LDK378 dihydrochloride
CAS No. 1380575-43-8
LDK378 dihydrochloride ( Ceritinib dihydrochloride )
产品货号. M22108 CAS No. 1380575-43-8
Ceritinib dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK tyrosine kinase(IC50 of 200 pM), and also inhibits IGF-1R, InsR, and STK22D (IC50 values of 8, 7, and 23 nM, respectively).
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥348 | 有现货 |
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10MG | ¥470 | 有现货 |
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50MG | ¥689 | 有现货 |
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100MG | ¥1021 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称LDK378 dihydrochloride
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述Ceritinib dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK tyrosine kinase(IC50 of 200 pM), and also inhibits IGF-1R, InsR, and STK22D (IC50 values of 8, 7, and 23 nM, respectively).
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产品描述Ceritinib dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK tyrosine kinase(IC50 of 200 pM), and also inhibits IGF-1R, InsR, and STK22D (IC50 values of 8, 7, and 23 nM, respectively), shows great antitumor potencyIn vitro experiments also showed that lipopolysaccharide (LPS)-induced migration of MDSCs was similarly owing to the activation of GRK2 and upregulation of CCR2 by LPS, whereas the treatment with LDK378 partially blocked the LPS-induced phosphorylation of p38 and GRK2 and decreased the expression of CCR2 on the cell surface, therefore leading to the suppression of MDSC migration[1].?LDK378 significantly improved the survival of CLP-induced polymicrobial septic mice, which was paralleled by reduced organ injury, decreased release of inflammatory cytokines and decreased recruitment of MDSCs to the spleen.?Importantly, LDK378 inhibited the migration of MDSCs to the spleen by blocking the CLP-mediated upregulation of CC chemokine receptor 2 (CCR2), a chemokine receptor critical for the recruitment of MDSCs.?Mechanistically, LDK378 treatment blocked the CLP-induced CCR2 upregulation of MDSCs via partially inhibiting the phosphorylation of p38 and G-protein-coupled receptor kinase-2 (GRK2) in bone marrow MDSCs of septic mice.
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同义词Ceritinib dihydrochloride
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通路Angiogenesis
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靶点ALK
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受体ALK
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研究领域Cancer
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适应症Soft Tissue Sarcoma
化学信息
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CAS Number1380575-43-8
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分子量631.06
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分子式C28H38Cl3N5O3S
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纯度>98% (HPLC)
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溶解度H2O:170 mg/mL (269.39 mM); DMSO:95 mg/mL (150.54 mM; Need ultrasonic)
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SMILESCl.Cl.CC(C)Oc1cc(C2CCNCC2)c(C)cc1Nc1ncc(Cl)c(Nc2ccccc2S(=O)(=O)C(C)C)n1
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Hu J , Zhang W , Liu Y , et al. LDK378 inhibits the recruitment of myeloid‐derived suppressor cells to spleen via the p38–GRK2–CCR2 pathway in mice with sepsis[J]. Immunology and Cell Biology, 2019.
产品手册
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