ChemicalBook--->CAS DataBase List--->2764850-23-7

2764850-23-7

2764850-23-7 Structure

2764850-23-7 Structure
IdentificationBack Directory
[Name]

LMTK3 inibitor C28
[CAS]

2764850-23-7
[Synonyms]

LMTK3 inibitor C28
[Molecular Formula]

C18H11F3N4O
[MOL File]

2764850-23-7.mol
[Molecular Weight]

356.31
Chemical PropertiesBack Directory
[storage temp. ]

-10 to -25°C
[solubility ]

Soluble to 50 mM in DMSO and to 20 mM in ethanol
[form ]

Solid
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM),that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM[1].
[Biological Activity]

C28 is a potent lemur tyrosine kinase 3 (LMTK3) inhibitor (IC50 = 67 nM). Disrupts interaction of LMTK3 and HSP90 leading to degradation of LMTK3. Also inhibits CLK, DYRK1α, IRAK4 and HIPK2 (IC50 values are 5 nM, 6 nM, 41 nM and 48 nM respectively). C28 inhibits growth and increases apoptosis in breast cancer cell lines (IC50 = 6.5-14.77 μM) and reduces growth of tumors in xenograft and transgenic mouse models of breast cancer. Also reduces levels of ERα.
[storage]

Store at -20°C
[References]

[1] Agnarelli A, et al. The Inhibitory Properties of a Novel, Selective LMTK3 Kinase Inhibitor. Int J Mol Sci. 2023 Jan 3;24(1):865. DOI:10.3390/ijms24010865
Spectrum DetailBack Directory
[Spectrum Detail]

LMTK3 inibitor C28(2764850-23-7)1HNMR
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