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Purity: ≥98%
Elacestrant 2 HCl (RAD1901 dihydrochloride) is a potent and orally bioavailable SERD (selective estrogen receptor degrader) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. It has potential antineoplastic and estrogen-like activities. Upon oraladministration of higher doses of RAD1901, this agent acts as a SERD, which binds to the estrogen receptor (ER) and induces a conformational change that results in the degradation of the receptor. This may inhibit the growth and survival of ER-expressing cancer cells. At lower doses of this agent, RAD1901 acts as a SERM and has estrogen-like effects in certain tissues, which can both reduce hot flashes and protect against bone loss. In addition, RAD1901 is able to cross the blood-brain barrier (BBB). In Jan 2023, FDA approved Elacestrant for treating breast cancer.
| ln Vitro |
The concentration-dependent inhibition of ERα expression in MCF-7 cells (EC50 = 0.6 nM) is observed with elacestrant dihydrochloride (RAD1901; 0.5 nM-10 µM; 48 h) [1]. 48 hours of elacestrant dihydrochloride (0–1 µM). is shown to have concentration-dependent antiproliferative action (EC50 = 4 pM) on ER-acute MCF-7 cells triggered by estradiol (E2) [1]. Progesterone receptors (PGR, PR, and an ER) in MCF7 and T47D cell lines are reduced by elacestrant diHCl (0–1 µM; 24 or 48 hours).
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| ln Vivo |
Elecestrant dihydrochloride multiplexes anti-E2-mediated promotion of proliferation in a dose-dependent manner (0.3-120 mg/kg; po; once daily for 40 days) [1]. Even if elacestrant diHCl is totally stopped, tumor growth inhibition may persist [2].
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: ER-positive MCF-7 cells (estradiol (E2) stimulation) Tested Concentrations: 0-1 μM Incubation Duration: 48 hrs (hours) Experimental Results: Anti-proliferative activity was shown. cell. 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 |
C30H40CL2N2O2
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|---|---|
| Molecular Weight |
531.5568
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| CAS # |
1349723-93-8
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| Related CAS # |
Elacestrant;722533-56-4;Elacestrant S enantiomer dihydrochloride;2309762-30-7;Elacestrant (S enantiomer);2309762-29-4
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
OC1=CC=C2C[C@H](C3=CC=C(OC)C=C3N(CC4=CC=C(CCNCC)C=C4)CC)CCC2=C1.[H]Cl.[H]Cl
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| InChi Key |
XGFHYCAZOCBCRQ-FBHGDYMESA-N
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| InChi Code |
InChI=1S/C30H38N2O2.2ClH/c1-4-31-17-16-22-6-8-23(9-7-22)21-32(5-2)30-20-28(34-3)14-15-29(30)26-11-10-25-19-27(33)13-12-24(25)18-26/h6-9,12-15,19-20,26,31,33H,4-5,10-11,16-18,21H2,1-3H32*1H/t26-/m1../s1
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| Chemical Name |
(R)-6-(2-(ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol
dihydrochloride
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| Synonyms |
RAD1901 dihydrochloride RAD-1901 RAD 1901 RAD1901 HCl salt Elacestrant
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| HS Tariff Code |
2934.99.9001
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| 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, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~188.13 mM)
H2O : ~50 mg/mL (~94.06 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.87 mg/mL (5.40 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.87 mg/mL (5.40 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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: ≥ 2.5 mg/mL (4.70 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (4.70 mM) 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 25.0 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. Solubility in Formulation 5: ≥ 2.5 mg/mL (4.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: ≥ 0.57 mg/mL (1.07 mM) (saturation unknown) in 1% DMSO + 99% Saline (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 | 1.8813 mL | 9.4063 mL | 18.8126 mL | |
| 5 mM | 0.3763 mL | 1.8813 mL | 3.7625 mL | |
| 10 mM | 0.1881 mL | 0.9406 mL | 1.8813 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.
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