Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Temuterkib (LY3214996) 是高效选择性的ERK1和ERK2抑制剂,IC50为 5 nM,具有潜在的抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 678 | 现货 | ||
2 mg | ¥ 980 | 现货 | ||
5 mg | ¥ 1,820 | 现货 | ||
10 mg | ¥ 2,820 | 现货 | ||
25 mg | ¥ 4,690 | 现货 | ||
50 mg | ¥ 6,680 | 现货 | ||
100 mg | ¥ 8,900 | 现货 | ||
500 mg | ¥ 17,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,820 | 现货 |
产品描述 | Temuterkib (LY3214996) is a potent and selective, orally available inhibitor of the extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity. |
靶点活性 | ERK2:5 nM, ERK1:5 nM |
体外活性 | LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to LY3214996[1]. |
体内活性 | In tumor xenograft models, LY3214996 inhibits PD biomarker phospho-p90RSK1 in tumors and the PD effects are correlated with compound exposures and anti-tumor activities. LY3214996 shows either similar or superior anti-tumor activity as compared to other published ERK inhibitors in BRAF or RAS mutant cell lines and xenograft models. Oral administration of single-agent LY3214996 significantly inhibits tumor growth in vivo and is well tolerated in BRAF or NRAS mutant melanoma, BRAF or KRAS mutant colorectal, lung and pancreatic cancer xenografts or PDX models. Therefore, LY3214996 can be tailored for treatment of cancers with MAPK pathway alteration. In addition, LY3214996 has anti-tumor activity in a Vemurafenib-resistant A375 melanoma xenograft model due to MAPK reactivation, may have potential for treatment of melanoma patients who have failed BRAF therapies. More importantly, LY3214996 can be combined with investigational and approved agents in preClinicalal models, particularly KRAS mutant models. Combination treatment of LY3214996 and CDK4/6 inhibitor abemaciclib is well tolerated and results in potent tumor growth inhibition or regression in multiple in vivo cancer models, including KRAS mutant colorectal and non-small cell lung cancers[1]. |
别名 | LY3214996 |
分子量 | 453.56 |
分子式 | C22H27N7O2S |
CAS No. | 1951483-29-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12 mg/mL (26.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2048 mL | 11.0239 mL | 22.0478 mL | 55.1195 mL |
5 mM | 0.441 mL | 2.2048 mL | 4.4096 mL | 11.0239 mL | |
10 mM | 0.2205 mL | 1.1024 mL | 2.2048 mL | 5.5119 mL | |
20 mM | 0.1102 mL | 0.5512 mL | 1.1024 mL | 2.756 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Temuterkib 1951483-29-6 MAPK ERK inhibit Extracellular signal regulated kinases LY-3214996 LY 3214996 LY3214996 Inhibitor inhibitor