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Chemical Structure| 1951483-29-6 同义名 : LY3214996
CAS号 : 1951483-29-6
货号 : A668057
分子式 : C22H27N7O2S
纯度 : 99%+
分子量 : 453.56
MDL号 : MFCD31544324
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(39.69 mM)，配合低频超声助溶，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：
生物活性
靶点

  • ERK2

    ERK2, IC50:5 nM

  • ERK1

    ERK1, IC50:5 nM
描述 ERK1 (Extracellular Signal-Regulated Kinase 1) and ERK2 belong to the MAP kinase family. ERK1 and ERK2 are the 2 ERKs which play an important role in the MAPK/ERK cascade. Depending on the cellular context, the MAPK/ERK cascade mediates diverse biological functions such as cell growth, adhesion, survival and differentiation through the regulation of transcription, translation, cytoskeletal rearrangements[2]. LY3214996 is a selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. Anti-tumor activity of LY3214996 was observed in tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation[1]. Another report suggested that LY3214996 may be effective against patient derived RAS-mutant NSCLC cell lines[3]. In tumor xenograft models, LY3214996 inhibits pharmadynamic biomarker phospho-p90RSK1 in tumors. 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[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.02mL

2.20mL

1.10mL

22.05mL

4.41mL

2.20mL
参考文献

[1]Abstract 4973: Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations

[2]Functions of ERK1 and ERK2.

[3]Abstract 5467: Efficacy of the ERK inhibitor LY3214996 and the PI3K/mTOR inhibitor LY3023414 in patient-derived RAS-mutant NSCLC models