Adarotene (Synonyms: ST1926) |
| Catalog No.GC13959 |
An atypical retinoid
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 496868-77-0
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
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.
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. | |
| Cas No. | 496868-77-0 | SDF | |
| Synonyms | ST1926 | ||
| Chemical Name | (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 | ||
| Formula | C25H26O3 | M.Wt | 374.47 |
| Solubility | ≥ 37.4 mg/mL in DMSO, ≥ 10.97 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *