JQAD1|cas:2417097-18-6|西域试剂

JQAD1,98.70%

产品编号：Bellancom-145765| CAS NO：2417097-18-6| 分子式：C₄₈H₅₂F₄N₆O₉| 分子量：932.95

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货号	价格	库存与货期
Bellancom-145765	￥4000.00	杭州北京（现货）
Bellancom-145765	￥7000.00	杭州北京（现货）
Bellancom-145765	￥14800.00	杭州北京（现货）

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JQAD1

产品介绍

JQAD1 是 CRBN 依赖的 PROTAC，选择性靶向 EP300 进行降解。JQAD1 抑制 EP300 表达和 H3K27ac 修饰。JQAD1 诱导细胞凋亡 (apoptosis)。JQAD1 可用于癌症研究。

生物活性

JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.

体外研究

JQAD1在对照组 Kelly NB 细胞而不是 CRBN 敲除细胞中抑制 EP300 的表达，抑制 H3K27ac 修饰，并诱导凋亡。
JQAD1 (0.5 or 1 μM; 6-96 h) 处理导致早期时间依赖性诱导亚 G1 峰，表明 Kelly 和 NGP细胞凋亡死亡。
JQAD1 (1 μM; 12-36 h) 诱导 Kelly NB 细胞凋亡。
JQAD1 (0.5 μM; 24 h) 处理的细胞表现出促凋亡的 BH3 效应物 BIM、BID 和 PUMA 以及促凋亡介质 BAX 及其抑制剂 BCL2 和 MCL1 的上调。
JQAD1 (0.5 and 1 μM; 24 h) 破坏 MYCN 表达。
JQAD1 (0.5 μM; 24 h) 导致染色质上 H3K27ac 缺失。
JQAD1 (1.2 nM-20 μM; 5 days) 具有广泛的 CRBN 依赖的跨癌细胞系抗肿瘤活性。
JQAD1 以时间依赖的方式诱导 EP300 降解，最早在 16 小时。

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

Western Blot Analysis

Cell Line:	MYCN-amplified NB cells
Concentration:	0.1, 0.5, 1, 3, 5, and 10 µM
Incubation Time:	24 h
Result:	Demonstrated a dose-dependent decrease in EP300 expression along with a parallel loss of the H3K27ac modification. Induced selective loss of EP300 expression coincident with cleavage of PARP1, signaling the onset of apoptosis.

Western Blot Analysis

Cell Line:	Kelly NB cells
Concentration:	1 µM
Incubation Time:	12, 24, and 36 hours
Result:	Increased the expression of cleaved caspase-3 and cleaved PARP1 in a dose-dependent manner.

体内研究
(In Vivo)

JQAD1 (40 mg/kg; i.p.; 每日一次, 持续 21 天) 抑制 Kelly NB 细胞异种移植的 NSG 小鼠的肿瘤生长。

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

Animal Model:	NSG mice with Kelly NB cell xenografts
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; daily, for 21 days
Result:	Suppressed tumor growth and prolonged survival.

Animal Model:	CD1 mice
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection (Pharmacokinetic Analysis)
Result:	Had a half-life of 13.3 (±3.37 SD) hours in murine serum, with a C_max of 7 μmol/L.

体内研究

JQAD1 (40 mg/kg; i.p.; 每日一次, 持续 21 天) 抑制 Kelly NB 细胞异种移植的 NSG 小鼠的肿瘤生长。

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

Animal Model:	NSG mice with Kelly NB cell xenografts
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; daily, for 21 days
Result:	Suppressed tumor growth and prolonged survival.

Animal Model:	CD1 mice
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection (Pharmacokinetic Analysis)
Result:	Had a half-life of 13.3 (±3.37 SD) hours in murine serum, with a C_max of 7 μmol/L.

体内研究

JQAD1 (40 mg/kg; i.p.; 每日一次, 持续 21 天) 抑制 Kelly NB 细胞异种移植的 NSG 小鼠的肿瘤生长。

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

Animal Model:	NSG mice with Kelly NB cell xenografts
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; daily, for 21 days
Result:	Suppressed tumor growth and prolonged survival.

Animal Model:	CD1 mice
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection (Pharmacokinetic Analysis)
Result:	Had a half-life of 13.3 (±3.37 SD) hours in murine serum, with a C_max of 7 μmol/L.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (107.19 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.0719 mL	5.3593 mL	10.7187 mL
5 mM	0.2144 mL	1.0719 mL	2.1437 mL
10 mM	0.1072 mL	0.5359 mL	1.0719 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式