WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206202
CAS#: 1349723-93-8 (HCl)
Description: Elacestrant, also known as RAD1901, is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. Upon oral administration 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).
Hodoodo Cat#: H206202
Name: Elacestrant HCl
CAS#: 1349723-93-8 (HCl)
Chemical Formula: C30H40Cl2N2O2
Exact Mass: 530.25
Molecular Weight: 531.560
Elemental Analysis: C, 67.79; H, 7.59; Cl, 13.34; N, 5.27; O, 6.02
Related CAS #: 1349723-93-8 (HCl) 722533-56-4 (free base)
Synonym: RAD1901; RAD-1901; RAD 1901; RAD1901 HCl salt; Elacestrant dihydrochloride; Elacestrant HCl;
IUPAC/Chemical Name: (R)-6-(2-(ethyl(4-(2-(ethylamino)ethyl)benzyl)amino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol dihydrochloride
InChi Key: XGFHYCAZOCBCRQ-FBHGDYMESA-N
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,4-5,10-11,16-18,21H2,1-3H3;2*1H/t26-;;/m1../s1
SMILES Code: OC1=CC=C2C[C@H](C3=CC=C(OC)C=C3N(CC4=CC=C(CCNCC)C=C4)CC)CCC2=C1.[H]Cl.[H]Cl
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: Soluble in DMSO and water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
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:
| Biological target: | Elacestrant is a SERD with IC50s of 48 and 870 nM for ERα and ERβ, respectively. |
| In vitro activity: | This study investigated elacestrant's efficacy in a post-CDK4/6i setting, maintaining active ER signaling in CDK4/6i-resistant cell lines. Elacestrant inhibited cell growth in both CDK4/6i-sensitive and CDK4/6i-resistant cells, with consistent effects across various sensitivities and prior exposures to CDK4/6i. Elacestrant also degraded ER and downregulated GREB1 expression in all tested cell lines, showcasing its anti-tumor activity in clinically relevant CDK4/6i-resistant models in vitro. Reference: Breast Cancer Res. 2019 Dec 18;21(1):146. https://pubmed.ncbi.nlm.nih.gov/31852484/ |
| In vivo activity: | Elacestrant may be an option for patients with HR+/HER2- breast cancer whose disease progressed on fulvestrant in the metastatic setting. Elacestrant retains efficacy in breast cancer cells that have acquired resistance to currently available ER targeting therapies. Analysis of the subset of breast cancer patients enrolled in the EMERALD study who had previously received a fulvestrant-containing regimen indicated better progression-free survival with elacestrant than with standard-of-care endocrine therapy. Reference: Breast Cancer Res Treat. 2023 Aug;201(1):43-56. https://pubmed.ncbi.nlm.nih.gov/37318638/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100.0 | 188.13 | |
| H2O | 50.0 | 94.06 |
The following data is based on the product molecular weight 531.56 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 |
| Formulation protocol: | 1. 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. 2. 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. 3. Dubash TD, Bardia A, Chirn B, Reeves BA, LiCausi JA, Burr R, Wittner BS, Rai S, Patel H, Bihani T, Arlt H, Bidard FC, Kaklamani VG, Aftimos P, Cortés J, Scartoni S, Fiascarelli A, Binaschi M, Habboubi N, Iafrate AJ, Toner M, Haber DA, Maheswaran S. Modeling the novel SERD elacestrant in cultured fulvestrant-refractory HR-positive breast circulating tumor cells. Breast Cancer Res Treat. 2023 Aug;201(1):43-56. doi: 10.1007/s10549-023-06998-w. Epub 2023 Jun 15. PMID: 37318638; PMCID: PMC10300156. 4. Hageman E, Lussier ME. Elacestrant for ER-Positive HER2-Negative Advanced Breast Cancer. Ann Pharmacother. 2023 Oct 27:10600280231206131. doi: 10.1177/10600280231206131. Epub ahead of print. PMID: 37888769. |
| In vitro protocol: | 1. 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. 2. 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. |
| In vivo protocol: | 1. Dubash TD, Bardia A, Chirn B, Reeves BA, LiCausi JA, Burr R, Wittner BS, Rai S, Patel H, Bihani T, Arlt H, Bidard FC, Kaklamani VG, Aftimos P, Cortés J, Scartoni S, Fiascarelli A, Binaschi M, Habboubi N, Iafrate AJ, Toner M, Haber DA, Maheswaran S. Modeling the novel SERD elacestrant in cultured fulvestrant-refractory HR-positive breast circulating tumor cells. Breast Cancer Res Treat. 2023 Aug;201(1):43-56. doi: 10.1007/s10549-023-06998-w. Epub 2023 Jun 15. PMID: 37318638; PMCID: PMC10300156. 2. Hageman E, Lussier ME. Elacestrant for ER-Positive HER2-Negative Advanced Breast Cancer. Ann Pharmacother. 2023 Oct 27:10600280231206131. doi: 10.1177/10600280231206131. Epub ahead of print. PMID: 37888769. |
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.
