计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
CUDC-101是HDAC，EGFR和HER2抑制剂，IC50分别为4.4，2.4和15.7 nM。A potent inhibitor of HDACs and receptor tyrosine kinases
Information
CUDC-101 is a potent multi-targeted inhibitor againstHDAC,EGFRand HER2 withIC50of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
In vitro
Specific for class I and class II HDACs, CUDC-101 does not inhibit class III Sir-type HDACs. CUDC-101 displays weak activity against other protein kinases including KDR/VEGFR2, Lyn, Lck, Abl-1, FGFR-2, Flt-3, and Ret with IC50 of 0.85 μM, 0.84 μM, 5.91 μM, 2.89 μM, 3.43 μM, 1.5 μM, abd 3.2 μM, respectively. CUDC-101 displays broad antiproliferative activity in many human cancer cell types with IC50 of 0.04-0.80 μM, exhibiting a higher potency than erlotinib, lapatinib, and combinations of vorinostat with either erlotinib or lapatinib in most cases. CUDC-101 potently inhibits lapatinib- and erlotinib-resistant cancer cell lines. CUDC-101 inhibits the erlotinib-resistant EGFR mutant T790M although its effects are incomplete with an Amax of ~60% of peak enzyme activity after inhibition. CUDC-101 treatment increases the acetylation of histone H3 and H4, as well as the acetylation of non-histone substrates of HDAC such as p53 and α-tubulin, in a dose-dependant manner in various cancer cell lines. CUDC-101 also suppresses HER3 expression, Met amplification, and AKT reactivation in tumor cells.
In vivo
Administration of CUDC-101 at 120 mg/kg/day induces tumor regression in the Hep-G2 liver cancer model, which is more efficacious than that of erlotinib at its maximum tolerated dose (25 mg/kg/day) and vorinostat at an equimolar concentration dose (72 mg/kg/day). CUDC-101 inhibits the growth of erlotinib-sensitive H358 NSCLC xenografts in a dose-dependent manner. CUDC-101 also shows potent inhibition of tumor growth in the erlotinib-resistant A549 NSCLC xenograft model. CUDC-101 produces significant tumor regression in the lapatinib-resistant, HER2-negative, EGFR-overexpressing MDA-MB-468 breast cancer model and the EGFR-overexpressing CAL-27 head and neck squamous cell carcinoma (HNSCC) model. Additionally, CUDC-101 inhibits tumor growth in the K-ras mutant HCT116 colorectal and EGFR/HER2 (neu)-expressing HPAC pancreatic cancer models.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~10 μM
Incubation Time：72 hours
Powder Purity:≥99%
规格
英文别名
7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
CUDC-101
生化机理
CUDC-101 是一种针对 HDAC、表皮生长因子受体和 HER2 的强效多靶点抑制剂，其 IC50 值分别为 4.4 nM、2.4 nM 和 15.7 nM，可抑制 I/II 类 HDAC，但不能抑制 III 类 Sir 型 HDAC。第一阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
组蛋白去乙酰化酶抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
COC1=C(C=C2C(=C1)N=CN=C2NC3=CC=CC(=C3)C#C)OCCCCCCC(=O)NO
分子量
434.49
Reaxy-Rn
13122626
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=13122626&ln=
技术文档
高级数据
产品属性
| ALogP | 4 |
|---|
关联靶点（人）
ERBB2
Tclin
受体酪氨酸蛋白激酶 erbB-2(Receptor tyrosine-protein kinase erbB-2)
(5 活性数据)
EGFR
Tclin
表皮生长因子受体(Epidermal growth factor receptor)
(9 活性数据)
HDAC4
Tclin
组蛋白去乙酰化酶4(Histone deacetylase 4)
(2 活性数据)
HDAC6
Tclin
组蛋白去乙酰化酶6(Histone deacetylase 6)
(2 活性数据)
HDAC1
Tclin
组蛋白去乙酰化酶1(Histone deacetylase 1)
(2 活性数据)
HDAC7
Tclin
组蛋白去乙酰化酶7(Histone deacetylase 7)
(2 活性数据)
HDAC9
Tclin
组蛋白去乙酰化酶9(Histone deacetylase 9)
(2 活性数据)
HDAC2
Tclin
组蛋白去乙酰化酶2(Histone deacetylase 2)
(2 活性数据)
HDAC10
Tclin
组蛋白去乙酰化酶10(Histone deacetylase 10)
(4 活性数据)
HDAC8
Tclin
组蛋白去乙酰化酶8(Histone deacetylase 8)
(2 活性数据)
HDAC5
Tclin
组蛋白去乙酰化酶5(Histone deacetylase 5)
(2 活性数据)
HDAC3
Tclin
组蛋白去乙酰化酶3(Histone deacetylase 3)
(2 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 38 mg/mL (195.6 mM); Ethanol: 38 mg/mL (195.6 mM); Water: Insoluble;
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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