Ceritinib dihydrochloride NEW
Price | $43 | $58 | $71 |
Package | 5mg | 10mg | 25mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-15 |
Product Details
Product Name: Ceritinib dihydrochloride | CAS No.: 1380575-43-8 |
Purity: 99.99% | Supply Ability: 10g |
Release date: 2024/11/15 |
Product Introduction
Bioactivity
名稱(chēng) | Ceritinib dihydrochloride |
描述 | Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable, 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], demonstrating significant antitumor potency. |
體外活性 | 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]. |
體內(nèi)活性 | Ceritinib 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, Ceritinib 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, Ceritinib 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]. |
存儲(chǔ)條件 | store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | H2O : 5 mg/mL (7.92 mM), Sonication is recommended. DMSO : 95 mg/mL (150.54 mM), Sonication is recommended. |
關(guān)鍵字 | inhibit | Inhibitor | Ceritinib dihydrochloride | ALK tyrosine kinase receptor | LDK378 | LDK 378 | Anaplastic lymphoma kinase (ALK) | LDK378 Dihydrochloride | Cluster of differentiation 246 | IGF-1R | Insulin Receptor | LDK-378 | Ceritinib Dihydrochloride | Ceritinib | Anaplastic lymphoma kinase | CD246 | LDK-378 Dihydrochloride | LDK 378 Dihydrochloride |
相關(guān)產(chǎn)品 | Alectinib hydrochloride | Lorlatinib | SB-431542 | DMH-1 | RepSox | Crizotinib | Ceritinib | LDN-193189 2HCl | HNMPA | A 83-01 | PD173074 | ALK-IN-1 |
相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 激酶抑制劑庫(kù) | 酪氨酸激酶分子庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | FDA 上市激酶抑制劑庫(kù) | FDA 上市藥物庫(kù) | 抗癌上市藥物庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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