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Ceritinib dihydrochloride

Catalog No. T1791L CAS 1380575-43-8

Synonyms: LDK378 dihydrochloride

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Ceritinib dihydrochloride Chemical Structure

Ceritinib dihydrochloride, CAS 1380575-43-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 58.00
25 mg	In stock	$ 71.00
50 mg	In stock	$ 85.00
100 mg	In stock	$ 126.00
1 mL * 10 mM (in DMSO)	In stock	$ 60.00

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Purity: 99.99%

Biological Description

Chemical Properties

Storage & Solubility Information

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
Targets&IC50	ALK:0.2 nM , INSR:7 nM , STK22D:23 nM, IGF-1R:8 nM
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].

Synonyms	LDK378 dihydrochloride
Molecular Weight	631.06
Formula	C28H38Cl3N5O3S
CAS No.	1380575-43-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 5 mg/mL (7.92 mM), Sonication is recommended.

DMSO: 95 mg/mL (150.54 mM), Sonication is recommended.

References and Literature

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. 2. Marsilje TH, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013, Jun 6.

Related compound libraries

This product is contained In the following compound libraries：

FDA-Approved Kinase Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library

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Keywords

Ceritinib dihydrochloride 1380575-43-8 Angiogenesis Tyrosine Kinase/Adaptors IGF-1R ALK inhibit Inhibitor ALK tyrosine kinase receptor LDK378 LDK 378 Anaplastic lymphoma kinase (ALK) LDK378 Dihydrochloride Cluster of differentiation 246 Insulin Receptor LDK-378 LDK378 dihydrochloride Ceritinib Dihydrochloride Ceritinib Anaplastic lymphoma kinase CD246 LDK-378 Dihydrochloride LDK 378 Dihydrochloride inhibitor

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