1339928-25-4CUDC-907

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商品编号：C126527

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商品名称：1339928-25-4CUDC-907
商品毛重：0.00
单位：件
上架时间：2017-11-01 18:29:58

名称: CUDC-907英文名称: CUDC-907≥99%产品编号 C126527
CAS号: 1339928-25-4分子式 C₂₃H₂₄N₈O₄S分子量508.55

属性

溶解性	DMSO 102 mg/mL Water Ethanol
存贮条件	储存温度-20°C

描述

别名	N-hydroxy-2-(((2-(6-methoxypyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)(methyl)amino)pyrimidine-5-carboxamide;N-hydroxy-2-(((2-(6-methoxypyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)(methyl)amino)pyrimidine-5-carboxamide
生化机理	Description: IC50 Value: 1.7/5.0/1.8/2.8 nM (HDAC1/2/3/10); 19/54/39 nM (PI3Kα/β/δ) [1] CUDC-907 potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes. in vitro: CUDC-907 induced the accumulation of acetylated histone H3, tubulin, and p53, as well as p21 expression in a dose-dependent manner (Supplementary Figs. S2-S5). Similarly, we observed that CUDC-907 inhibited the PI3K pathway, as indicated by the dose-dependent decreases in phosphorylation of AKT and its downstream targets, 4EBP-1 and p70S6, in H460 cells. CUDC-907 induced caspase-3 and -7 activation in HCT-116 colon cancer cells in a dose-dependent manner [1]. in vivo: oral administration of CUDC-907 inhibited growth of the Daudi cancer cell xenografts in a dose-dependent manner. Tumor stasis was observed at 100 mg/kg in this model without obvious toxicity. Furthermore, CUDC-907 caused tumor regression or stasis after intravenous (50 mg/kg) or oral administration (100 mg/kg) in a xenograft tumor model of SU-DHL4 diffuse large B-cell lymphoma (DLBCL) and caused tumor stasis in KRAS-mutant A549 NSCLC cell xenografts [1]. Toxicity: oral administration of CUDC-907 inhibited growth of the Daudi cancer cell xenografts in a dose-dependent manner. Tumor stasis was observed at 100 mg/kg in this model without obvious toxicity [1]. Clinical trial: Phase I Study to Assess the Safety, Tolerability and Pharmacokinetics of CUDC-907 in Patients With Lymphoma or Multiple Myeloma. Phase 1
备注	CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. Phase 1.