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GNE-272

    
≥98%

GNE-272

源葉(MedMol)
S84185 一鍵復制產品信息
1936428-93-1
C22H27FN6O2
426.4872
貨號 規格 價格 上海 北京 武漢 南京 購買數量
S84185-5mg
≥98% ¥1900.00 貨期:2-3天 - - -
S84185-10mg
≥98% ¥3000.00 貨期:2-3天 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300

產品描述: GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300
靶點: IC50: 0.02 μM (CBP), 0.03 μM (EP300), 13 μM (BRD4);EpigeneticReaderDomain
體外研究: GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. When tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel, GNE-272 does not inhibit any target at >30%. In addition, GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). The compound has good potency in the BRET cellular assay. In an orthogonal measure of the target engagement, GNE-272 is shown to inhibit the expression of MYC10 (MV4?11 cell line) with an EC50 of 0.91 μM and good correlation between the BRET and MYC cellular assays is observed
體內研究: GNE-272 demonstrates 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. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model
溶解性: soluble  in  DMSO
保存條件: -20℃
配置溶液濃度參考:
1mg 5mg 10mg
1 mM 2.345 ml 11.724 ml 23.447 ml
5 mM 0.469 ml 2.345 ml 4.689 ml
10 mM 0.234 ml 1.172 ml 2.345 ml
50 mM 0.047 ml 0.234 ml 0.469 ml
注意: 部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。

參考文獻

質檢證書(COA)

如何獲取質檢證書(COA)?
請輸入貨號和一個與之匹配的批號。
例如:
批號:JS298415 貨號:S20001-25g
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摩爾濃度計算器

質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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