溶解性 | DMSO 102 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
存贮条件 | 储存温度-20°C |
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. |
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 |
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 |
非美诺司他
CUDC-907 (订货以英文为准)
编号:C126527
CAS号:1339928-25-4
分子式:C23H24N8O4S
分子量:508.55
产品名称 | CUDC-907 |
中文名称 | 非美诺司他 |
CAS号 | 1339928-25-4 |
分子式(M.F.) | C23H24N8O4S |
分子量(M.W.) | 508.55 |
储存条件 | -20°C储存 |
Reaxys-RN | 6467047 |
个人防护设备 | Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter |
RTECS | EY8555800 |
WGK德国 | 3 |
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