Elacestrant
Elacestrant Basic information
- Product Name:
- Elacestrant
- Synonyms:
-
- Elacestrant
- Elacestrant (RAD1901)
- 2-Naphthalenol, 6-[2-[ethyl[[4-[2-(ethylamino)ethyl]phenyl]methyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydro-, (6R)-
- Elacestrant ISO 9001：2015 REACH
- inhibit,RAD 1901,Estrogen Receptor/ERR,Inhibitor,Elacestrant,RAD-1901
- (6R)-6-2-ethyl(4-2-(ethylamino)ethylphenylmethyl)amino-4-methoxyphenyl-5,6,7,8-tetrahydronaphthalen-2-ol
- (R)-6-[2-[Ethyl[4-[2-(ethylamino)ethyl]benzyl]amino]-4-methoxyphenyl]-5,6,7,8-tetrahydronaphthalen-2-ol
- Venadaparib Impurity 54
- CAS:
- 722533-56-4
- MF:
- C30H38N2O2
- MW:
- 458.63
- EINECS:
- 258-984-3
- Product Categories:
-
- API
- Mol File:
- 722533-56-4.mol
Elacestrant Chemical Properties
- Boiling point:
- 609.5±55.0 °C(Predicted)
- Density
- 1.111±0.06 g/cm3(Predicted)
- pka
- 10.36±0.40(Predicted)
- form
- Solid
- color
- White to off-white
- InChI
- 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
- InChIKey
- SIFNOOUKXBRGGB-AREMUKBSSA-N
- SMILES
- C1=C2C(C[C@H](C3=CC=C(OC)C=C3N(CC)CC3=CC=C(CCNCC)C=C3)CC2)=CC=C1O
Elacestrant Usage And Synthesis
Uses
Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo[1][2].
in vivo
Elacestrant (0.3-120 mg/kg; p.o.; single daily for 40 days) antagonizes E2-mediated uterine stimulation in a dose-dependent manner in vivo[1].
Elacestrant (30, 60 mg/kg; p.o.; single daily for 4 weeks) induces complete tumor growth inhibition in mice[2].
Tumor growth inhibition is maintained for 4 weeks after Elacestrant withdrawal[2].
| Animal Model: | MCF7 cell line xenograft model of mice[2]. |
| Dosage: | 30, 60 mg/kg |
| Administration: | Oral administration; single daily for 4 weeks. |
| Result: | Inhibited growth of tumor. |
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. DOI:10.1097/CAD.0000000000000271
[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. DOI:10.1158/1078-0432.CCR-16-2561
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