EPZ020411 hydrochloride|cas:2070015-25-5|西域试剂

EPZ020411 hydrochloride,98.15%

产品编号：Bellancom-12970A| CAS NO：2070015-25-5| 分子式：C₂₅H₃₉ClN₄O₃| 分子量：479.06

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-12970A	￥2000.00	杭州北京（现货）
Bellancom-12970A	￥3500.00	杭州北京（现货）
Bellancom-12970A	￥6500.00	杭州北京（现货）
Bellancom-12970A	￥11500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

EPZ020411 hydrochloride

产品介绍

EPZ020411 hydrochloride 是一种选择性的 PRMT6 抑制剂，其 IC₅₀ 值为 10 nM，比作用于 PRMT1 和 PRMT8 选择性高 10 倍多。EPZ020411 hydrochloride 可用于癌症的研究。

生物活性

EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC₅₀ of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer.

体外研究

EPZ020411 hydrochloride (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells.
EPZ020411 hydrochloride (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival.

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

Western Blot Analysis

Cell Line:	A375 cells
Concentration:	0-20 μM
Incubation Time:	24 hours
Result:	Dose-dependently decreased H3R2 methylation in A375 cells with an IC₅₀ of 0.634 μM.

Cell Viability Assay

Cell Line:	Cultured cochleae cells
Concentration:	20 and 40 μM
Incubation Time:	6 hours
Result:	Suppressed the apoptotic cascade induced by aminoglycosides and also inhibited cisplatin-induced apoptosis in the hair cells of the cochlear explants after pretreatment deposed. Reduced hair cell loss caused by cisplatin treatment.

体内研究
(In Vivo)

EPZ020411 hydrochloride (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model.
1.19 Pharmacokinetic Parameters of EPZ020411 hydrochloride in rats.

	Rats IV 1 mg/kg	Rats SC 5 mg/kg
CL (mL/min/kg)	19.7±1.0
V_ss (L/kg)	11.1±1.6
t_1/2 (h)	8.54±1.43	9.19±1.60
t_max (h)		0.444
C_max (ng/mL)		844±306
AUC_0-τ (h·ng/mL)	745±34	2456±135
AUC_0-inf (h·ng/mL)	846±45	2775±181
F (%)		65.6±4.3

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

Animal Model:	C57BL/6J wild-type mice at P28 with acute ototoxicity model
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; 10 mg/kg once
Result:	Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice.

体内研究

	Rats IV 1 mg/kg	Rats SC 5 mg/kg
CL (mL/min/kg)	19.7±1.0
V_ss (L/kg)	11.1±1.6
t_1/2 (h)	8.54±1.43	9.19±1.60
t_max (h)		0.444
C_max (ng/mL)		844±306
AUC_0-τ (h·ng/mL)	745±34	2456±135
AUC_0-inf (h·ng/mL)	846±45	2775±181
F (%)		65.6±4.3

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

Animal Model:	C57BL/6J wild-type mice at P28 with acute ototoxicity model
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; 10 mg/kg once
Result:	Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice.

体内研究

	Rats IV 1 mg/kg	Rats SC 5 mg/kg
CL (mL/min/kg)	19.7±1.0
V_ss (L/kg)	11.1±1.6
t_1/2 (h)	8.54±1.43	9.19±1.60
t_max (h)		0.444
C_max (ng/mL)		844±306
AUC_0-τ (h·ng/mL)	745±34	2456±135
AUC_0-inf (h·ng/mL)	846±45	2775±181
F (%)		65.6±4.3

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

Animal Model:	C57BL/6J wild-type mice at P28 with acute ototoxicity model
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; 10 mg/kg once
Result:	Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice.

性状

Solid

溶解性数据

In Vitro:

0.1 M HCL : 50 mg/mL (104.37 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)

DMSO : 50 mg/mL (104.37 mM; Need ultrasonic)

H₂O : 20 mg/mL (41.75 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0874 mL	10.4371 mL	20.8742 mL
5 mM	0.4175 mL	2.0874 mL	4.1748 mL
10 mM	0.2087 mL	1.0437 mL	2.0874 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 (stored under nitrogen)。-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： PBS
Solubility: 25 mg/mL (52.19 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.22 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 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.22 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.22 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。