SML3771
LMTK3 inhibitor C28
≥98% (HPLC)
别名:
6-(4-Pyridinyl)-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazine, 6-(Pyridin-4-yl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazine
产品名称
LMTK3 inhibitor C28, ≥98% (HPLC)
InChI
1S/C18H11F3N4O/c19-18(20,21)26-14-3-1-2-13(10-14)16-11-23-17-5-4-15(24-25(16)17)12-6-8-22-9-7-12/h1-11H
InChI key
SFBZOJORTROAIE-UHFFFAOYSA-N
SMILES string
FC(OC1=CC=CC(C2=CN=C3C=CC(C4=CC=NC=C4)=NN32)=C1)(F)F
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Compound C28 is an orally active, potent, ATP-competitive lemur tyrosine kinase 3 (LMTK3) inhibitor with additional inhibitory potency against only 4 other kinases among a panel of 140 (IC50 = 67 nM/LMTK3, 5 nM/CLK, 6 nM/DYRK1α, 48 nM/HIPK2, 41 nM/IRAK4). LMTK3 promotes proteasome-mediated LMTK3 degradation and decreases proliferation of cancer cultures (NCI-60 panel IC50 <10 μM) and displays antitumor efficacy in xenograft and transgenic breast cancer mouse models in vivo (10 mg/mL via dialy p.o.).
Orally active, potent, ATP-competitive lemur tyrosine kinase 3 (LMTK3), CLK, DYRK1α, HIPK2 inhibitor with anticancer efficacy in cultures and in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
The Inhibitory Properties of a Novel, Selective LMTK3 Kinase Inhibitor
International Journal of Molecular Sciences, 24(1), 865-865 (2023)
LMTK3 inhibition affects microtubule stability
Molecular Cancer, 20(1), 53-53 (2021)
Angeliki Ditsiou et al.
Science advances, 6(46) (2020-11-15)
Elucidating signaling driven by lemur tyrosine kinase 3 (LMTK3) could help drug development. Here, we solve the crystal structure of LMTK3 kinase domain to 2.1Å resolution, determine its consensus motif and phosphoproteome, unveiling in vitro and in vivo LMTK3 substrates.
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