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HY-13020 GSK1838705A的机制（别名GSK1838705A）：ALK
技术参数：价格和可用性
M.Wt：532.57
分子式：C27H29FN8O3
纯度：> 98％
贮存：贮存在-20℃2年
CAS号：1116235-97-2
溶解性：DMSO≥107mg/mL;水浓度为1mg/mL;乙醇浓度为1mg/mL
生物活性的：
是一种有效的小分子IGF-IR，胰岛素受体和间变性淋巴瘤激酶（ALK）抑制剂的IC50分别为2.0，1.6和0.5海里。 防止来自固体和恶性血液病，包括多发性骨髓瘤，尤因氏肉瘤，并阻碍在体内生长的人类肿瘤异种移植的细胞系在体外增殖。尽管胰岛素受体的抑制作用，对葡萄糖稳态的影响zui小，得到在有效剂量。在0.1和0.3毫克/公斤口服单剂量的导致到35％和65％的预防，IGF-IR的磷酸化，分别，而剂量≥1毫克/公斤，导致完成的配体诱导的IGF-IR的磷酸化的抑制。同时，在30毫克/公斤的剂量，预防持续？化合物注射后的24小时。 也抑制了间变性淋巴瘤激酶（ALK），介导的异常??增长的间变性大细胞淋巴瘤，神经母细胞瘤，非小细胞肺癌的一个子集。由于其抑制ALK中，提供了良好的耐受剂量在体内引起的ALK-依赖性肿瘤完全消退。
HY-13020 (Synonyms GSK 1838705A) Mechanisms:ALK
Technical Data: Price and Availability of
M.Wt: 532.57
Formula: C27H29FN8O3
Purity: >98%
Storage: at -20℃ 2 years
CAS No.: 1116235-97-2
Solubility: DMSO ≥107mg/mL; Water <1mg/mL; Ethanol <1mg/mL
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Biological Activity of :
is a potent small-molecule IGF-IR, the insulin receptor and anaplastic lymphoma kinase (ALK) inhibitor with IC50 of 2.0, 1.6 and 0.5 nM, respectively. prevents the in vitro proliferation of cell lines derived from solid and hematologic malignancies, including multiple myeloma and Ewing’s sarcoma, and retards the growth of human tumor xenografts in vivo. Despite the inhibitory effect of on insulin receptor, minimal effects on glucose homeostasis were obtained at efficacious doses. A single oral dose of at 0.1 and 0.3 mg/kg led to 35% and 65% prevention of IGF-IR phosphorylation, respectively, whereas doses ≥1 mg/kg led to complete inhibition of ligand-induced IGF-IR phosphorylation. Meanwhile, at a dose of 30 mg/kg, prevention was lasted for ?24 hours after compound injection. also suppresses the anaplastic lymphoma kinase (ALK), which mediates the aberrant growth of anaplastic large-cell lymphomas, some neuroblastomas, and a subset of non–small cell lung cancers. Due to its inhibition of ALK, gives rise to complete regression of ALK-dependent tumors in vivo at well-tolerated doses
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