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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。

化合物

ROS1-IN-1
Cat.No: T61478
Synonym:
Target:
ALK/ROS1-IN-1
Cat.No: T10286
Synonym:
Target: Others
Entrectinib
Cat.No: T3678
Synonym: RXDX-101,恩曲替尼,NMS-E628
Target: Trk receptor, ROS, ALK, Autophagy, ROS Kinase
PF-06463922 acetate
Cat.No: T70060
Synonym:
Target:
APG-2449
Cat.No: T79363
Synonym:
Target: ROS Kinase
Antiproliferative agent-34
Cat.No: T79368
Synonym:
Target: EGFR
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