Bioactivity | ADTL-EI1712 is a potent, orally active, and selective dual-target inhibitor of ERK1 and ERK5, inhibition rates of ERK1/5 at 1 μM are 93.54% and 89.35%, respectively. ADTL-EI1712 can induce regulated cell death, a form of cell death that relies on the activation of genetically encoded machinery, to overcome compensatory mechanism in specific cancer cells in vitro and in vivo[1]. |
Invitro | ADTL-EI1712 对 HL-60、MKN-74 和 HeLa 细胞具有抗增殖活性,IC50 值分别为 1.26+0.57、2.55+0.66、>50 μM[1]。ADTL-EI1712 (0.5 μM, 24 h) 可在 MKN-74 细胞中诱导受调节的细胞死亡并伴有自噬 (autophagy)[1]。 0 --> ADTL-EI1712 相关抗体: |
In Vivo | ADTL-EI1712 (50 mg/kg,口服,每天一次,持续16天) 显著抑制 HL-60 和 MKN-74 细胞异种移植小鼠模型中的肿瘤体积,而 HeLa 细胞组的抗肿瘤作用要弱得多[1]。 |
Name | ADTL-EI1712 |
CAS | 2414916-45-1 |
Formula | C22H18Cl2N4O2S2 |
Molar Mass | 505.44 |
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]. Wang G, et al. Discovery of a Novel Dual-Target Inhibitor of ERK1 and ERK5 That Induces Regulated Cell Death to Overcome Compensatory Mechanism in Specific Tumor Types. J Med Chem. 2020 Apr 23;63(8):3976-3995. |