Elacestrant free base | 722533-56-4 | SERD | SERM

MedKoo Cat#: 333073 | Name: Elacestrant free base

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Elacestrant, also known as RAD1901, is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM). Elacestrant exhibits potent in vitro bioactivity as a selective estrogen receptor degrader (SERD), showing effective antagonism and degradation of estrogen receptor alpha (ERα) in ER-positive breast cancer cell lines. In MCF-7 and T47D cells, Elacestrant inhibits estrogen-driven proliferation with IC₅₀ values in the range of 1–3 nM. It induces dose-dependent degradation of ERα protein, with maximal degradation observed at concentrations as low as 10–30 nM. In ESR1-mutant models (e.g., Y537S and D538G), which are resistant to fulvestrant, Elacestrant retains potent antiproliferative effects, reducing cell viability with IC₅₀ values around 5–20 nM.

Chemical Structure

Elacestrant free base

CAS#722533-56-4 (free base)

Theoretical Analysis

MedKoo Cat#: 333073

Name: Elacestrant free base

CAS#: 722533-56-4 (free base)

Chemical Formula: C30H38N2O2

Exact Mass: 458.2933

Molecular Weight: 458.65

Elemental Analysis: C, 78.56; H, 8.35; N, 6.11; O, 6.98

Price and Availability

Size	Price	Availability
5mg	USD 150.00	Ready to ship
10mg	USD 250.00	Ready to ship
25mg	USD 450.00	Ready to Ship
50mg	USD 750.00	Ready to ship
100mg	USD 1,250.00	Ready to ship
1g	USD 3,650.00	Ready to ship
2g	USD 6,250.00	Ready to Ship

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

1349723-93-8 (HCl) 722533-56-4 (free base)

Synonym

RAD1901; RAD-1901; RAD 1901; RAD1901 Elacestrant; Elacestrant free base

IUPAC/Chemical Name

(R)-6-(2-(ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol

InChi Key

SIFNOOUKXBRGGB-AREMUKBSSA-N

InChi Code

InChI=1S/C30H38N2O2/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,4-5,10-11,16-18,21H2,1-3H3/t26-/m1/s1

SMILES Code

OC1=CC=C2C[C@H](C3=CC=C(OC)C=C3N(CC)CC4=CC=C(CCNCC)C=C4)CCC2=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 458.65 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Bidard FC, Kaklamani VG, Neven P, Streich G, Montero AJ, Forget F, Mouret- Reynier MA, Sohn JH, Taylor D, Harnden KK, Khong H, Kocsis J, Dalenc F, Dillon PM, Babu S, Waters S, Deleu I, García Sáenz JA, Bria E, Cazzaniga M, Lu J, Aftimos P, Cortés J, Liu S, Tonini G, Laurent D, Habboubi N, Conlan MG, Bardia A. Elacestrant (oral selective estrogen receptor degrader) Versus Standard Endocrine Therapy for Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer: Results From the Randomized Phase III EMERALD Trial. J Clin Oncol. 2022 Oct 1;40(28):3246-3256. doi: 10.1200/JCO.22.00338. Epub 2022 May 18. Erratum in: J Clin Oncol. 2023 Aug 10;41(23):3962. PMID: 35584336; PMCID: PMC9553388. 2: Hoy SM. Elacestrant: First Approval. Drugs. 2023 Apr;83(6):555-561. doi: 10.1007/s40265-023-01861-0. PMID: 37060385. 3: Bardia A, Aftimos P, Bihani T, Anderson-Villaluz AT, Jung J, Conlan MG, Kaklamani VG. EMERALD: Phase III trial of elacestrant (RAD1901) vs endocrine therapy for previously treated ER+ advanced breast cancer. Future Oncol. 2019 Oct;15(28):3209-3218. doi: 10.2217/fon-2019-0370. Epub 2019 Aug 20. PMID: 31426673. 4: Bardia A, Kaklamani V, Wilks S, Weise A, Richards D, Harb W, Osborne C, Wesolowski R, Karuturi M, Conkling P, Bagley RG, Wang Y, Conlan MG, Kabos P. Phase I Study of Elacestrant (RAD1901), a Novel Selective Estrogen Receptor Degrader, in ER-Positive, HER2-Negative Advanced Breast Cancer. J Clin Oncol. 2021 Apr 20;39(12):1360-1370. doi: 10.1200/JCO.20.02272. Epub 2021 Jan 29. PMID: 33513026; PMCID: PMC8078341. 5: Sanchez KG, Nangia JR, Schiff R, Rimawi MF. Elacestrant and the Promise of Oral SERDs. J Clin Oncol. 2022 Oct 1;40(28):3227-3229. doi: 10.1200/JCO.22.00841. Epub 2022 Jun 23. PMID: 35737918. 6: Elacestrant Dihydrochloride. Am J Health Syst Pharm. 2023 May 24;80(11):643-645. doi: 10.1093/ajhp/zxad050. PMID: 36960661. 7: Bhatia N, Thareja S. Elacestrant: a new FDA-approved SERD for the treatment of breast cancer. Med Oncol. 2023 May 16;40(6):180. doi: 10.1007/s12032-023-02045-2. PMID: 37191763. 8: Varella L, Cristofanilli M. Evaluating Elacestrant in the Management of ER- Positive, HER2-Negative Advanced Breast Cancer: Evidence to Date. Onco Targets Ther. 2023 Mar 23;16:189-196. doi: 10.2147/OTT.S400563. PMID: 36993871; PMCID: PMC10041978. 9: Lipsyc-Sharf M, Tolaney SM. Elacestrant: who are optimal candidates for the first oral SERD? Ann Oncol. 2023 May;34(5):449-451. doi: 10.1016/j.annonc.2023.02.006. Epub 2023 Feb 20. PMID: 36813113. 10: Beumer JH, Foldi J. Pharmacology and pharmacokinetics of elacestrant. Cancer Chemother Pharmacol. 2023 Aug;92(2):157-163. doi: 10.1007/s00280-023-04550-7. Epub 2023 Jun 14. PMID: 37314500. 11: Pancholi S, Simigdala N, Ribas R, Schuster E, Leal MF, Nikitorowicz-Buniak J, Rega C, Bihani T, Patel H, Johnston SR, Dowsett M, Martin LA. Elacestrant demonstrates strong anti-estrogenic activity in PDX models of estrogen-receptor positive endocrine-resistant and fulvestrant-resistant breast cancer. NPJ Breast Cancer. 2022 Nov 29;8(1):125. doi: 10.1038/s41523-022-00483-1. PMID: 36446866; PMCID: PMC9709100. 12: Elacestrant Prolongs Progression-Free Survival in Advanced Breast Cancer. Cancer Discov. 2022 Jul 6;12(7):1609. doi: 10.1158/2159-8290.CD-RW2022-095. PMID: 35621343. 13: Olivier T, Prasad V. Elacestrant in metastatic breast cancer: Is the "standard of care" meeting standard requirements? Transl Oncol. 2022 Jan;15(1):101273. doi: 10.1016/j.tranon.2021.101273. Epub 2021 Nov 16. PMID: 34798371; PMCID: PMC8605291. 14: Elacestrant (Orserdu) for advanced or metastatic breast cancer. Med Lett Drugs Ther. 2023 Mar 6;65(1671):38-40. doi: 10.58347/tml.2023.1671d. PMID: 36877283. 15: Chen YC, Yu J, Metcalfe C, De Bruyn T, Gelzleichter T, Malhi V, Perez-Moreno PD, Wang X. Latest generation estrogen receptor degraders for the treatment of hormone receptor-positive breast cancer. Expert Opin Investig Drugs. 2022 Jun;31(6):515-529. doi: 10.1080/13543784.2021.1983542. Epub 2021 Oct 25. PMID: 34694932. 16: Shah N, Mohammad AS, Saralkar P, Sprowls SA, Vickers SD, John D, Tallman RM, Lucke-Wold BP, Jarrell KE, Pinti M, Nolan RL, Lockman PR. Investigational chemotherapy and novel pharmacokinetic mechanisms for the treatment of breast cancer brain metastases. Pharmacol Res. 2018 Jun;132:47-68. doi: 10.1016/j.phrs.2018.03.021. Epub 2018 Mar 28. PMID: 29604436; PMCID: PMC5997530. 17: Patel HK, Tao N, Lee KM, Huerta M, Arlt H, Mullarkey T, Troy S, Arteaga CL, Bihani T. Elacestrant (RAD1901) exhibits anti-tumor activity in multiple ER+ breast cancer models resistant to CDK4/6 inhibitors. Breast Cancer Res. 2019 Dec 18;21(1):146. doi: 10.1186/s13058-019-1230-0. PMID: 31852484; PMCID: PMC6921513. 18: Jacobson A. Elacestrant Improves Progression-Free Survival After Endocrine Therapy for Estrogen Receptor-Positive Metastatic Breast Cancer. Oncologist. 2022 Mar 28;27(Suppl 1):S7-S8. doi: 10.1093/oncolo/oyac015. PMID: 35348779; PMCID: PMC8963147. 19: Lüftner D. New treatment options for hormone receptor positive breast cancer in 2023. Curr Opin Obstet Gynecol. 2023 Feb 1;35(1):62-66. doi: 10.1097/GCO.0000000000000834. Epub 2022 Nov 7. PMID: 36341983. 20: Bihani T, Patel HK, Arlt H, Tao N, Jiang H, Brown JL, Purandare DM, Hattersley G, Garner F. 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. doi: 10.1158/1078-0432.CCR-16-2561. Epub 2017 May 4. PMID: 28473534.