價(jià)格 | ¥913 | ¥1720 | ¥7690 |
包裝 | 2mg | 5mg | 25mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2025-02-28 |
中文名稱:化合物 GNE-272 | 英文名稱:GNE-272 |
CAS:1936428-93-1 | 品牌: TargetMol |
產(chǎn)地: 美國(guó) | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
產(chǎn)品類別: 抑制劑 | |
貨號(hào): T15400 |
名稱 | GNE-272 |
描述 | GNE-272 is a selective inhibitor of CBP/EP300 (IC50: 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively) and a selective in vivo probe for CBP/EP300. |
體外活性 | GNE-272 does not inhibit any target at >30% when tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel. GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. The compound has good potency in the BRET cellular assay. GNE-272 is shown to inhibit the expression of MYC10 (MV4?11 cell line) (EC50: 0.91 μM) and a good correlation between the BRET and MYC cellular assays is observed. |
體內(nèi)活性 | GNE-272 displays a marked antiproliferative effect in hematologic cancer cell lines. Which modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. GNE-272 shows low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM. |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 100 mg/mL (235.59 mM), Sonication is recommended. |
關(guān)鍵字 | GNE 272 | GNE-272 | GNE272 |
相關(guān)產(chǎn)品 | Bisdemethoxycurcumin | dBET6 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | CeMMEC1 | (+)-JQ-1 | Curcumin | Naphthol AS-E | J-147 | ABBV-744 | Piflufolastat | Hexamethylene bisacetamide | Anacardic Acid |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.265100萬(wàn)人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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