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CUDC-101,HDAC，EGFR和HER2抑制剂, 组蛋白去乙酰化酶抑制剂

规格或纯度: ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
C127191-10mg
 10mg 现货 Stock Image
C127191-25mg
 25mg 现货 Stock Image
C127191-50mg
 50mg 现货 Stock Image
C127191-100mg
 100mg 现货 Stock Image
C127191-250mg
 250mg 期货 Stock Image
大包装询价 添加到收藏夹 比较  SDS中文版  DATASHEET
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基本描述

英文别名 CUDC-101|1012054-59-9|CUDC 101|7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide|CUDC101|7-[[4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yl]oxy]-N-hydroxyheptanamide|CHEMBL598797|1A7Y9MP123|7-[4-(3-ethynylanilino)-7-methoxyq
规格或纯度 ≥98%
英文名称 CUDC-101
生化机理 CUDC-101 inhibits the erlotinib-resistant EGFR mutant T790M althoμgh 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.
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 50mg、10mg、100mg卖完停产，不再备货
产品介绍

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

CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively.
A potent inhibitor of HDACs and receptor tyrosine kinases

产品属性

ALogP 4

名称和标识符

IUPAC Name 7-[4-(3-ethynylanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyheptanamide
INCHI InChI=1S/C24H26N4O4/c1-3-17-9-8-10-18(13-17)27-24-19-14-22(21(31-2)15-20(19)25-16-26-24)32-12-7-5-4-6-11-23(29)28-30/h1,8-10,13-16,30H,4-7,11-12H2,2H3,(H,28,29)(H,25,26,27)
InChi Key PLIVFNIUGLLCEK-UHFFFAOYSA-N
Canonical SMILES COC1=C(C=C2C(=C1)N=CN=C2NC3=CC=CC(=C3)C#C)OCCCCCCC(=O)NO
Isomeric SMILES COC1=C(C=C2C(=C1)N=CN=C2NC3=CC=CC(=C3)C#C)OCCCCCCC(=O)NO
PubChem CID 24756910
分子量 434.49

化学和物理性质

溶解性 DMSO ≥40mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

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参考文献

1. Cai X, Zhai HX, Wang J, Forrester J, Qu H, Yin L, Lai CJ, Bao R, Qian C.  (2010)  Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer..  J Med Chem,  53  (5):  (2000-9).  [PMID:20143778]
2. Shimizu T, LoRusso PM, Papadopoulos KP, Patnaik A, Beeram M, Smith LS, Rasco DW, Mays TA, Chambers G, Ma A et al..  (2014)  Phase I first-in-human study of CUDC-101, a multitargeted inhibitor of HDACs, EGFR, and HER2 in patients with advanced solid tumors..  Clin Cancer Res,  20  (19):  (5032-40).  [PMID:25107918]
3. Galloway TJ, Wirth LJ, Colevas AD, Gilbert J, Bauman JE, Saba NF, Raben D, Mehra R, Ma AW, Atoyan R et al..  (2015)  A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma..  Clin Cancer Res,  21  (7):  (1566-73).  [PMID:25573383]
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