| Description | INCB3619 is a selective and potent inhibitor of ADAM with antitumour effects, inhibiting ADAM10, ADAM17, MMP12 and MMP15. |
| In vitro | 双重 ADAM 抑制剂 INCB3619 抑制 heregulin 切割，IC50值为0.24μM[1]。用不同浓度的吉非替尼和 INCB3619（2-10 µM）处理无血清培养基中的 A549 细胞 96 h，发现 INCB3619 使 A549 细胞对吉非替尼敏感[1]。 |
| In vivo | INCB3619 使用 ALZET 渗透泵以 30 或 60 mg/kg/d 的剂量皮下给药，持续 14 天，结果显示 ADAM 抑制剂 INCB3619 抑制吉非替尼耐药的 HER3 自分泌机制，在体内具有抗肿瘤活性，并使肿瘤对化疗药物敏感[1]。 |
| Target activity | Heregulin:0.24 μM |
| Synonyms | INCB-3619, INCB 3619 |
| molecular weight | 413.47 |
| Molecular formula | C22H27N3O5 |
| CAS | 791826-72-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Bin-Bing S Zhou, et al. Targeting ADAM-mediated ligand cleavage to inhibit HER3 and EGFR pathways in non-small cell lung cancer. Cancer Cell. 2006 Jul;10(1):39-50. 2. Wiernik A, Foley B, Zhang B, Verneris MR, Warlick E, Gleason MK, Ross JA, Luo X, Weisdorf DJ, Walcheck B, Vallera DA, Miller JS. Targeting natural killer cells to acute myeloid leukemia in vitro with a CD16 x 33 bispecific killer cell engager and ADAM17 inhibition. Clin Cancer Res. 2013 Jul 15;19(14):3844-55. doi: 10.1158/1078-0432.CCR-13-0505. PubMed PMID: 23690482; PubMed Central PMCID: PMC3715574. 3. Floyd DH, Kefas B, Seleverstov O, Mykhaylyk O, Dominguez C, Comeau L, Plank C, Purow B. Alpha-secretase inhibition reduces human glioblastoma stem cell growth in vitro and in vivo by inhibiting Notch. Neuro Oncol. 2012 Oct;14(10):1215-26. PubMed PMID: 22962413; PubMed Central PMCID: PMC3452340. 4. Witters L, Scherle P, Friedman S, Fridman J, Caulder E, Newton R, Lipton A. Synergistic inhibition with a dual epidermal growth factor receptor/HER-2/neu tyrosine kinase inhibitor and a disintegrin and metalloprotease inhibitor. Cancer Res. 2008 Sep 1;68(17):7083-9. doi: 10.1158/0008-5472.CAN-08-0739. PubMed PMID: 18757423. |