| 货号 | 21429-100mg |
| 描述 | KX2-391 is a highly selective and potent Src kinase inhibitor with strong anticancer properties that binds specifically to the substrate binding site of Src kinase (IC50 = 20 nM for Src kinase autophosphorylation; IC50 = 100 nM and 25 nM in human tumor cells in the presence and absence of human plasma, respectively; GI50 = 9, 13, 26, and 60 nM in HuH7, PLC/PRF/5, Hep 3B, and Hep G2 hepatocellular carcinoma cell lines, respectively).1,2,3 It does not affect PDGFR, EGFR, JAK1, JAK2, Lck, or ZAP70.4,5 In ERα positive breast cancer cells, KX2-391 induced apoptosis through activation of caspases 6, 7, 8, and 9.4 It can also induce p53 expression and stimulate caspase-3 and PARP cleavage in vitro.1 KX2-391 has been through Phase I and Phase II clinical trials for patients with acute myeloid leukemia, solid tumors, prostate cancers, and lymphoma.1,3 A Phase II clinical trial is ongoing for a formulation of KX2-391 in ointment form for patients with actinic keratosis, a disorder of the skin that can lead to squamous cell carcinoma. |
| 别名 | KX 01; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Naing, A.,Cohen, R.,Dy, G.K., et al. A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignancies. Invest New Drugs 31(4), 967-973 (2013). 2.Lau, G.M.,Lau, G.M.,Yu, G.-L., et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig. Dis. Sci. 54(7), 1465-1474 (2009). 3.Antonarakis, E.S.,Heath, E.I.,Posadas, E.M., et al. A phase 2 study of KX2-391, an oral inhibitor of Src kinase and tubulin polymerization, in men with bone-metastatic castration-resistant prostate cancer. Cancer Chemother. Pharmacol. 71(4), 883-892 (2013). 4.Anbalagan, M.,Carrier, L.,Glodowski, S., et al. KX-01, a novel Src kinase inhibitor directed toward the peptide substrate site, synergizes with tamoxifen in estrogen receptor α positive breast cancer. Breast Cancer Res. Treat. 132(2), 391-409 (2012). 5.Fallah-Tafti, A.,Foroumadi, A.,Tiwari, R., et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur. J. Med. Chem. 46(10), 4853-4858 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 431.5 |
| 分子式 | C26H29N3O3 |
| CAS号 | 897016-82-9 |
| 稳定性 | ≥ 2 years |
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