SML3771

LMTK3 inhibitor C28

≥98% (HPLC)

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₁₈H₁₁F₃N₄O
• CAS Number: 2764850-23-7
• Molecular Weight: 356.30
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (Warmed)
• storage temp.: -10 to -25°C
• SMILES string: FC(OC1=CC=CC(C2=CN=C3C=CC(C4=CC=NC=C4)=NN32)=C1)(F)F
• 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

Description

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable