Bioactivity | LY900009 is a potent and orally active, First-in-class inhibitor of Notch signaling via selective inhibition of the γ-secretase protein (GSI). LY900009 inhibited Notch signalling in tumor cell lines and endothelial cells (IC50 range: 0.005-20 nM). LY900009 can be used for advanced cancer research[1]. |
In Vivo | 在大鼠模型中,LY900009 (口服灌胃;3 mg/kg;单剂量) 通过形成渗漏脉管系统抑制血管生成,并在 Notch 依赖性肿瘤模型中导致肿瘤消退[1]。 |
Name | LY900009 |
CAS | 209984-68-9 |
Formula | C23H27N3O4 |
Molar Mass | 409.48 |
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]. Shubham Pant, et al. A first-in-human phase I study of the oral Notch inhibitor, LY900009, in patients with advanced cancer. Eur J Cancer. 2016 Mar;56:1-9. |