SML2051
LY2109761
≥98% (HPLC)
Sinónimos:
4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]-quinoline, LY-2109761
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About This Item
Fórmula empírica (notación de Hill):
C26H27N5O2
Número de CAS:
Peso molecular:
441.52
Número MDL:
Código UNSPSC:
12352200
En este momento no podemos mostrarle ni los precios ni la disponibilidad
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Ensayo
≥98% (HPLC)
Formulario
powder
color
white to beige
solubilidad
DMSO: 2 mg/mL, clear
temp. de almacenamiento
−20°C
cadena SMILES
[n]21nc(c(c2CCC1)c4c5c(ncc4)cc(cc5)OCCN6CCOCC6)c3ncccc3
InChI
1S/C26H27N5O2/c1-2-9-27-22(4-1)26-25(24-5-3-11-31(24)29-26)21-8-10-28-23-18-19(6-7-20(21)23)33-17-14-30-12-15-32-16-13-30/h1-2,4,6-10,18H,3,5,11-17H2
Clave InChI
IHLVSLOZUHKNMQ-UHFFFAOYSA-N
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]
Orally active, potent and selective TGFβRI/II dual inhibitor with anti-cancer efficacy in in cultures and in vivo.
Código de clase de almacenamiento
11 - Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
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