1616428-23-9

1616428-23-9 structure

Name: Luxeptinib
Chemical Name: 1-{3-Fluoro-4-[7-(4-methyl-1H-imidazol-2-yl)-1-oxo-2,3-dihydro-1H-isoindol-4-yl]phenyl}-3-(2,4,6-trifluorophenyl)urea
CAS Number: 1616428-23-9
Molecular Formula: C₂₅H₁₇F₄N₅O₂
Molecular Weight: 495.43
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Btk
Create Date: 2021-12-20 09:31:02
Modify Date: 2024-01-14 18:05:28
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].

Name	1-{3-Fluoro-4-[7-(4-methyl-1H-imidazol-2-yl)-1-oxo-2,3-dihydro-1H-isoindol-4-yl]phenyl}-3-(2,4,6-trifluorophenyl)urea
Synonyms	1-{3-Fluoro-4-[7-(4-methyl-1H-imidazol-2-yl)-1-oxo-2,3-dihydro-1H-isoindol-4-yl]phenyl}-3-(2,4,6-trifluorophenyl)urea Urea, N-[4-[2,3-dihydro-7-(4-methyl-1H-imidazol-2-yl)-1-oxo-1H-isoindol-4-yl]-3-fluorophenyl]-N'-(2,4,6-trifluorophenyl)-

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[1][2][3][4].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3 Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk
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]. Cell Proliferation Assay[1] Cell Line: MEC-1 CLL cells Concentration: 0.1~10 µM Incubation Time: 72 hours Result: Inhibited cells proliferation with an IC50 of 32 nM.
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

Density	1.5±0.1 g/cm3
Boiling Point	663.8±55.0 °C at 760 mmHg
Molecular Formula	C₂₅H₁₇F₄N₅O₂
Molecular Weight	495.43
Flash Point	355.3±31.5 °C
Exact Mass	495.131836
LogP	4.44
Vapour Pressure	0.0±2.0 mmHg at 25°C
Index of Refraction	1.674
Storage condition	2-8°C

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