首页 工具
登录
购物车
Refametinib

Refametinib

产品编号 T6636   CAS 923032-37-5
别名: BAY 86-97661, 瑞法替尼//瑞美替尼, BAY 869766, RDEA119

Refametinib (RDEA119) 是可口服的、非 ATP 竞争和选择性的 MEK1/MEK2变构抑制剂,IC50分别为 19 和 47 nM。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
Refametinib Chemical Structure
Refametinib, CAS 923032-37-5
规格 价格/CNY 货期 数量
1 mg ¥ 263 现货
2 mg ¥ 375 现货
5 mg ¥ 598 现货
10 mg ¥ 923 现货
25 mg ¥ 1,530 现货
50 mg ¥ 2,260 现货
100 mg ¥ 3,920 现货
1 mL * 10 mM (in DMSO) ¥ 777 现货
产品目录号及名称: Refametinib (T6636)
点击图片重新获取验证码
选择批次  
纯度: 100%
纯度: 99.84% ee: 97.95%
纯度: 99.53%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).
靶点活性 MEK2:47 nM, MEK1:19 nM
体外活性 RDEA119 is selectively bound directly to an allosteric pocket in the MEK1/2 enzymes, and highly efficacious at inhibiting cell proliferation in several tumor cell lines, including A375, SK-MEI-28, Colo205, HT-29 and BxPC3. RDEA119 inhibits anchorage-dependent growth of human cancer cell lines harboring the gain-of-function V600E BRAF mutant with GI50 values ranging from 67 to 89 nM. Under anchorage-independent conditions, GI50 values for all cell lines tested are similar (40-84 nM). RDEA119 shows a tissue selectivity that reduces its potential for central nervous system–related side effects. [1] RDEA119 potently inhibits the proliferation of the 4 cell lines that harbored BRAF mutation but has no or modest effects on the other 4 cells that harbored wild-type BRAF (IC50 of 0.034-0.217 μM vs. 1.413-34.120 μM). This inhibitory effect of RDEA119 in selected cell lines OCUT1 (BRAF V600E(+), PIK3CA H1047R(+)) and SW1376 (BRAF V600E(+)) is enhanced by combination with the mTOR inhibitor, temsirolimus. RDEA119 and temsirolimus also show synergistic effects on autophagic death of OCUT1 and KAT18 cells selectively tested. [2]
体内活性 Oral administration of RDEA119 at 50 mg/kg on a once daily x 14 schedule leads to a 68% tumor growth inhibition (TGI) in human melanoma A375 tumor model. Oral administration of RDEA119 at 25 mg/kg on a once a once daily x 14 schedule leads to a 123% TGI in human colon carcinoma Colo205 tumor model (TGI > 100% occurs when the tumor shrinks below its starting volume). A dose of 25 mg/kg once daily x 14 produces 56% and 67% TGI for HT-29 and A431 tumors, respectively. [1]
激酶实验 MEK Kinase Assay: Kinase inactive murine ERK2 (mERK2) K52A/T183A is affinity purified from Escherichia coli expressed using the pET21a vector. MEK1 kinase activity is determined using mERK2 K52A T183A as the substrate. Recombinant MEK1 enzyme (5 nM) is first activated by 0.02 unit or 1.5 nM of RAF1 in the presence of 25 mM HEPES (pH 7.8), 1 mM MgCl2, 50 mM NaCl, 0.2 mM EDTA, and 50 μM ATP for 30 minutes at 25 °C. The reactions are initiated by adding 2 μM of mERK2K52A T183A and 2.5 μCi [γ-33P] ATP in a total volume of 20 μL. The MEK2 kinase activity is determined similarly except that activation by RAF1 is not needed and 11 nM of MEK2 enzyme (active) are used in the assays.Kinase profiling is performed by Invitrogen using their Select Screen Kinase Profiling Service. The Z'-LYTE biochemical assay is used. RDEA119 is assayed in quadruplicate at 10 μM against 205 kinases.
细胞实验 For anchorage-dependent growth inhibition experiments, cells are plated in white 384-well plates at 1,000/20 μL/well or white 96-well microplates at 4,000/100 μL/well. After 24-h incubation at 37 °C, 5% CO2, and 100% humidity, RDEA119 is incubated for 48 hours at 37 °C and assayed using CellTiter-Glo. For the 96-well anchorage-independent growth assay, wells of an "ultralow binding" plate (Corning) are filled with 60 μL of a 0.15% agarose solution in complete RPMI 1640. Then, 60 μL of complete RPMI 1640 containing 9,000 cells in 0.15% agarose are added per well. After 24 hour, 60 μL of a 3 × drug solution in agarose-free complete RPMI 1640 are added. After 7 d, 36 μL of 6 × 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)- 2H-tetrazolium, inner salt reagent are added per well. After 2 hours at 37 °C, absorbance at 490 nm is determined on the M5 plate reader. (Only for Reference)
别名 BAY 86-97661, 瑞法替尼//瑞美替尼, BAY 869766, RDEA119
分子量 572.34
分子式 C19H20F3IN2O5S
CAS No. 923032-37-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 93 mg/mL (162.5 mM)

DMSO: 93 mg/mL (162.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.7472 mL 8.7361 mL 17.4721 mL 43.6803 mL
5 mM 0.3494 mL 1.7472 mL 3.4944 mL 8.7361 mL
10 mM 0.1747 mL 0.8736 mL 1.7472 mL 4.368 mL
20 mM 0.0874 mL 0.4368 mL 0.8736 mL 2.184 mL
50 mM 0.0349 mL 0.1747 mL 0.3494 mL 0.8736 mL
100 mM 0.0175 mL 0.0874 mL 0.1747 mL 0.4368 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Iverson C, et al, Cancer Res, 2009, 69(17), 6839-6847. 2. Liu D, et al, Int J Cancer, 2010, 127(12), 2965-2973. 3. Li Y, He Y, Peng J, et al. Mutant Kras co-opts a proto-oncogenic enhancer network in inflammation-induced metaplastic progenitor cells to initiate pancreatic cancer[J]. Nature Cancer. 2020: 1-17.
AZD8330 Trametinib (DMSO solvate) TAK-733 MEK-IN-6 hydrate BI-847325 RO4987655 Ro 5126766 Refametinib R enantiomer

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 酪氨酸激酶分子库 抗癌药物库 抗癌活性化合物库 ReFRAME 相关化合物库 抑制剂库 抗癌化合物库 细胞重编程化合物库 免疫/炎症分子化合物库 细胞凋亡化合物库

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
计算 重置

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

Refametinib 923032-37-5 MAPK MEK MEK1 allosteric inhibit BAY 86-97661 Inhibitor 瑞法替尼//瑞美替尼 MAP2K MEK2 BAY869766 orally MAPKK RDEA-119 Mitogen-activated protein kinase kinase BAY-869766 tumor BAY 869766 RDEA119 RDEA 119 inhibitor

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼