Bioactivity | Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KDSPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells[1]. |
Target | Nur77 |
Invitro | Nur77 antagonist 1(Compound ja) 对来自不同组织的肿瘤细胞具有选择性,与人类正常乳腺细胞系相比(MCF-10A 的 IC50为48.01 ± 2.86),ja对所有测试的TNBC细胞系(MDA-MB-231, HCC-1806和BT549的IC50分别为0.40 ± 0.03、0.38 ± 0.08和2.12 ± 0.15)具有高度选择性的抗增殖活性[1]。Nur77 antagonist 1 (0-2 μM, 6 h) 以Nur77依赖性方式诱导MDA-MB-231-sictr细胞凋亡[1]。Nur77 antagonist 1 (0-5 μM, 6 h) 通过介导MDA-MB-231细胞中的TP53磷酸化途径,诱导Nur77依赖性细胞周期阻滞和凋亡[1]。 0 --> Nur77 antagonist 1 相关抗体: Western Blot Analysis[1] Cell Line: |
In Vivo | Nur77 antagonist 1(Compound ja) (10 mg/kg, 腹腔注射) 在乳腺癌MDA-MB-231异种移植裸鼠模型中具有良好的抗肿瘤效果和良好的体内耐受性[1]。Nur77 antagonist 1 (1.25-5 μM) 在斑马鱼胚胎模型中具有良好的体内安全性[1]。 Animal Model: |
Name | Nur77 antagonist 1 |
CAS | 2378780-25-5 |
Formula | C25H32N8OS |
Molar Mass | 492.64 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Qin J, et al. Discovery of 5-(Pyrimidin-2-ylamino)-1H-indole-2-carboxamide Derivatives as Nur77 Modulators with Selective and Potent Activity Against Triple-Negative Breast Cancer. J Med Chem. 2023 Nov 20. |