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Chemical Structure| 1421438-81-4 同义名 : LY3039478
CAS号 : 1421438-81-4
货号 : A236352
分子式 : C22H23F3N4O4
纯度 : 98%+
分子量 : 464.438
MDL号 : MFCD26142650
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(75.36 mM)，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
描述 LY3039478 is a potent Notch-1 intracellular domain (N1ICD) cleavage inhibitor with IC50 value of 0.41nM in SAR assays[1]. It inhibited N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment, and also resulted in the induction of apoptosis in a Notch-dependent xenograft model[2]. LY3039478 at concentration of 1μM and 10μM significantly inhibited the growth of Caki and 769-P, with decreased expression of Myc and Cyclin A1, two protein driven by Notch. G0/G1 cell cycle arrest could also be observed. Oral administration of LY3039478, 3 days per week, led a significant increase of survival and delayed tumor growth of immunodeficient NSG mice xenografted with 769-P CCRCC cells[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A2780 cells Function assay 24 h Inhibition of gamma-secretase mediated cleavage of Notch 1 in human A2780 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA, IC50=0.00103 μM 24900678
A375 cells Function assay 24 h Inhibition of gamma-secretase mediated cleavage of Notch 1 in human A375 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA, IC50=0.00048 μM 24900678
BxPC3 cells Function assay 24 h Inhibition of gamma-secretase mediated cleavage of Notch 1 in human BxPC3 cells assessed as nuclear accumulation of Notch 1 intracellular domain (N1ICD) after 24 hrs by ELISA, IC50=0.00039 μM 24900678
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.77mL

2.15mL

1.08mL

21.53mL

4.31mL

2.15mL
参考文献

[1]Warren J. P. Discovery of a Novel Notch Inhibitor.The 8th SCI-RSC Symposium on Proteinase Inhibitor Design April 15-16, 2013, Basel, Switzerland.

[2]Mark H. B, Hong G, et al. Novel inhibitor of Notch signaling for the treatment of cancer. Abstract 1131, AACR 104th Annual Meeting 2013.

[3]Bhagat TD, Zou Y, et al. Notch Pathway Is Activated via Genetic and Epigenetic Alterations and Is a Therapeutic Target in Clear Cell Renal Cancer. J Biol Chem. 2017 Jan 20;292(3):837-846.