Elacestrant (RAD1901) (Synonyms: RAD1901) |
| カタログ番号GC33025 |
Elacestrant (RAD1901) (RAD1901) は、ERα の IC50 が 48 および 870 nM の経口投与可能な選択的エストロゲン受容体分解剤 (SERD) です。および ERβ、それぞれ。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 722533-56-4
Sample solution is provided at 25 µL, 10mM.
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Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ER) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
RAD1901 selectively binds to and degrades the ER and is a potent antagonist of ER-positive breast cancer cell proliferation. RAD1901 treatment exhibits dose-dependent inhibition of ERα expression, with an EC50 of 0.6 nM. Treatment of ER-positive MCF-7 cells with E2 results in a potent and dose-dependent increase in proliferation, with an EC50 of 4 pM. Treatment of cells with RAD1901 in the presence of 10 pM E2 resultsin a dose-dependent decrease in proliferation, with an IC50 value of 4.2 nM[1].
RAD1901 produces a robust and profound inhibition of tumor growth in MCF-7 xenograft models. RAD1901-treated animals survived longer than those treated with either control or fulvestrant. RAD1901 preserves ovariectomy-induced bone loss and preventes the uterotropic effects of E2[1].
[1]. Garner F, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56.
Kinase experiment: | RAD1901 is serially diluted in ES2 screening buffer to concentrations ranging from 10 to 10-6 μM. Aliquots (25 μL) of each dilution are added to a black 384-well microtiter plate, in triplicate. The ER–Fluormone complex is prepared as directed, with 2 nM Fluormone ES2 and 30 nM ER. A 25 μL aliquot of this preparation is added to each reaction well. The plates are sealed and incubated in the dark at room temperature for 4 h. Polarization values for each well are measured and plotted against the concentration of the test compound. The IC50 is determined from at least three independent experiments, with E2 serving as a positive control[1]. |
Cell experiment: | For proliferation assays, MCF-7 cells are treated with 2% charcoal-stripped FBS–MEM containing 10 pM E2 with either RAD1901 or additional E2 at concentrations ranging from 10-9 to 1 M. The medium is removed after 48 h of incubation and the cells are lysed by adding 100 μl of CellTiter Glo. The plates are gently mixed on a plate shaker for 10 min before the luminescent signal is measured on a luminometer. The EC50 and IC50of the test compound are then defined[1]. |
Animal experiment: | Mice: RAD1901 is stored as a dry powder, formulated for use as a homogenous suspension in 0.5% (w/v) methylcellulose in deionized water. Fourteen days after tumor cell implantation, the mice are randomized into nine groups of 15 animals each and treated with vehicle, tamoxifen (1 mg/animal every other day), fulvestrant (0.5 mg/animal daily), or RAD1901 (0.3, 1, 3, 10, 30, 60, 90, and 120 mg/kg daily). Tumor volumes are evaluated twice per week[1]. |
References: [1]. Garner F, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56. | |
| Cas No. | 722533-56-4 | SDF | |
| 同義語 | RAD1901 | ||
| Canonical SMILES | OC1=CC=C2C[C@H](C3=CC=C(OC)C=C3N(CC)CC4=CC=C(CCNCC)C=C4)CCC2=C1 | ||
| Formula | C30H38N2O2 | M.Wt | 458.63 |
| 溶解度 | Soluble in DMSO | 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. |
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| 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 | 2.1804 mL | 10.902 mL | 21.8041 mL |
| 5 mM | 436.1 μL | 2.1804 mL | 4.3608 mL |
| 10 mM | 218 μL | 1.0902 mL | 2.1804 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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.
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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