SML2051
LY2109761
≥98% (HPLC)
Synonim(y):
4-[5,6-Dihydro-2-(2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-7-[2-(4-morpholinyl)ethoxy]-quinoline, LY-2109761
Zaloguj sięWyświetlanie cen organizacyjnych i kontraktowych
About This Item
Wzór empiryczny (zapis Hilla):
C26H27N5O2
Numer CAS:
Masa cząsteczkowa:
441.52
Numer MDL:
Kod UNSPSC:
12352200
Polecane produkty
Próba
≥98% (HPLC)
Postać
powder
kolor
white to beige
rozpuszczalność
DMSO: 2 mg/mL, clear
temp. przechowywania
−20°C
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
Klucz InChI
IHLVSLOZUHKNMQ-UHFFFAOYSA-N
Zastosowanie
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.
Działania biochem./fizjol.
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.
This page may contain text that has been machine translated.
Kod klasy składowania
11 - Combustible Solids
Klasa zagrożenia wodnego (WGK)
WGK 3
Temperatura zapłonu (°F)
Not applicable
Temperatura zapłonu (°C)
Not applicable
Certyfikaty analizy (CoA)
Poszukaj Certyfikaty analizy (CoA), wpisując numer partii/serii produktów. Numery serii i partii można znaleźć na etykiecie produktu po słowach „seria” lub „partia”.
Masz już ten produkt?
Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.
Jia Fang et al.
Scientific reports, 7, 43851-43851 (2017-03-04)
Previous studies have shown that CD61 (integrin-β3) promotes the differentiation of human umbilical cord mesenchymal stem cells (hUC-MSCs) into germ-like cells. However, the mechanism remains unclear. In this study, we showed that overexpression of CD61 in canine adipose-derived mesenchymal stem
Markus D Lacher et al.
Cancer research, 66(3), 1648-1657 (2006-02-03)
Expression of the Coxsackie and Adenovirus Receptor (CAR) is frequently reduced in carcinomas, resulting in decreased susceptibility of such tumors to infection with therapeutic adenoviruses. Because CAR participates physiologically in the formation of tight-junction protein complexes, we examined whether molecular
Chen Zhao et al.
Science (New York, N.Y.), 356(6335) (2017-03-11)
The stem cell niche is a complex local signaling microenvironment that sustains stem cell activity during organ maintenance and regeneration. The mammary gland niche must support its associated stem cells while also responding to systemic hormonal regulation that triggers pubertal
Davide Melisi et al.
Molecular cancer therapeutics, 7(4), 829-840 (2008-04-17)
Most pancreatic cancer patients present with inoperable disease or develop metastases after surgery. Conventional therapies are usually ineffective in treating metastatic disease. It is evident that novel therapies remain to be developed. Transforming growth factor beta (TGF-beta) plays a key
Xuan Liu et al.
BioMed research international, 2017, 2613198-2613198 (2017-03-17)
JPJD was an ideal alternative traditional Chinese medicine compound in the prevention and treatment of CRC, but its underlying mechanisms has not been fully elucidated. In this study, we demonstrated in vitro that TGF-β-induced EMT promoted the invasion and metastasis
Nasz zespół naukowców ma doświadczenie we wszystkich obszarach badań, w tym w naukach przyrodniczych, materiałoznawstwie, syntezie chemicznej, chromatografii, analityce i wielu innych dziedzinach.
Skontaktuj się z zespołem ds. pomocy technicznej