XY018 是一种有效的ROR-γ选择性拮抗剂。XY018 作用于 293T 细胞，抑制 ROR-γ 活性，EC50为 190 nM。XY018 与 ROR-γ 疏水配体结合域 (LBD) 结合 。
| 生物活性 | XY018 is a potentROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD)[1]. |
| IC50& Target[1][2] | ROR-γ 0.19 μM (IC50, in 293 T cells) | ROR-α 7.57 μM (IC50, in 293 T cells) |
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体外研究
(In Vitro) | XY018 (0.07-10 μM; 4 days) inhibit CRPC tumors C4-2B cells growth and survival[1].
XY018 inhibits Gal4-RORγ-LBD and Gal4-RORα-LBD with IC50s of 0.19±0.02 and 7.57 μM in 293 T cells, respectively[2].
XY018 shows anti-proliferation effects against the prostate cancer cell lines LNCaP, 22Rv1, C4-2B, DU145, and PC-3 with IC50s of 5.14±0.36, 9.00±0.33, 9.20, 28.43±0.89, and 11.14±1.78 μM, respectively[2].
Cell Viability Assay[1] | Cell Line: | CRPC tumors C4-2B | | Concentration: | 0.07, 0.15, 0.31, 0.62, 1.25, 2.5, 5, and 10 μM | | Incubation Time: | 4 days | | Result: | Inhibited growth and survival. |
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体内研究
(In Vivo) | XY018 (5 mg/kg; intraperitoneally i.p.; five times per week for 23 days) inhibit CRPC tumor growth in mice[1].
XY018 (10 mg/kg orally or 2 mg/kg intravenously) exhibits reasonable pharmacokinetics profiles in SD rats[2].
| Animal Model: | Four-week-old male SCID C.B17 mice (for C4-2B and VCaP) or BALB/c nu/nu athymic mice (for 22Rv1 and PC-3)[1] | | Dosage: | 5 mg/kg | | Administration: | Treated intraperitoneally (i.p.); five times per week for 23 days | | Result: | Tumor growth inhibition. |
| Animal Model: | Sprague Dawley rats[2] | | Dosage: | 10 mg/kg (po; 1 mg/mL); 2 mg/kg (iv;0.4 mg/mL) (Pharmacokinetic Analysis) | | Administration: | Orally administrated (10 mg/kg) and intravenously administrated (2 mg/kg); single dose | | Result: | High plasma exposure AUC(0–∞)value of 6444 (μg/L·h), half-life (T1/2=7.67±2.36 h) and maximum plasma concentration (Cmax) value of 839 (μg/L) after a 2 mg/kg iv administration.
Demonstrated a relatively low oral bioavailability of 19% after an oral administration. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(193.66 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9366 mL | 9.6830 mL | 19.3660 mL | | 5 mM | 0.3873 mL | 1.9366 mL | 3.8732 mL | | 10 mM | 0.1937 mL | 0.9683 mL | 1.9366 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.84 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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