| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
Elacestrant (RAD-1901; RAD1901; Orserdu) is a novel and potent estrogen receptor (ER) degrader with anticancer activity. It inhibits ERα and ERβ with IC50s of 48 and 870 nM, respectively.As an orally bioavailable selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), it has estrogen-like activities and acts by binding to ER and inducing a conformational change that results in the degradation of the receptor. In Jan 2023, FDA approved Elacestrant for treating breast cancer.
| ln Vitro |
Elacestrant (RAD1901; 0.5 nM-10 µM; 48 h) suppresses ERα expression in MCF-7 cells in a concentration-dependent manner (EC50 = 0.6 nM)[1]. Elacestrant (0-1 µM; 48 h) showed anti-proliferative action (EC50 = 4 pM) against estradiol (E2)-stimulated ER-positive MCF-7 cells in a concentration-dependent manner [1]. Elacestrant (0-1 µM; 24 or 48 h) in MCF7, T47D Elacestrant (0.01, 0.1, 1.0 µM) lowers the expression of progesterone receptors (PGR, PR; an ER target gene) in MCF7 and T47D cell lines [2].
|
|---|---|
| ln Vivo |
In a dose-dependent manner, elacestrant (0.3-120 mg/kg; po; once daily for 40 days) inhibits E2-mediated intellectual stimulation [1]. Elacetrant (30, 60 mg/kg; po; 10 days per day). Even after the medicine is stopped, elacestrant can still stop tumor growth [2].
|
| Cell Assay |
Cell proliferation assay [1]
Cell Types: ER-positive MCF-7 cells (estradiol (E2)-stimulated) [1] Tested Concentrations: 0-1 μM Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated anti-proliferative activity on cells. . Western Blot Analysis[1] Cell Types: MCF-7 Cell Tested Concentrations: 0.5 nM-10 µM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition of ERα expression in a dose-dependent manner (EC50 of 0.6 nM). Western Blot Analysis[2] Cell Types: MCF7, T47D and HCC1428 Cell Tested Concentrations: 0-1 µM Incubation Duration: 24 or 48 hrs (hours) Experimental Results: diminished estrogen receptor protein expression. |
| Animal Protocol |
Animal/Disease Models: Mouse MCF7 cell line xenograft model [2].
Doses: 30, 60 mg/kg Route of Administration: Oral; one time/day for 4 weeks Experimental Results: Inhibition of tumor growth. |
| 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.
[2]. Bihani T, et al. Elacestrant (RAD1901), a Selective Estrogen Receptor Degrader (SERD), Has Antitumor Activity in Multiple ER+ Breast Cancer Patient-derived Xenograft Models. Clin Cancer Res. 2017 Aug 15;23(16):4793-4804. |
| Molecular Formula |
C₃₀H₃₈N₂O₂
|
|---|---|
| Molecular Weight |
458.63
|
| Exact Mass |
458.29
|
| Elemental Analysis |
C, 78.56; H, 8.35; N, 6.11; O, 6.98
|
| CAS # |
722533-56-4
|
| Related CAS # |
Elacestrant dihydrochloride;1349723-93-8;Elacestrant S enantiomer dihydrochloride;2309762-30-7;Elacestrant (S enantiomer);2309762-29-4
|
| Appearance |
Solid powder
|
| SMILES |
O(C([H])([H])[H])C1C([H])=C([H])C(=C(C=1[H])N(C([H])([H])C([H])([H])[H])C([H])([H])C1C([H])=C([H])C(C([H])([H])C([H])([H])N([H])C([H])([H])C([H])([H])[H])=C([H])C=1[H])[C@@]1([H])C([H])([H])C2C([H])=C([H])C(=C([H])C=2C([H])([H])C1([H])[H])O[H]
|
| Synonyms |
RAD1901RAD-1901RAD 1901Orserdu
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~160 mg/mL (~348.87 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4 mg/mL (8.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 4 mg/mL (8.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 4 mg/mL (8.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1804 mL | 10.9020 mL | 21.8041 mL | |
| 5 mM | 0.4361 mL | 2.1804 mL | 4.3608 mL | |
| 10 mM | 0.2180 mL | 1.0902 mL | 2.1804 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
