Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3185 |
R112
(E)-Elafibranor |
Syk | Angiogenesis; Tyrosine Kinase/Adaptors |
R112 ((E)-Elafibranor) 是ATP 竞争性的 Syk 激酶抑制剂,它能够抑制Syk 激酶活性,Ki=6 nM,IC50=226 nM。 | |||
T10965 |
DBPR112
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
DBPR112 是一种口服有效的基于氟嘧啶的 EGFR 抑制剂,对 EGFRWT 和 EGFRL858R/T790M 的 IC50 分别为 15 nM 和 48 nM。DBPR112 可以占据 ATP 结合位点。DBPR112 具有显着的抗肿瘤功效。 | |||
T23383 |
SR11237
SR 11237 |
Others; RAR/RXR | Metabolism; Others |
SR11237 是一种泛视黄醇 X 受体 (RXR) 激动剂。 SR11237 导致 RXR/RXR 同源二聚体形成并反式激活包含 RXR 反应元件的报告基因。 | |||
T69498 | DBPR112 HCl | ||
DBPR112 is a potent EGFR inhibitor (IC50=487 nM) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. DBPR112), DBPR112 not only displayed a potent inhibitory activity against EGFRL858R/T790M double mutations but also exhibited tenfold potency better than the third-generation inhibitor, osimertinib,against EGFR and HER2 exon 20 insertion mutations. Overall, pharmacokinetic improvement through lead-to-candidate optimization yielded fourfold oral AUC better that afatinib alon... |