HY-13020 GSK1838705A的機制（別名GSK1838705A）：ALK
GSK1838705A技術(shù)參數(shù)：價格和可用性GSK1838705A
GSK1838705A M.Wt：532.57
GSK1838705A分子式：C27H29FN8O3
GSK1838705A純度：> 98％
GSK1838705A貯存：貯存在-20℃2年
GSK1838705A CAS號：1116235-97-2
GSK1838705A溶解性：DMSO≥107mg/mL;水濃度為1mg/mL;乙醇濃度為1mg/mL
生物活性的GSK1838705A：
GSK1838705A是一種有效的小分子IGF-IR，胰島素受體和間變性**瘤激酶（ALK）抑制劑的IC50分別為2.0，1.6和0.5海里。 GSK1838705A防止來自固體和惡性血液病，包括多發(fā)性骨髓瘤，尤因氏肉瘤，并阻礙在體內(nèi)生長的人類腫瘤異種移植的細胞系在體外增殖。盡管胰島素受體GSK1838705A的抑制作用，對葡萄糖穩(wěn)態(tài)的影響*小，得到在有效劑量。在0.1和0.3毫克/公斤口服單劑量的GSK1838705A導(dǎo)致到35％和65％的預(yù)防，IGF-IR的磷酸化，分別，而劑量≥1毫克/公斤，導(dǎo)致完成的配體誘導(dǎo)的IGF-IR的磷酸化的抑制。同時，在30毫克/公斤的劑量，預(yù)防持續(xù)？化合物注射后的24小時。 GSK1838705A也抑制了間變性**瘤激酶（ALK），介導(dǎo)的異常??增長的間變性大細胞**瘤，神經(jīng)母細胞瘤，非小細胞肺癌的一個子集。由于其抑制ALK中，GSK1838705A提供了良好的耐受劑量在體內(nèi)引起的ALK-依賴性腫瘤完全消退。
HY-13020 GSK1838705A (Synonyms GSK 1838705A) Mechanisms:ALK
GSK1838705A Technical Data: Price and Availability of GSK1838705A
GSK1838705A M.Wt: 532.57
GSK1838705A Formula: C27H29FN8O3
GSK1838705A Purity: >98%
GSK1838705A Storage: at -20℃ 2 years
GSK1838705A CAS No.: 1116235-97-2
GSK1838705A Solubility: DMSO ≥107mg/mL; Water <1mg/mL; Ethanol <1mg/mL
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Biological Activity of GSK1838705A:
GSK1838705A 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. GSK1838705A 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 GSK1838705A on insulin receptor, minimal effects on glucose homeostasis were obtained at efficacious doses. A single oral dose of GSK1838705A 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. GSK1838705A 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, GSK1838705A gives rise to complete regression of ALK-dependent tumors in vivo at well-tolerated doses