OTX008 - CAS 286936-40-1
Catalog number: 286936-40-1
Category: Inhibitor
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OTX008, a calixarene derivative, is a galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities. In vitro, OTX008 effects in a panel of human cancer cell lines. In vivo, an ovarian xenograft model was employed to analyse the antitumour activity.
Solid powder
Acetamide, 2,2',2'',2'''-[pentacyclo[,7.19,13.115,19]octacosa-1(25),3,5,7(28),9,11,13(27),15,17,19(26),21,23-dodecaene-5,11,17,23-tetrayltetrakis(oxy)]tetrakis[N-[2-(dimethylamino)ethyl]-.; OTX-008; OTX 008; OTX008; PTX008; PTX-008; PTX 008; calixarene 0118; N(2dimethylamino)ethyl)acetamidyl calix4arene
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1.Inhibition of Galectin-1 Sensitizes HRAS-driven Tumor Growth to Rapamycin Treatment.
Michael JV;Wurtzel JG;Goldfinger LE Anticancer Res. 2016 Oct;36(10):5053-5061.
The goal of this study was to develop combinatorial application of two drugs currently either in active use as anticancer agents (rapamycin) or in clinical trials (OTX008) as a novel strategy to inhibit Harvey RAS (HRAS)-driven tumor progression. HRAS anchored to the plasma membrane shuttles from the lipid ordered (L;o;) domain to the lipid ordered/lipid disordered border upon activation, and retention of HRAS at these sites requires galectin-1. We recently showed that genetically enforced L;o; sequestration of HRAS inhibited mitogen-activated protein kinase (MAPK) signaling, but not phoshatidylinositol 3-kinase (PI3K) activation. Here we show that inhibition of galectin-1 with OTX008 sequestered HRAS in the L;o; domain, blocked HRAS-mediated MAPK signaling, and attenuated HRAS-driven tumor progression in mice. HRAS-driven tumor growth was also attenuated by treatment with mammalian target of rapamycin (mTOR) inhibitor rapamycin, and this effect was further enhanced in tumors driven by L;o;-sequestered HRAS. These drugs also revealed bidirectional cross-talk in HRAS pathways. Moreover, dual pathway inhibition with OTX008 and rapamycin resulted in nearly complete ablation of HRAS-driven tumor growth.
2.Suppression of Retinal Neovascularization by Inhibition of Galectin-1 in a Murine Model of Oxygen-Induced Retinopathy.
Yang N;Zhang W;He T;Xing Y J Ophthalmol. 2017;2017:5053035. doi: 10.1155/2017/5053035. Epub 2017 Mar 24.
Galectin-1 (Gal-1) has been proved to be an important factor in the process of tumor angiogenesis recently. As a small molecule, OTX008 serves as a selective inhibitor of Gal-1. In this study, the role of Gal-1 and the antiangiogenic effect of OTX008 on retinal neovascularization (RNV) were investigated using a mouse model of oxygen-induced retinopathy. The outcome indicated that Gal-1 was overexpressed and closely related to retinal neovessels in OIR. After intravitreal injection of OTX008 at P12, the RNV was significantly reduced at P17, measuring by cross-sectional H&E staining and whole-mount fluorescence. Our results demonstrate the inhibitory function of OTX008 on RNV, which provides a promising strategy of treating retinal angiogenic diseases such as retinopathy of prematurity and proliferative diabetic retinopathy.
3.Galectin-1 is a new fibrosis protein in type 1 and type 2 diabetes.
Al-Obaidi N;Mohan S;Liang S;Zhao Z;Nayak BK;Li B;Sriramarao P;Habib SL FASEB J. 2018 Jul 5:fj201800555RR. doi: 10.1096/fj.201800555RR. [Epub ahead of print]
Chronic exposure of tubular renal cells to high glucose contributes to tubulointerstitial changes in diabetic nephropathy. In the present study, we identified a new fibrosis gene called galectin-1 (Gal-1), which is highly expressed in tubular cells of kidneys of type 1 and type 2 diabetic mouse models. Gal-1 protein and mRNA expression showed significant increase in kidney cortex of heterozygous Akita;+/-; and db/db mice compared with wild-type mice. Mouse proximal tubular cells exposed to high glucose showed significant increase in phosphorylation of Akt and Gal-1. We cloned Gal-1 promoter and identified the transcription factor AP4 as binding to the Gal-1 promoter to up-regulate its function. Transfection of cells with plasmid carrying mutations in the binding sites of AP4 to Gal-1 promoter resulted in decreased protein function of Gal-1. In addition, inhibition of Gal-1 by OTX-008 showed significant decrease in p-Akt/AP4 and protein-promoter activity of Gal-1 and fibronectin. Moreover, down-regulation of AP4 by small interfering RNA resulted in a significant decrease in protein expression and promoter activity of Gal-1. We found that kidney of Gal-1;-/-; mice express very low levels of fibronectin protein.
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