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CAS No. : 1012054-59-9
MCE 国际站:CUDC-101
产品活性:CUDC-101 是一种高效的 HDAC、EGFR 和 HER2 抑制剂,对应的 IC50 值分别为 4.4、2.4 和 15.7 nM。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK | Cell Cycle/DNA Damage | Epigenetics
In Vitro: CUDC-101 inhibits both class I and class II HDACs, but not class III, Sir-type HDACs. CUDC-101 displays broad antiproliferative activity in many human cancer cell types. CUDC-101 is a potent and selective HDAC, EGFR, and HER2 inhibitor with only weak inhibition of the following protein kinases (IC50): KDR (VEGFR2) (849 nM), Src (11000 nM), Lyn (840 nM), Lck (5910 nM), Abl-1 (2890 nM), FGFR-2 (3430 nM), Flt-3 (1500 nM), and Ret (3200 nM). CUDC-101 (300 nM) inhibits both the full length AR (flAR) and the AR variant AR-V7. CUDC-101 is the most active agent in all three ATC cell lines screened for inhibitors of EGFR and HDACs, with half-maximal inhibitory concentration (IC50) at 0.15 μM for 8505c, and 1.66 μM for both C-643 and SW-1736 cells. CUDC-101 inhibits cancer cell migration and modulates epithelial-mesenchymal transition marker expression in ATC cells. CUDC-101 also inhibits HDAC and MAPK pathway, induces p21, and decreases survivin and XIAP expression in ATC cells. CUDC-101 (1 μM) increases the acetylation of p53 and α-tubulin, nonhistone substrates of HDAC, in treated cancer cells. CUDC-101 modulates RTK activity and expression and exhibits immediate and stable inhibition of RTK and downstream Akt signaling.
In Vivo: CUDC-101 (120 mg/kg, iv, daily) induces tumor regression in the Hep-G2 liver cancer model and is more efficacious than erlotinib at its maximum tolerated dose (MTD). In the erlotinib-resistant A549 NSCLC xenograft model, CUDC-101 (120 mg/kg) shows potent inhibition of tumor growth. In the erlotinib-sensitive H358 NSCLC models, CUDC-101 (15, 30, 60 mg/kg, i.v.) inhibits tumor growth in a dose-dependent manner. CUDC-101 (120 mg/kg) causes 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. CUDC-101 (120 mg/kg) also inhibits tumor growth in the K-ras mutant HCT116 colorectal and EGFR/HER2 (neu)-expressing HPAC pancreatic cancer models. In an in vivo mouse model of metastatic ATC, CUDC-101 inhibits tumor growth and metastases, and significantly prolongs survival. CUDC-101 (120 mg/kg) is effective against a broad range of tumor types in xenograft models.
相关产品:Covalent Screening Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Covalent Screening Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Anti-Hepatitis C Virus Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Osteogenesis Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | YF479 | EGFR/HER2/CDK9-IN-2 | Lapatinib ditosylate | BMS-690514 | Erlotinib-d6 hydrochloride | EGFR/CDK2-IN-1 | JBJ-04-125-02 | KD 5170 | EGFR-IN-22 | HDAC-IN-48 | EGFR-IN-34 | Epertinib | Ponezumab | Remetinostat | HDAC-IN-30 | Erlotinib Hydrochloride | EGFR-IN-36 | HDAC-IN-52 | EGFR-IN-62 | Genistein | Panitumumab (anti-EGFR) | Lirafugratinib | Lapatinib-d7 dihydrochloride | CG347B | (E/Z)-CP-724714 | Psammaplin A | TAS0728 | Rezivertinib | JPS016 | HDAC6-IN-9
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