| Bioactivity | TH-Z835 is a mutant selective KRAS (G12D) inhibitor with an IC50 of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange[1]. |
| Invitro | TH-Z835 降低 PANC-1 细胞中的 pERK 水平，IC50 值小于 2.5 μM[1]。TH-Z835 在其他非 G12D 突变癌细胞系（包括 4T1 (KRAS(WT))、MIA PaCa-2 (KRAS(G12C))、CFPAC-1 (KRAS(G12V)) 和 HCT116 (KRAS(G13D)) 细胞中具有抗增殖作用，降低 pERK 和 pAKT 水平并诱导细胞凋亡，表明存在脱靶效应[1]。 |
| In Vivo | TH-Z835（10mg/kg；腹膜内注射）可减少 C57BL/6 小鼠模型中的肿瘤体积。TH-Z835 在体内诱导细胞凋亡并抑制 MAPK 信号传导[1]。 |
| Name | TH-Z835 |
| CAS | 2766209-50-9 |
| Formula | C30H38N6O |
| Molar Mass | 498.66 |
| 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]. Mao Z, et al. KRAS(G12D) can be targeted by potent inhibitors via formation of salt bridge. Cell Discov. 2022 Jan 25;8(1):5. |