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RO4929097 {[allProObj[0].p_purity_real_show]}

货号:A306723 同义名: RG-4733

RO4929097 is an inhibitor of γ secretase, the IC50s of Aβ40 and notch are 14 nM and 5 nM, respectively.

RO4929097 化学结构 CAS号:847925-91-1
RO4929097 化学结构
CAS号:847925-91-1
RO4929097 3D分子结构
CAS号:847925-91-1
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]}
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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 活性说明 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.
AUC24 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 469.4
SMILES Code O=C(N[C@H]1C2=CC=CC=C2C3=CC=CC=C3NC1=O)C(C)(C)C(NCC(F)(F)C(F)(F)F)=O
MDL No. MFCD18384976
别名 RG-4733
运输蓝冰
InChI Key OJPLJFIFUQPSJR-INIZCTEOSA-N
Pubchem ID 49867930
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案一
方案二
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

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