OTX008-Calixarene-0118-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEOTX008Cat. No.: HY-19756CAS No.: 286936-40-1Synonyms: Calixarene 0118; PTX008分式: CHNO分量: 937.18作靶點(diǎn): Galectin作通路: Immunology/Inflammation儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) Ethanol : 33

2、.33 mg/mL (35.56 mM)DMSO : 10 mg/mL (10.67 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.0670 mL 5.3352 mL 10.6703 mL5 mM 0.2134 mL 1.0670 mL 2.1341 mL10 mM 0.1067 mL 0.5335 mL 1.0670 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)

3、驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1 mg/mL (1.07 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecu

4、les 您邊的抑制劑師www.MedChemESolubility: 1 mg/mL (1.07 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 1 mg/mL (1.07 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 OTX008個(gè)半乳糖凝集素 1 (galectin-1) 的選擇性抑制劑。IC50 & Target Galectin-1 1.體外研究 Growth inhibitory concentrations (GI50) of OTX008 in a large

5、 panel of human solid tumour cell lines rangesfrom 3 to 500 M. A significant correlation between OTX008 GI50 values and Gal1 mRNA (LGALS1) andprotein expression levels in the panel of cancer cells is observed. In SQ20B and A2780-1A9 cells, OTX008inhibits Gal1 expression and ERK1/2 and AKT-dependent

6、survival pathways, and induces G2/M cell cyclearrest through CDK1. OTX008 enhances the anti-proliferative effects of Semaphorin-3A (Sema3A) in SQ20Bcells and reverses invasion induced by exogenous Gal1 1. OTX008 affects endothelial cell proliferation,motility, invasiveness, and cord formation. Tumor

7、 cell proliferation is also inhibited, with differences insensitivity among cell lines (IC50 from 1 to 190 M) 2.體內(nèi)研究 OTX008 inhibits growth of A2780-1A9 xenografts. OTX008 treatment is associated with down-regulation ofGal1 and Ki67 in treated tumours, as well as decreased microvessel density and VE

8、GFR2 expression.Finally, combination studies show OTX008 synergy with several cytotoxic and targeted therapies, principallywhen OTX008 is administered first 1.PROTOCOLAnimal Mice 1Administration 1 A total of 8106 A2780-1A9 ovarian cells are injected subcutaneously into the right lateral flank of fem

9、alenu/nu athymic mice. Once tumours are palpable (50 mm3), mice are randomised to receive treatmentintraperitoneally with either PBS (3 times/week), 5 mg/kg OTX008 (3 times/week), 6 mg/kg cisplatin (days 1,8 and 15) or 10 mg/kg docetaxel (days 1, 8 and 15). Tumour size was measured twice weekly with

10、 calipersand tumour volume is calculated as 3.14(width2)/length 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Astorgues-Xerri L, et al. OTX008, a selective small-molecule inhibitor of galectin-1, downregulates cancer cell proliferation,

11、 invasion andtumour angiogenesis. Eur J Cancer. 2014 Sep;50(14):2463-77.2. Zucchetti M, et al. Pharmacokinetics and antineoplastic activity of galectin-1-targeting OTX008 in combination with sunitinib. CancerChemother Pharmacol. 2013 Oct;72(4):879-87.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: Product has not