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Ro 5126766

Ro 5126766

产品编号 T6971   CAS 946128-88-7
别名: RO5126766, CH5126766

Ro5126766 是双重MEK/RAF 抑制剂,抑制BRAFV600E、CRAF、MEK 和 BRAF,IC50分别为 8.2、56、160 和 190 nM。

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Ro 5126766, CAS 946128-88-7
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产品目录号及名称: Ro 5126766 (T6971)
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纯度: 98.3%
纯度: 98.13%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM, 19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively. Phase 1.
靶点活性 BRAF:19 nM, CRAF:56 nM, BRaf V600E:8.2 nM, MEK1:160 nM
体外活性 In HCT116 KRAS-mutant colorectal cancer cells, CH5126766 significantly reduces the levels of phospho-MEK and phospho-ERK. CH5126766 inhibits RAF kinase by binding to MEK1, and causes MEK to become a dominant negative inhibitor of RAF. [1] In Raf or RAS-mutant cell lines SK-MEL-28, SK-MEL-2, MIAPaCa-2, SW480, HCT116, and PC3 cells, CH5126766 inhibits cell growth with IC50 of 65, 28, 40, 46, and 277 nM, respectively. In two melanoma cell lines with the BRAF V600E or NRAS mutation, RO5126766 induces G1 cell cycle arrest accompanied by up-regulation of the CDK inhibitor p27 and down-regulation of cyclinD1. [3]
体内活性 In an HCT116 (G13D KRAS) mouse xenograft model, CH5126766 (25 mg/kg, p.o.) inhibits ERK signaling output more effectively than a standard MEK inhibitor that induces MEK phosphorylation and has potent antitumor activity. [1] In the HCT116 (K-ras) and COLO205 (B-raf) mutant xenografts, CH5126766 (0.3 mg/kg) causes significant decreases in [18?F]FDG uptake. [2] In the SK-MEL-2 xenograft model, RO5126766 also suppresses the tumor growth. [3]
激酶实验 MEK and RAF kinase enzyme assays: The inhibitory activities against CRAF, BRAF, or BRAF V600E enzymes are measured by quantification of phosphorylation of inactive K97R MEK1 [MEK1] by recombinant RAF proteins [BRAF: B-RAF wt, BRAF V600E: B-RAF V600E or CRAF: Raf-1] with Europium-anti-MEK1/2 (pSer218/222) antibody and SureLight allophycocyanine-anti-6his antibody by measuring time-resolved fluorescence (TRF). Alternatively, the inhibitory activities against the RAF enzymes are measured by quantification of phosphorylation of a fluorescein-labeled peptide corresponding to human MEK1 212-224 and human MEK2 217-229 (5-Fl-SGQLIDSMANSFV-NH2, MEKtide) by using the IMAP fluorescence polarization (FP) Screening Express Kit. Inhibition of MEK1 is evaluated by a coupled assay with active MEK1 (MEK1 S218E/S222E) and unactive dephosphorylated ERK2 (MAP kinase 2/Erk 2). The phosphorylation of a fluorescent-labeled peptide substrate (FAM-Erktide, IPTTPITTTYFFFK-5FAM-COOH) by ERK2 is quantified by using the IMAP FP Screening Express Kit.
细胞实验 The number of viable cells is determined using the Cell Counting Kit-8 assay according to the manufacturer's instructions. After the incubation of cells for 72 h with the indicated concentrations of various agents, kit reagent WST-8 is added to the medium and incubated for a further 4 h. The absorbance of samples (450 nm) is determined using a scanning multiwell spectrophotometer that serves as an ELISA reader. Cell numbers and viability are also measured using the ViaCount Assay according to the manufacturer's instructions.(Only for Reference)
别名 RO5126766, CH5126766
分子量 471.46
分子式 C21H18FN5O5S
CAS No. 946128-88-7

存储

 | Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 87 mg/mL (184.5 mM)

Ethanol: <1 mg/mL

H2O: <1 mg/mL

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Ishii N, et al. Cancer Res. 2013, 73(13), 4050-4060. 2. Miller CR, et al. Gynecol Oncol. 2014, 133(1), 128-137. 3. Wada M, et al. PLoS One. 2014, 9(11), e113217.
6H05 B-Raf IN 13 PROTAC B-Raf degrader 1 Pseudoginsenoside Rh2 I-37 Griffipavixanthone LY2452473 NSC-70220

相关化合物库

该产品包含在如下化合物库中:
MAPK 抑制剂库 抗胰腺癌化合物库 激酶抑制剂库 抗肥胖化合物库 抗前列腺癌化合物库 HIF-1化合物库 抗癌临床化合物库 已知活性化合物库 ReFRAME 相关化合物库 抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
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计算器

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稀释计算器
配液计算器
分子量计算器
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Ro 5126766 946128-88-7 MAPK Raf MEK MAPKK RO5126766 CH 5126766 CH5126766 Raf kinases Mitogen-activated protein kinase kinase inhibit Ro-5126766 CH-5126766 MAP2K Inhibitor inhibitor

 

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