SML2051

LY2109761

≥98% (HPLC)

• Synonym(s): 4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]-quinoline, LY-2109761
• Empirical Formula (Hill Notation): C₂₆H₂₇N₅O₂
• CAS Number: 700874-71-1
• Molecular Weight: 441.52
• Número MDL: MFCD12923354

Properties

• ensayo: ≥98% (HPLC)
• formulario: powder
• color: white to beige
• solubilidad: DMSO: 2 mg/mL, clear
• temp. de almacenamiento: −20°C

Description

Aplicación

LY2109761 has been used as an inhibitor of type I and II transforming growth factor-beta (TGFβ) receptors to reduce the phosphorylation of SMAD2 (mothers against decapentaplegic homolog) in HepG2 cells.[1]

Acciones bioquímicas o fisiológicas

LY2109761 is a potent and orally active TGF-β receptor (TGFβR) type I & II dual inhibitor (IC50 = 70 and 322 nM against TGFβRI/ALK5 and TGFβRII autophosphorylation, respectively, with 4 μM ATP), inhibiting Fyn/JNK3/Lck/MKK6/SAPK2α only at much higher concentrations (58-89% inhibition at 20 μM) and exhibiting little or no potency against 37 other kinases (IC50 >20 μM). LY2109761 inhibits 0.25 ng/mL TGFβ-induced NIH/3T3 proliferation in cultures (IC50 = 210 nM; 2-hr pretreatment prior to TGFβ for 24 hrs) and suppresses human MX1 breast carcinoma xenograft tumor growth in mice in vivo (by ∼80% on day 37; 75 mg/kg p.o. bid from day 7 to 20). When administered in combination with gemcitabine (25 mg/kg/day i.p.), LY2109761 (50 mg/kg p.o. bid) is shown to significantly reduce tumor burden and spontaneous abdominal metastases in a murine model of metastatic pancreatic cancer.

LY2109761 suppresses transforming growth factor (TGF)-β1-induced fibroblasts proliferation and collagen synthesis in hypertrophic scar fibroblasts. Therefore, it is used in treating hypertrophic scars.[2]

Safety Information

• Código de clase de almacenamiento: 13 - Non Combustible Solids
• WGK: WGK 3
• Punto de inflamabilidad F: Not applicable
• Punto de inflamabilidad C: Not applicable