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Kobe0065 {[allProObj[0].p_purity_real_show]}

货号：A550431

Kobe0065 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with Ki of 46 ± 13 μM.

Kobe0065 化学结构
CAS号：436133-68-5

Kobe0065 3D分子结构
CAS号：436133-68-5

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Kobe0065 纯度/质量文件产品仅供科研

货号：A550431 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

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Kobe0065 生物活性

描述

Ras oncoproteins belong to the Ras family of small GTPases and function as molecular switches by cycling between GTP-bound active and GDP-bound inactive forms in intracellular signaling pathways controlling cell growth, differentiation, and apoptosis. Interconversion between the two forms is reciprocally catalyzed by guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs). Kobe0065, a novel and effective inhibitor of Ras-Raf interaction, competitively inhibits the binding of H-Ras⋅GTP to c-Raf-1 RBD with a K_i value of 46 ± 13 μM. The IC₅₀ value of Kobe0065 for inhibiting Ras⋅GTP is around 20 μM. Kobe0065 at 20 μM efficiently inhibited the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing H-Ras^G12V. Kobe0065 at 50 μM almost completely abolished the accelerating effect of the distal site without apparently affecting the catalytic activity of the GEF domain itself. Kobe0065 efficiently inhibited colony formation of H-ras^G12V–transformed NIH 3T3 cells in soft agar in a dose-dependent manner with IC₅₀ value of around 0.5 μM. In a xenograft of SW480 cells in nude mice, daily oral administration of kobe0065 at the dose of 80 mg/kg caused ∼40–50% inhibition of the tumor growth. By doubling the dose to 160 mg/kg, the activity of Kobe0065 became more evident^[3].

Kobe0065 参考文献

[1]Shima F, Yoshikawa Y, et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction. Proc Natl Acad Sci U S A. 2013 May 14;110(20):8182-7.

[2]Shima F, Yoshikawa Y, et al. Discovery of small-molecule Ras inhibitors that display antitumor activity by interfering with Ras·GTP-effector interaction. Enzymes. 2013;34 Pt. B:1-23.

[3]Shima F, Yoshikawa Y, Ye M, et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction. Proc Natl Acad Sci U S A. 2013;110(20):8182‐8187

Kobe0065 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.12mL

2.22mL

1.11mL

22.23mL

4.45mL

2.22mL

Kobe0065 技术信息

CAS号	436133-68-5
分子式	C₁₅H₁₁ClF₃N₅O₄S
分子量	449.792

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 40 mg/mL(88.93 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

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

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分子量

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全球学术期刊中引用的产品

Kobe0065 质控信息

Kobe0065 生物活性

Kobe0065 参考文献

Kobe0065 实验方案

Kobe0065 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

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Kobe0065 纯度/质量文件产品仅供科研