CUDC-101,1012054-59-9

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YZ剂描述：

产品名称：CUDC-101

产品别名：7-[[4-(3-乙炔基苯基氨基)-7-甲氧基喹唑啉-6-基]氧基]-N-羟基庚酰胺

英文别名：Curis

靶点：EGFR ,HDAC ,HDAC1 ,HDAC6 ,HDAC3

CAS：1012054-59-9

纯度：98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

CUDC-101是一种有效的，多靶点YZ剂，作用于HDAC，EGFR和HER2，IC50分别为4.4 nM， 2.4 nM，和15.7 nM，且YZI/II型HDACs，但是对III型， Sir-type HDACs没有YZ作用。CUDC-101作为特异性YZ一类和二类HDACs家族的YZ剂，不能YZ第三类HDACs家族。CUDC-101还对其他的蛋白激酶包括KDR/VEGFR2， Lyn,，Lck， Abl-1， FGFR-2， Flt-3和 Ret具有微弱的YZ活性。IC50分别是0.85 μM，0.84 μM，5.91 μM，2.89 μM，3.43 μM，1.5 μM和 3.2 μM。

溶解性：DMSO ：16 mg/mL (36.8 mM)

体外研究：

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.

体内研究：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.

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