)C=CC(=O)O)O
分子式 C25H26O3 分子量 374.47
溶解度 ≥ 37.4 mg/mL in DMSO, ≥ 10.97 mg/mL in EtOH with ultrasonic and warming 储存条件 Store at -20°C
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储备液的保存方式和期限:-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。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6704 mL 13.3522 mL 26.7044 mL
5 mM 0.5341 mL 2.6704 mL 5.3409 mL
10 mM 0.267 mL 1.3352 mL 2.6704 mL
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