|(S)-N-(2,3-二羟基丙基)-3-((2-氟-4-碘苯基)氨基)异烟酰胺|CsnPharm

CAS No.: 1236699-92-5

N-[(2S)-2,3-二羟基丙基]-3-[(2-氟-4-碘苯基)氨基]-4-吡啶甲酰胺 Catalog No. CSN13700

Synonyms: AS703026;MSC1936369B;SAR-245509

AS7-03026 is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 MEK1

IC50:5nM-2μM MEK2

IC50:5nM-2μM
描述MEKs, which are members of the MAPKK family, can activate both ERK1 and ERK2 by catalyzing the phosphorylation on T202/Y204. It is found that the tumor growth, like multiple myeloma, and survival, as well as angiogenesis and drug resistance are markedly associated with the MEK/ERK signal transduction pathway. Pimasertib is a potent and selective inhibitor of MEK1/2. As prediction by the inhibition of MEK1/2 kinase activity, incubation with Pimasertib at concentration ranging in 5-2000nM for 1h caused dose-dependent as well as time-dependent, at concentration of 200nM within 72h, decrease of p-ERK1/2 in U266 cells. A further study showed that Pimasertib can targeted multiple myeloma cells in the BMSCs microenvironment specifically through block of MEK/ERK pathway and improved agent. Exposure to Pimasertib at concentration>20nM significantly decreased the secretion of the cytokines induced by adhesion of MM cells to BMSCs, including VEGF and IL-6 in a dose-dependent manner. Treatment with 0.5μM Pimasertib alone over 8h significantly triggered apoptosis, shown as PARP and caspase 3 cleavage in H929 MM cells, as well as increased subG0 and decreased S phase cell population at 0.1μM in both H929 and U266 cells within 72h. Combination of Pimasertib (20nM-20μM) with anti-MM drugs rapamycin (0.1-100nM) for 2 days can augment MM1S cell death. Orally treatment with Pimasertib at dose of both 15mg/kg and 30mg/kg, BID, 5 days per week for 2 weeks, inhibited human MM cell growth in mice bearing H929 MM tumours, accompanied with decreased p-ERK and induced apoptosis. Reduced percentage of CD34+ cells and microvascular density can also be observed in H929 tumours from mice treated with Pimasertib, suggesting the possible inhibitory effect on angiogenesis by Pimasertib in vivo^[1].
作用机制Pimasertib is an non-ATP competitive inhibitor of MEK1/2.^[1]
细胞研究
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
human COLO205 cells - Function assay - Inhibition of MEK1 in human COLO205 cells, IC50=0.00181 μM 24755426
动物研究
剂量
Mice: min = 10 mg/kg^[2], max = 30 mg/kg^[1]

给药途径
p.o.
临床研究

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human COLO205 cells	-	Function assay	-	Inhibition of MEK1 in human COLO205 cells, IC50=0.00181 μM	24755426

动物研究
剂量	Mice: min = 10 mg/kg^[2], max = 30 mg/kg^[1]
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01992874	Neoplasms	Phase 1	Completed	-	United States, Massachusetts ... more >> Please Contact U.S. Medical Information Located in Rockland, Massachusetts, United States Collapse <<
NCT01693068	N-Ras Mutated Locally Advanced... more >> or Metastasis Malignant Cutaneous Melanoma Collapse <<	Phase 2	Completed	-	-
NCT01713036	Locally Advanced or Metastatic... more >> Solid Tumors Collapse <<	Phase 1	Completed	-	Hungary ... more >> Research Site Budapest, Hungary Collapse <<

更多
参考文献

[1] Kim K, Kong SY, et al. Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. Br J Haematol. 2010;149(4):537-49.
[2] Yoon J, Koo KH, Choi KY. MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy. Cancer Res. 2011;71(2):445-53.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3191 mL
- 11.5955 mL
- 23.1911 mL
- 5 mM
- 0.4638 mL
- 2.3191 mL
- 4.6382 mL
- 10 mM
- 0.2319 mL
- 1.1596 mL
- 2.3191 mL

技术信息

CAS号

1236699-92-5

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H15FIN3O3

运输

蓝冰

分子量

431.20

别名

AS703026;MSC1936369B;SAR-245509

溶解度

DMSO	500.0 mg/mL (1159.6 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	11 mg/mL	suspension

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靶点	Description	IC50
MEK1		IC50:5nM-2μM
MEK2		IC50:5nM-2μM

N-[(2S)-2,3-二羟基丙基]-3-[(2-氟-4-碘苯基)氨基]-4-吡啶甲酰胺 Catalog No. CSN13700

靶点选择性

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