XY018|cas:1873358-87-2|西域试剂

XY018,99.90%

产品编号：Bellancom-120210| CAS NO：1873358-87-2| 分子式：C₂₃H₁₅F₇N₂O₄| 分子量：516.37

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-120210	￥1100.00	杭州北京（现货）
Bellancom-120210	￥1800.00	杭州北京（现货）
Bellancom-120210	￥6000.00	杭州北京（现货）
Bellancom-120210	￥9500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

XY018

产品介绍

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 potent ROR-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).

体外研究

XY018 (0.07-10 μM; 4 days) inhibit CRPC tumors C4-2B cells growth and survival.
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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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.

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 .
XY018 (10 mg/kg orally or 2 mg/kg intravenously) exhibits reasonable pharmacokinetics profiles in SD rats.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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)
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
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 (T_1/2=7.67±2.36 h) and maximum plasma concentration (C_max) value of 839 (μg/L) after a 2 mg/kg iv administration. Demonstrated a relatively low oral bioavailability of 19% after an oral administration.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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)
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
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 (T_1/2=7.67±2.36 h) and maximum plasma concentration (C_max) value of 839 (μg/L) after a 2 mg/kg iv administration. Demonstrated a relatively low oral bioavailability of 19% after an oral administration.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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)
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
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 (T_1/2=7.67±2.36 h) and maximum plasma concentration (C_max) value of 839 (μg/L) after a 2 mg/kg iv administration. Demonstrated a relatively low oral bioavailability of 19% after an oral administration.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (193.66 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。