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CUDC-101

CAS No. : 1012054-59-9

MCE 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

作用靶点：EGFR  |  HDAC

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  |  Trichostatin A  |  Gefitinib  |  Trastuzumab  |  Erlotinib  |  Cetuximab  |  AG490  |  4-Phenylbutyric acid  |  Valproic acid  |  Entinostat  |  Sulforaphane  |  Romidepsin  |  Genistein  |  RGFP966  |  AG-1478  |  Tasquinimod  |  Pertuzumab  |  Corin  |  BI-4020  |  Tacedinaline  |  NSC 228155  |  Dacinostat  |  Pelitinib  |  ITSA-1  |  Mubritinib  |  SIS17  |  TX1-85-1

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