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非美诺司他, 组蛋白去乙酰化酶抑制剂

规格或纯度: 98%
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货号 (SKU) 包装规格 是否现货 价格 数量
C126527-1mg
 1mg 现货 Stock Image
C126527-5mg
 5mg 现货 Stock Image
C126527-10mg
 10mg 现货 Stock Image
C126527-25mg
 25mg 现货 Stock Image
C126527-50mg
 50mg 现货 Stock Image
C126527-100mg
 100mg 现货 Stock Image
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基本描述

英文别名 CUDC-907|Fimepinostat|1339928-25-4|CUDC 907|CUDC907|PI3K/HDAC Inhibitor|Fimepinostat [USAN]|N-hydroxy-2-[[2-(6-methoxypyridin-3-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl-methylamino]pyrimidine-5-carboxamide|N-hydroxy-2-(((2-(6-methoxypyridin-
规格或纯度 98%
英文名称 CUDC-907
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) 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 . 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 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 . Clinical trial: Phase I Study to Assess the Safety, Tolerability and Pharmacokinetics of CUDC-907 in Patients With Lymphoma or Multiple Myeloma.
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

产品介绍 

CUDC-907是一种PI3K和HDAC双重抑制剂，作用于PI3Kα和HDAC1/2/3/10，IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。CUDC-907 在乳腺癌细胞中可诱导细胞周期阻滞与凋亡。

产品属性

ALogP 1.3

名称和标识符

IUPAC Name N-hydroxy-2-[[2-(6-methoxypyridin-3-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl-methylamino]pyrimidine-5-carboxamide
INCHI InChI=1S/C23H24N8O4S/c1-30(23-25-11-15(12-26-23)22(32)29-33)13-16-9-17-19(36-16)21(31-5-7-35-8-6-31)28-20(27-17)14-3-4-18(34-2)24-10-14/h3-4,9-12,33H,5-8,13H2,1-2H3,(H,29,32)
InChi Key JOWXJLIFIIOYMS-UHFFFAOYSA-N
Canonical SMILES CN(CC1=CC2=C(S1)C(=NC(=N2)C3=CN=C(C=C3)OC)N4CCOCC4)C5=NC=C(C=N5)C(=O)NO
Isomeric SMILES CN(CC1=CC2=C(S1)C(=NC(=N2)C3=CN=C(C=C3)OC)N4CCOCC4)C5=NC=C(C=N5)C(=O)NO
PubChem CID 54575456
分子量 508.55

化学和物理性质

溶解性 DMSO 102 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

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参考文献

1. Qian C, Lai CJ, Bao R, Wang DG, Wang J, Xu GX, Atoyan R, Qu H, Yin L, Samson M et al..  (2012)  Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling..  Clin Cancer Res,  18  (15):  (4104-13).  [PMID:22693356]
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