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MedChemExpress - Model Luxeptinib -1616428-23-9

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Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells[1][2][3][4].
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chronic lymphocytic leukemia
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hematologic malignancies
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MCE products for research use only. We do not sell to patients.

Luxeptinib

MCE China：Luxeptinib

Brand：MedChemExpress (MCE)

Cat. No.HY-139535

CAS：1616428-23-9

Synonyms：CG-806

Purity：99.30%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells.

In Vitro：Luxeptinib (MEC-1 CLL cells; 0.1~10 µM; 72 hours) inhibits cells proliferation with an IC50 of 32 nM[1]. Luxeptinib inhibits BCR signaling-induced phosphorylation of BTK, PLCg2, AKT, ERK1/2, S6 ribosomal protein and strongly suppresses SYK phosphorylation in primary chronic lymphocytic leukemia (CLL) cells[1]. Luxeptinib (MV4-11 cells; 500 pM; 1 hour) completely inhibits phosphorylation of FLT3 and STAT5[2].

IC50 & Target：Pan-FLT3/Pan-BTK[1] In Vitro Luxeptinib (MEC-1 CLL cells; 0.1~10 µM; 72 hours) inhibits cells proliferation with an IC50 of 32 nM[1]. Luxeptinib inhibits BCR signaling-induced phosphorylation of BTK, PLCg2, AKT, ERK1/2, S6 ribosomal protein and strongly suppresses SYK phosphorylation in primary chronic lymphocytic leukemia (CLL) cells[1]. Luxeptinib (MV4-11 cells; 500 pM; 1 hour) completely inhibits phosphorylation of FLT3 and STAT5[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Luxeptinib Related Antibodies Cell Proliferation Assay[1] Cell Line: MEC-1 CLL cells

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References：

[1]. Ekaterina Kim MS, et al. CG-806, a First-in-Class Pan-FLT3/Pan-BTK Inhibitor, Exhibits Broad Signaling Inhibition in Chronic Lymphocytic Leukemia Cells. bloodjournal Blood blood (2019). 134 (Supplement_1) : 3051.

[2]. Abstract 44: CG′806, a first-in-class FLT3/BTK inhibitor, exhibits potent activity against AML patient samples with mutant or wild type FLT3, as well as other hematologic malignancy subtypes

[3]. Guopan Yu,et al.CG '806, a Novel Pan-FLT3/BTK Multi-Kinase Inhibitor, Induces Cell Cycle Arrest, Apoptosis or Autophagy in AML Cells Depending on FLT3 Mutation Status. Blood blood (2017).130 (Suppl_1) : 462

[4]. Aptose Biosciences to Present CG’806 Data at AACR Hematologic Malignancies Meeting

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。