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Ceritinib dihydrochloride

Ceritinib dihydrochloride
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Purity:99.99%
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Ceritinib dihydrochloride

Catalog No. T1791LCas No. 1380575-43-8
Ceritinib dihydrochloride (LDK378 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 potency
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Pack SizePriceAvailabilityQuantity
5 mg$43In Stock
10 mg$58In Stock
25 mg$71In Stock
50 mg$85In Stock
100 mg$126In Stock
1 mL x 10 mM (in DMSO)$60In Stock
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Product Introduction

Bioactivity
Description
Ceritinib dihydrochloride (LDK378 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 potency
In vitro
In 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].
In vivo
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[1].
AliasLDK378 dihydrochloride
Chemical Properties
Molecular Weight631.06
FormulaC28H38Cl3N5O3S
Cas No.1380575-43-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: 5 mg/mL (7.92 mM)
DMSO: 95 mg/mL (150.54 mM)
Solution Preparation Table
DMSO/H2O
1mg5mg10mg50mg
1 mM1.5846 mL7.9232 mL15.8464 mL79.2318 mL
5 mM0.3169 mL1.5846 mL3.1693 mL15.8464 mL
DMSO
1mg5mg10mg50mg
10 mM0.1585 mL0.7923 mL1.5846 mL7.9232 mL
20 mM0.0792 mL0.3962 mL0.7923 mL3.9616 mL
50 mM0.0317 mL0.1585 mL0.3169 mL1.5846 mL
100 mM0.0158 mL0.0792 mL0.1585 mL0.7923 mL

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