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Cat. No.	Product Name	Target	Signaling Pathways
T3059	ALK-IN-1 AP26113,Brigatinib,AP26113-analog	EGFR; IGF-1R; ALK	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	ALK-IN-1 (AP26113) 是一种高效的、选择性的 ALK 激酶抑制剂。
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).
T72931	TRK/ALK-IN-1
	TRK/ALK-IN-1 是一种有效的 TRK 和 ALK 双重抑制剂。TRK/ALK-IN-1 在酶促测定中与抗增殖活性非常吻合，对 TRKA、ALKIC50值分别为 2.2、9.3 和 38 nM< sup>WT 和 ALKL1196M。TRK/ALK-IN-1具有研究癌症疾病的潜力。
T79392	ALK/EGFR-IN-1	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	ALK/EGFR-IN-1（Compound 8l）是一款高效的ALK/EGFR双重抑制剂，专门针对EGFR和ALK的磷酸化过程进行抑制。该化合物对H1975细胞内的EGFRL858R/T790M突变体和BaF3细胞内的EML4-ALK表达类型表现出优异的抑制活性，其IC50值分别为4.3 nM和3.6 nM。ALK/EGFR-IN-1用于非小细胞肺癌（NSCLC）的科学研究具有重要应用价值。
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。
T83146	ALK-IN-27
	ALK-IN-27（化合物1）是一种有效的ALK抑制剂，展现出抗肿瘤活性。在Ba/F3 CLIP1-LTK细胞中，ALK-IN-27的IC50为2.7 nM。
T61443	Trk-IN-7
	Trk-IN-7 (compound I-6) is a highly potent inhibitor of TRK, exhibiting IC50 values ranging from 0.25-10 nM for TRKA, TRKB, and TRKC, respectively. In addition, Trk-IN-7 demonstrates notable inhibition against EML4-ALK (IC50 <15 nM), as well as ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC50 = 5-50 nM) [1].
T79393	ALK/EGFR-IN-2
	ALK/EGFR-IN-2 是一种高效的 ALK 和 EGFR 双重抑制剂，能够诱导癌细胞凋亡及 G0/G1 细胞周期停滞。此化合物在 H1975、PC9 和 Baf3-EML4-ALK 癌熙胞株的增殖抑制实验中，其 IC50 值分别为0.0034、0.0065 和 0.0018 μM，表明其对这些癌熙胞系具有显著的抑制作用。
T74522	ALK-IN-21
	ALK-IN-21（Compound B10）是一款高效的ALK抑制剂，其针对ALKWT、ALKL1196M和ALKG1202R的IC50值依次为4.59 nM、2.07 nM和5.95 nM。该化合物能显著抑制ALK阳性的Karpas299与H2228细胞系的增殖，均展现出0.07 μM的IC50值。ALK-IN-21主要用于研究间变性大细胞淋巴瘤。
T79394	ALK/EGFR-IN-3
	ALK/EGFR-IN-3 为ALK与EGFR的强效双重抑制剂，有效遏制H1975、PC9以及Baf3-EML4-ALK癌细胞系的生长，其IC50值分别为0.1360、0.0332及0.0339 μM。
T83856	AP-1
	AP-1是一种微型化的蛋白质水解靶向嵌合体（PROTAC），由吲哚美辛（±）连接的间变性淋巴瘤激酶（ALK）配体和E3泛素连接酶配体通过超短连接器相连。在10至300 nM浓度范围内使用时，AP-1能高效降解Karpas-299细胞中高表达的ALK融合蛋白NPM-ALK，此效应可被蛋白酶体抑制剂MG-132阻断。它还能降解在SN-N-SH和NCI H3122细胞中表达的ALK融合蛋白EML4-ALK及含有苯丙氨酸至亮氨酸替换突变（ALKF1174L）的ALK。AP-1对依赖ALK的Karpas-299细胞具有细胞毒性（IC50 = 0.1265 nM），但对非ALK依赖的THP-1细胞无细胞毒性（IC50 = 2,704 nM）。在给药剂量为25, 50, 和100 mg/kg时，能减小NCI H3122小鼠移植瘤模型中的肿瘤体积。
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).
T38584	ALK-IN-12
	ALK-IN-12 is a highly potent and orally active inhibitor of anaplastic lymphoma kinase (ALK), demonstrating an exceptional IC50 value of 0.18 nM. Additionally, ALK-IN-12 displays inhibitory activity against insulin-like growth factor 1 receptor (IGF1R) and insulin receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. Notably, its antitumor effects have been observed, making it a promising compound for targeted cancer therapy.
T62613	ALK5-IN-26
	ALK5-IN-26 (EX-22) 是一种 ALK(Activin receptor-like kinase) 的抑制剂。ALK5-IN-26 对 ALK5 (IC50≤1 nM) 具有抑制作用。ALK5-IN-26 能够用于研究癌症。
T37585	Ensartinib
	Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring N...
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。
T61872	Trk-IN-10
	Trk-IN-10 (Compound 14j) is a highly effective inhibitor of TRK, with an IC50 of 0.86 nM against TrkA and 6.92 nM against TrkA G595R. As an RTK, Trk plays a crucial role as a drug target in solid tumors. Trk-IN-10 (IC50 = 350 nM against ALK) demonstrates superior selectivity in inhibiting Trk, which has potential implications for toxicity reduction [1].

化合物

ALK-IN-1

Cat.No: T3059

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