Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T61478 | ROS1-IN-1 | ||
ROS1-IN-1 (Compound 31) is a highly effective and specific inhibitor of the ROS1 kinase, displaying a remarkable inhibitory concentration (IC 50) of 0.097 μM [1]. | |||
T10286 |
ALK/ROS1-IN-1
|
Others | Others |
ALK/ROS1-IN-1 is a potent and selective anti-crizotinib-resistant ALK/ROS1 dual inhibitor (IC50s: 0.530 μM and 0.174 μM for ROS1 and ALK enzyme). | |||
T3678 |
Entrectinib
RXDX-101,恩曲替尼,NMS-E628 |
Trk receptor; ROS; ALK; Autophagy; ROS Kinase | Angiogenesis; Autophagy; Immunology/Inflammation; Tyrosine Kinase/Adaptors |
Entrectinib (RXDX-101) 是一种可口服的 Trk、ROS1和 ALK 抑制剂,具有抗肿瘤和中枢神经活性,抑制 TrkA、TrkB、TrkC、ROS1 和 ALK 的 IC50值分别为 1、3、5、12 和 7 nM。 | |||
T70060 |
PF-06463922 acetate
|
||
PF-06463922 acetate is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC). | |||
T79363 | APG-2449 | ROS Kinase | Tyrosine Kinase/Adaptors |
APG-2449为口服活性的ALK/ROS1/FAK抑制剂,在非小细胞肺癌(NSCLC)的小鼠模型中显示出显著的抗肿瘤效果。 | |||
T79368 | Antiproliferative agent-34 | EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Antiproliferative agent-34 (Compound A14) 是一种多激酶抑制剂,能有效抑制包括EGFRL858R/T790M在内的特定EGFR基因变异形式,IC50为177 nM,对EGFRWT则为1567 nM。它还能抑制JAK2、ROS1、FLT3、FLT4和PDGFRα的活性,其IC50分别为30.93、106.90、108.00、226.60和42.53 nM。在正常氧气环境中,Antiproliferative agent-34对H1975和HCC827细胞株的抑制IC50值低于40 nM,而在低氧环境下,其抑制效能增强4至6倍,IC50值降至低于10 nM。 |