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ALK
Anaplastic lymphoma kinase (ALK), discovered in 1994, was first described as a fusion partner in the chromosomal translocation in anaplastic large cell lymphoma (ALCL), from which ALK takes its name.Several years passed before the unveiling of the full-length ALK receptor tyrosine kinase (RTK), which consists of an extracellular ligand-binding domain, a transmembrane domain and an intracellular tyrosine kinase domain.The characterisation of downstream ALK signalling events has focused on fusion proteins such as NPM-ALK and EML4-ALK, where kinase activation and signalling is driven by oligomerisation.Wild-type ALK is a membrane-bound receptor.In general, ALK activates multiple signalling pathways, such as the PI3K-AKT, CRKL-C3G, MEKK2/3-MEK5-ERK5, JAKSTAT and MAPK pathways.Activation of adaptor proteins and other cellular proteins, such as PTPN11, Src, FRS2, Shc-GRB2, IRS2, GSK-3a and FAK, has been observed downstream of ALK, indicating roles for alternative pathways. Other reported downstream ALK targets include BIM, p27, cyclin D2, NIPA, RAC1, CDC42, p130CAS, SHP1 and FYVE finger containing phosphoinositide kinase (PIKFYVE).ALK kinase signalling across different tumour types, such as NSCLC, ALCL and neuroblastoma, shares many features, but also exhibits certain differences.
References
1.Hallberg B, Palmer RH. Ann Oncol. 2016 Sep;27 Suppl 3:iii4-iii15.
References
1.Hallberg B, Palmer RH. Ann Oncol. 2016 Sep;27 Suppl 3:iii4-iii15.
Angiogenesis
ALK
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Zotizalkib
产品货号 : M37625
cas no: 2648641-36-3
Zotizalkib (TPX-0131) 是一种有效、选择性、CNS 渗透性和口服活性的野生型 ALK 抑制剂 (IC50 为 1.4 nM) 和 ALK 抗性突变，例如 G1202R (IC50 为 0.3 nM)、L1196M (IC50 为 0.3 nM)。Zotizalkib 具有很强的抗肿瘤活性。
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ALK-IN-27
产品货号 : M37318
cas no: 2739866-40-9
ALK-IN-27 (compound 1) 是一种有效的 ALK 抑制剂。ALK-IN-27 显示出抗肿瘤活性。对于 Ba/F3 CLIP1-LTK 细胞，ALK-IN-27 的 IC50 为 2.7 nM。
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ALK-IN-26
产品货号 : M37104
cas no: 2447607-85-2
ALK-IN-26 (compound 4a) 是 ALK 抑制剂，对 ALK 酪氨酸激酶的 IC50 值为7.0 μM。ALK-IN-26 有良好的药代动力学特性和血脑屏障通透性。ALK-IN-26 能够引起细胞凋亡、自噬和坏死。ALK-IN-26 能够用于胶质母细胞瘤研究。
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INCB-000928
产品货号 : M37084
cas no: 2173389-57-4
Zilurgisertib (INCB-000928; NBU-928) 是一种选择性的 ALK 2 抑制剂，用于研究癌症等疾病。
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Ascrinvacumab
产品货号 : M36744
cas no: 1463459-96-2
Ascrinvacumab (PF-03446962) 是一种人 IgG2 单克隆抗体，靶向 ALK-1。Ascrinvacumab 显示出与人 ALK1 的结合效能，Kd 值为 7 nM。Ascrinvacumab 可用于肝细胞癌 (HCC) 的研究。
