|4-(3-吡啶-2-基-1H-吡唑-4-基)喹啉|CsnPharm

CAS No.: 396129-53-6

4-(3-(Pyridin-2-yl)-1H-pyrazol-4-yl)quinoline Catalog No. CSN11348

Synonyms: HTS466284;TGF-β RI Kinase Inhibitor

LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, exhibits 7-fold selectivity over TGFβR-II.

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实验方案

技术信息

生物活性

靶点 TGFβR1

IC50:59nM
描述The TGF-β pathway regulates a wide variety of cellular processes in many different cell types and biological contexts. There are three identified TGF receptor ligands, TGF-β1, 2 and 3. Activated TGF-β ligands can interact with TGF-β type II receptors (TβRII), then recruit and phosphorylate the TGF-β type I receptors (also called as TβRI or ALK5). In turn, activated TβRI phosphorylates SMAD2 and SMAD3 at C-terminal serine residues. Following that, phosphorylated SMAD and SMAD3 assemble into heterodimeric and trimeric complexes with SMAD4. Then the trimeric complex translocates into the nucleus and regulates the expression of TGF-β target genes^[2]. LY364947 is a multiple inhibitor with IC50 values of 0.059, 0.4, 1.4uM for TGF-βRI, TGF-βRII and MLK-7, respectively (measured by kinase activity)^[1]. Addition of 400nM LY364947 for 24h can block the Smad phosphorylation induced by exogenous TGFβ1 in U251, U87MG and GL261 glioma cell lines. Pre-treatment with 400nM LY364947 for24 hours before radiation exposure could significantly increase the radio sensitivity in all the three cell lines, accompanied with the decreased radiation-induced phosphorylation of ATM Ser-1981 and P53-Ser15 as well as fewer γH2AX foci, a marker of DNA damage response. These indicated that TGFβ inhibition by LY364947 could abrogate the response to DNA damage and increase radio sensitivity in glioma cells^[3]. Treatment with 2µM LY364947 for 24h can prevent TGF-β-induced epithelial-mesenchymal transition in NMuMg cells^[4].
作用机制LY364947 is an ATP competitive inhibitor of the TGFβ type I receptor.^[4]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HepG2 cells	-	Function assay	-	Inhibition of TGF-beta-induced expression of PAI-luciferase reporter in HepG2 cells, IC50=0.06 μM	14643325
mink Mv1Lu lung cells	-	Function assay	-	Inhibition of TGFbeta R1 induced transcriptional activation of p3TP-Lux in mink Mv1Lu lung cells, IC50=0.04 μM	16539403
NIH3T3 cells	-	Function assay	-	Inhibitory activity against TGF-beta-stimulated proliferation in NIH3T3 cells, IC50=0.081 μM	16539403

更多
动物研究
剂量
Mice (i.p.): 10 mg/kg^[5], 1 mg/kg^[6]

给药途径
i.p.
参考文献

动物研究
剂量	Mice (i.p.): 10 mg/kg^[5], 1 mg/kg^[6]
给药途径	i.p.

[1] Li HY, Wang Y, et al. Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7. J Med Chem. 2006 Mar 23;49(6):2138-42.
[2] Colak S, Ten Dijke P, et al. Targeting TGF-β Signaling in Cancer. Trends Cancer. 2017 Jan;3(1):56-71.
[3] Hardee ME, Marciscano AE, et al. Resistance of glioblastoma-initiating cells to radiation mediated by the tumor microenvironment can be abolished by inhibiting transforming growth factor-β. Cancer Res. 2012 Aug 15;72(16):4119-29.
[4] Peng SB, Yan L, et al. Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition. Biochemistry. 2005 Feb 22;44(7):2293-304.

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
- 3.6724 mL
- 18.3618 mL
- 36.7237 mL
- 5 mM
- 0.7345 mL
- 3.6724 mL
- 7.3447 mL
- 10 mM
- 0.3672 mL
- 1.8362 mL
- 3.6724 mL

技术信息

CAS号

396129-53-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H12N4

运输

蓝冰

分子量

272.30

别名

HTS466284;TGF-β RI Kinase Inhibitor

溶解度

DMSO	50.0 mg/mL (183.6 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	1 mg/mL	clear
PO	0.5% CMC-Na	41 mg/mL	suspension

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4-(3-(Pyridin-2-yl)-1H-pyrazol-4-yl)quinoline Catalog No. CSN11348

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