RO4929097 | RG-4733 | γ-secretase Inhibitor | AmBeed-信号通路专用抑制剂

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RO4929097 {[allProObj[0].p_purity_real_show]}

货号：A306723 同义名： RG-4733

RO4929097（RG-4733）是一种γ分泌酶抑制剂，IC50为4 nM，抑制Aβ40和Notch的细胞加工，EC50分别为14 nM和5 nM。

RO4929097 化学结构
CAS号：847925-91-1

RO4929097 3D分子结构
CAS号：847925-91-1

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RO4929097 纯度/质量文件产品仅供科研

货号：A306723 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

RO4929097 生物活性

描述

RO4929097 is a potent and selective γ-secretase inhibitor with IC50 value of 4nM for γ-secretase enzyme assay, as well as EC50 values of 14nM and 5nM for Aβ40 and Notch processing in engineered cell lines, respectively. As γ-secretase is the key component of the enzymatic complex cleaving and activating NOTCH, RO4929097 can also inhibit NOTCH signaling indirectly. Treatment with RO4929097 dose-dependently suppressed the production of intracellular Notch at concentration ranging in 0.1-5μM for 5 days, reduced the expression of the downstream Notch target Hes1 at concentration ranging in 0.1-1μM for 24h, and producd a less transformed morphology in A549 cells. Orally administration of RO4929097 at dose of 3, 10, 30 and 60mg/kg, qd, for 14 days achieved tumor growth inhibition by 66%, 77%, 79% and 88% in the A549 xenograft model. Treatment with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule for a 21-day cycle achieved tumor growth inhibition by 91%. Inhibition of tumor growth remained prolonged and sustained up to 34 days post-treatment with reduced expression of several key angiogenic genes tested.

RO4929097 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
MGG23	30 μM	Cell Viability Assay	4 d	decreases cell viability	24495907
MGG4	30 μM	Cell Viability Assay	4 d	decreases cell viability	24495907
MGG6	30 μM	Cell Viability Assay	4 d	decreases cell viability	24495907
MGG8	30 μM	Cell Viability Assay	4 d	decreases cell viability	24495907

RO4929097 动物研究

Dose

Mice: 10 mg/kg^[2] (p.o.) Nude Mice: 3 mg/kg - 60 mg/kg^[1] (p.o.)

Administration

p.o.

Pharmacokinetics

Animal	Nude mice^[1]
Dose	10 mg/kg
Administration	p.o.
AUC_{24 h}	1100 ng·h/ml

RO4929097 参考文献

[1]Luistro L, He W, et al. Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties. Cancer Res. 2009 Oct 1;69(19):7672-80.

[2]Huynh C, Poliseno L, et al. The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma. PLoS One. 2011;6(9):e25264.

RO4929097 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.07mL

21.30mL

4.26mL

2.13mL

RO4929097 技术信息

CAS号	847925-91-1
分子式	C₂₂H₂₀F₅N₃O₃
分子量	469.404

别名	RG-4733
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(106.52 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 5 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

摩尔计算器

计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

体积

分子量

质量

*在制备母液时，请始终参考产品标签或 MSDS / COA（在产品页面可下载）上所显示的对应批次产品的分子量。

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

MGG23	30 μM	Cell Viability Assay	4 d	decreases cell viability	24495907
MGG4	30 μM	Cell Viability Assay	4 d	decreases cell viability	24495907
MGG6	30 μM	Cell Viability Assay	4 d	decreases cell viability	24495907
MGG8	30 μM	Cell Viability Assay	4 d	decreases cell viability	24495907
SUM149	0-10 μM	Cell Viability Assay	72 h	inhibits cell growth dose dependently	22547109
Sum190	0-10 μM	Cell Viability Assay	72 h	inhibits cell growth dose dependently	22547109
U87	30 μM	Cell Viability Assay	4 d	decreases cell viability	24495907
U87 R1	30 μM	Cell Viability Assay	4 d	decreases cell viability	24495907
WM115	10 uM	Function Assay	24 h	decreases the levels of NOTCH downstream target HES1	21980408
WM115	10 uM	Growth Inhibition Assay	0-18 d	inhibits cell growth time dependently	21980408
WM3248	10 uM	Function Assay	24 h	decreases the levels of NOTCH downstream target HES1	21980408
WM3248	10 uM	Growth Inhibition Assay	0-18 d	inhibits cell growth time dependently	21980408
WM35	10 uM	Function Assay	24 h	decreases the levels of NOTCH downstream target HES1	21980408
WM35	10 uM	Growth Inhibition Assay	0-18 d	inhibits cell growth time dependently	21980408
WM98.1	10 uM	Function Assay	24 h	decreases the levels of NOTCH downstream target HES1	21980408
WM98.1	10 uM	Growth Inhibition Assay	0-18 d	inhibits cell growth time dependently	21980408
WM983A	10 uM	Function Assay	24 h	decreases the levels of NOTCH downstream target HES1	21980408
WM983A	10 uM	Growth Inhibition Assay	0-18 d	inhibits cell growth time dependently	21980408

RO4929097 {[allProObj[0].p_purity_real_show]}

RO4929097 纯度/质量文件产品仅供科研

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RO4929097 生物活性

RO4929097 细胞研究

RO4929097 动物研究

RO4929097 参考文献

RO4929097 实验方案

RO4929097 技术信息

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RO4929097 {[allProObj[0].p_purity_real_show]}

RO4929097 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

RO4929097 质控信息

RO4929097 生物活性

RO4929097 细胞研究

RO4929097 动物研究

RO4929097 参考文献

RO4929097 实验方案

RO4929097 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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C

F

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RO4929097 纯度/质量文件产品仅供科研