计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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.
In Vitro
JQAD1 suppresses EP300 expression, suppresses the H3K27ac modification, and induces apoptosis, marked by PARP1 cleavage in control Kelly NB cells, but not in CRBN-knockout cells. JQAD1 (0.5 or 1 μM; 6-96 h) treatment resulted in early time-dependent induction of a sub-G1 peak, suggestive of apoptotic cell death in Kelly and NGP cells. JQAD1 (1 μM; 12-36 h) induces Kelly NB cell apoptosis. JQAD1 (0.5 μM; 24 h)-treated cells exhibits upregulation of the proapoptotic BH3-only effectors BIM, BID, and PUMA together with the proapoptotic mediator BAX and its inhibitors BCL2 and MCL1. JQAD1 (0.5 and 1 μM; 24 h) disrupts MYCN expression. JQAD1 (0.5 μM; 24 h) causes loss of H3K27ac at chromatin. JQAD1 (1.2 nM-20 μM; 5 days) has broad CRBN-dependent antineoplastic activity across cancer cell lines. JQAD1 induces EP300 degradation in a time-dependent manner as early as 16 hours. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 AnalysisCell 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.
In Vivo
JQAD1 (40 mg/kg; i.p.; daily, for 21 d) inhibits tumor growth in NSG mice with Kelly NB cell xenografts . MCE 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.
Form:Solid
规格
规格或纯度
≥98%
英文名称
JQAD1
生化机理
JQAD1 是一种依赖于 CRBN 的 PROTAC，可选择性地靶向降解 EP300。JQAD1 可抑制 EP300 的表达和 H3K27ac 的修饰。JQAD1 可诱导细胞凋亡。JQAD1 可用于癌症研究。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
932.95
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 100 mg/mL (107.19 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥98%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?20 °C条件下保存。需冷冻保存以维持规定的有效期。
本产品如何运输？
本产品采用保温箱配冰袋运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2417097-18-6，分子式为 C48H52F4N6O9，分子量为 932.95 g/mol。
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