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抑制剂/激活剂

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凋亡与自噬

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LY2109761

LY2109761是可口服，选择性的 TGF-β receptor type I/II 抑制剂，Ki分别为38 nM 和 300 nM。

货号：
TK0484
规格：

1mg

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	700874-71-1
生物活性	LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
分子式	C26H27N5O2
分子量	441.52
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 25 mg/mL (56.62 mM; Need ultrasonic)
体内研究	LY2109761 (50 mg/kg, p.o.) greatly reduces the tumor volume and increases the median survival duration of the mice to 45.0 days. The mice treated with LY2109761 develop significantly fewer metastatic lesions and, in some of them, no metastatic lesion, as indicated by the GFP signal, can be identified in the abdomen. LY2109761 enhances radiation-induced tumor growth delay in a U87MG subcutaneous xenograft tumor model in BALB/c nude mice. LY2109761 increases survival in an orthotopical CSLC glioblastoma model and enhanced antitumor activity of radiation.
体外研究	LY2109761 significantly inhibits the growth of L3.6pl/GLT soft agar colonies in a dose-dependent manner, and results in appr 33% inhibition at 2 μM and 73% inhibition at 20 μM. Targeting TβRI/II kinase activity with LY2109761 (5 μM) almost completely suppresses both the basal and TGF-β1-stimulated migration of L3.6pl/GLT cells. LY2109761 induces a dose-dependent reduction in phosphorylation of Smad-2. HLE endogenous phosphorylation of Smad-2 is inhibited by LY2109761. LY2109761 blocks migration on different ECM proteins and invasion of both HLE and HLF through a 3-dimensional structure. LY2109761 increases E-cadherin mRNA expression after 24 hours and protein levels after 48 hours. LY2109761 pretreatment reduces clonogenic survival in cell cultures of U87MG and T98 following radiation, resulting in an increase in the radiosensitivity with a DEF0.1 of 1.30 and 1.37, respectively.
文献	•Cell Res. 2020 Jul;30(7):610-622. •J Hepatol. 2015 Oct;63(4):863-73. •Sci Transl Med. 2020 Mar 25;12(536):eaay8456. •Nat Commun. 2017 Aug 18;8(1):286. •Cell Rep. 2020 Apr. •Sci Total Environ. 2020 Aug 20;731:139234. •Int J Biol Sci. 2019 Sep 7;15(11):2393-2407. •Biomed Pharmacother. 2020, 110610. •Ecotoxicol Environ Saf. 2021 Nov 30;228:113040. •Acta Pharmacol Sin. 2021 Mar 23. •J Dent Res. 2019 Jul;98(8):896-903. •FEBS J. 2020 Feb;287(4):783-799. •J Cell Mol Med. 2021 Apr;25(7):3498-3510. •Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836. •Int Immunopharmacol. 2020 Aug;85:106686. •Invest Ophthalmol Vis Sci. 2021 Jul 1;62(9):29. •J Cell Biochem. 2019 Oct;120(10):17872-17886. •Mol Immunol. 2018 Nov;103:173-181. •Int J Mol Med. 2020 Jul;46(1):167-178. •Int J Mol Med. 2015 Jun;35(6):1667-74. •Am J Transl Res. 2019 Apr 15;11(4):2155-2167. •Cell Biol Int. 2017 Sep;41(9):960-968. •Mol Cell Biochem. 2020 Jul;470(1-2):215-227. •Mol Cell Biochem. 2019 Jun;456(1-2):95-104. •Brain Sci. 2021 Jan 8;11(1):77. •Exp Ther Med. 2021 Jan;21(1):6. •Research Square Preprint. 2021 Sep. •First Department of Internal Medicine, Faculty of Medicine, UNIVERSITY of TOYAMA, TOYAMA, JAPAN. 2019 May. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

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