PT-2385 - HIF-2α 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPT-2385Cat. No.: HY-12867CAS No.: 1672665-49-4分式: CHFNOS分量: 383.34作靶點(diǎn): HIF/HIF Prolyl-Hydroxylase作通路: Metabolic Enzyme/Protease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) DMSO : 50 mg/mL (130.

2、43 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.6087 mL 13.0433 mL 26.0865 mL5 mM 0.5217 mL 2.6087 mL 5.2173 mL10 mM 0.2609 mL 1.3043 mL 2.6087 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)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

3、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: 2.5 mg/mL (6.52 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.52 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn o

4、il1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.52 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 PT-2385選擇性 HIF-2 抑制劑，Ki 值于 50 nM 1 2。IC50 & Target Kd: 1體外研究 PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1 1.體內(nèi)研究 PT-2385 (PT2385)

5、inhibits expression of HIF-2 regulated genes in a dose dependent manner in vivo. Tumoris regressed with PT-2385 (3 and 10 mg/kg, p.o., b.i.d. dose) in 786-O xenograft. PT-2385 (1,3 and 10mg/kg) also inhibits tumor-derived VEGFA protein levels. PT-2385 (10 mg/kg) treatment reduces proliferation(Ki67)

6、 and angiogenesis (CD-31) 1.戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) Nat Med. 2017 Nov;23(11):1298-1308. J Clin Invest. 2019 Jan 2;129(1):336-348. Cell Death Dis. 2017 Oct 12;8(10):e3095. Drug Metab Dispos. 2018 Apr;46(4):336-345. PLoS One. 2018 Dec 19;13(12):e0208579.See more customer validations on HYPERLINK / www.MedChemEREF

7、ERENCES1. Eli Wallace, Ph.D. PT2385: HIF-2 Antagonist for the Treatment of VHL Mutant ccRCC. 12th International VHL Medical SymposiumApril 8, 2016.2. Xie C, et al. Activation of intestinal hypoxia-inducible factor 2 during obesity contributes to hepatic steatosis. Nat Med. 2017Nov;23(11):1298-1308.McePdfHeightCaution: Product has not been fully validated for medical applications.For research u