| Bioactivity | HAT-SIL-TG-1&AT is a Janus tyrosine kinase (JAK) inhibitor with antitumor effects. HAT-SIL-TG-1&AT is the hypoxia-activated prodrug, witch inhibits JAK-STAT signaling in tumor tissue. And HAT-SIL-TG-1&AT inhibits HEL cells proliferation and downregulated phosphorylated STAT3/5 under hypoxic conditions[1]. |
| Invitro | HAT-SIL-TG-1&AT 在缺氧条件下可在细胞裂解物中以 TG-1 和 AT 的形式释放[1]。HAT-SIL-TG-1&AT (1-5 μM; 24 h) 抑制 HEL 细胞中 STAT3/5 的磷酸化，在 3 μM 时显着抑制[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | HAT-SIL-TG-1&AT (80 mg/kg；腹腔注射；每天一次，持续 14 天) 在 HEL 肿瘤异种移植雄性 Balb/c 裸鼠中表现出显着的肿瘤生长抑制。HAT-SIL-TG-1&AT 还诱导小鼠细胞凋亡[1]。 Animal Model: |
| Name | HAT-SIL-TG-1&AT |
| Formula | C60H69N17O11S |
| Molar Mass | 1236.36 |
| 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]. Chen X, et al. A JAK tyrosine kinase and pseudokinase Co-inhibition strategy combines enhanced potency and on-demand activation. Eur J Med Chem. 2023 Mar 15;250:115198. |