A-83-01-sodium-salt - TGF-β Receptor 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEA83-01 sodium saltCat. No.: HY-10432A分式: CHNNaS分量: 444.51作靶点: TGF- Receptor作通路: TGF-beta/Smad储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 100 mg/mL (224.97 mM; Need

2、ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 5 mg/mL (11.25 mM); Suspended solution; Need ultrasonic and warming2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 5 mg/mL (11.25 mM); Suspended solution; Need ultrasonic and warming3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubili

3、ty: 5 mg/mL (11.25 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 A 83-01 sodium salt种有效的 TGF- I 型受体 ALK5，及 ALK4 和 ALK7 抑制剂，能够抑制 ALK5，ALK4和 ALK7 诱导的转录，IC50 值分别为 12，45 和 7.5 nM。IC50 & Target IC50: 12 nM (ALK5, cell-based), 45 nM (ALK4 cell-based), 7.5 nM (A

4、LK7 cell-based) 1体外研究 A 83-01 sodium salt is a potent inhibitor of TGF- type I receptor ALK5 kinase, type I activin/nodal receptorALK4 and type I nodal receptor ALK7, reduces the level of ALK-5-induced transcription with an IC50 of 12nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced tra

5、nscription with IC50s of 45 nM and 7.5nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, andALK-1. A 83-01 (0.03-10 M) potently prevents the growth-inhibitory effects of TGF-, and completely inhibitsthe effect at 3 M. A 83-01 (1-10 M) inhibits TGF-indu

6、ced Smad activation in HaCaT cells 1. A 83-01 (1M) decreases cell motility, adhesion and invasion increased by TGF-1 in HM-1 cells, but does not changecell proliferation 2.体内研究 A 83-01 (50, 150 and 500 g/mouse, i.p.) significantly improves survival of the mice without body weight orneurobehavioral a

7、ppearances 2. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect inmice bearing M109 cells 3.PROTOCOLCell Assay 2 HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A 83-01 (1 M) or vehicle are thenadded for 12 hr followed by the addition of TGF-1 (1 ng/mL)

8、or vehicle for 60 hr. The number of viable cellsin each well is examined using the WST-1 assay 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administration 2 Female B6C3F1 mice used for the in vivo studies are maintained under specific

9、pathogen-free conditions. Toevaluate the effect of A 83-01 on the survival of mice bearing peritoneal dissemination, HM-1 cells (1106)are injected into the abdominal cavity via the left flank of the mouse. Starting the next day, A 83-01 (150 g/body) or vehicles (PBS with 0.5% DMSO) are injected into

10、 the abdominal cavity three times per week. Miceare euthanized before reaching the moribund state 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Gynecol Oncol. 2019 Mar 27. pii: S0090-8258(19)30136-2. Gynecol Oncol. 2019 Mar 27. pii: S009

11、0-8258(19)30136-2.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growthfactor-beta. Cancer Sci. 2005 Nov

12、;96(11):791-800.2. Yamamura S, et al. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutictarget in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8.3. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF- type I receptor inhibitor. Cancer Sci.2010 Oct;101(10):2207-13.McePdfHeightCautio