| Bioactivity | Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model[1]. |
| Invitro | Antitumor agent-101 (Compound 27) ( 0-5 μM；48 小时) 抑制 PANC-1 和 MDA-MB-231 细胞的增殖和克隆形成[1]。Antitumor agent-101 ( 0-10 μM；0-96 小时) 以浓度和时间依赖性方式有效降低 PANC-1 和 MDA-MB-231 细胞中的 H3K9me2 水平。 Cell Proliferation Assay[1] Cell Line: |
| In Vivo | Antitumor agent-101 (Compound 27) (2 mg/kg，腹腔注射，每周五天) 通过抑制 G9a/GLP 的甲基转移酶活性来抑制 PANC-1 异种移植肿瘤的生长[1]。Antitumor agent-101 (2 mg/kg，腹腔注射) 显示 Cmax 为 316 ng/mL，平均停留时间 (MRT) 为 0.61 小时[1]。 Animal Model: |
| Name | Antitumor agent-101 |
| CAS | 2848632-52-8 |
| Formula | C26H38N6O3 |
| Molar Mass | 482.62 |
| 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]. Feng Z, et.al. Structure-Based Design and Characterization of the Highly Potent and Selective Covalent Inhibitors Targeting the Lysine Methyltransferases G9a/GLP. J Med Chem. 2023 Jun 22;66(12):8086-8102. |
Antitumor agent-101
CAS: 2848632-52-8 F: C26H38N6O3 W: 482.62
Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5
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