G-15

Cas No.:	1161002-05-6
Chemical Name:	(3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline
Synonyms:	(3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline;(3aS,4R,9bR)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline;(3aR,4R,9bS)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline;G-15;(3aS,4R,9bR)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline (G-15);G15
SMILES:	C1=CC=C2C(=C1)[C@@H]3C=CC[C@@H]3[C@H](C4=CC5=C(C=C4Br)OCO5)N2
Formula:	C19H16NO2Br
M.Wt:	370.23984
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER) antagonist with a Ki of 20 nM[1][2].
In Vivo:	G15 (1.46 mg/kg; i.h.; twice a week for 14 weeks) decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice[1]. Animal Model: Four-week-old female Kunming mice (Urethane-induced adenocarcinoma)[1] Dosage: 1.46 mg/kg (combination with E2, 0.09 mg/kg and fulvestrant (Ful), 2.4 mg/kg) Administration: Subcutaneous injection; twice a week for 14 weeks Result: The number of tumor nodules decreased in the E2+Ful+G15 group.
In Vitro:	G15 (0.1-10 μM; 2 days) inhibits GPER-mediated proliferation stimulated by 17β-estradiol (E2) in A549 and H1793 cell lines[1]. G15 (1 μM; 48 hours) inhibits the response of GPER stimulated by E2 and G1 in A549 and H1793 cell lines[1]. Cell Proliferation Assay[1] Cell Line: A549, H1793 cell lines Concentration: 0.1, 1, 10 μM (combination with 10 nM E2) Incubation Time: 2 days Result: Inhibited GPER-mediated proliferation stimulated by E2. Western Blot Analysis[1] Cell Line: A549, H1793 cell lines Concentration: 1 μM (combination with 10 nM E2 and 10 nM G1) Incubation Time: 48 hours Result: Inhibited the response of GPER stimulated by E2 and G1.
References:	[1]. Liu C, et al. G-Protein-Coupled Estrogen Receptor Antagonist G15 Decreases Estrogen-Induced Development of Non-Small Cell Lung Cancer. Oncol Res. 2019 Feb 21;27(3):283-292 [2]. Girgert R, et al. Estrogen Signaling in ERα-Negative Breast Cancer: ERβ and GPER. Front Endocrinol (Lausanne). 2019 Jan 9;9:781.