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
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About This Item
Empirical Formula (Hill Notation):
C26H27N5O2
CAS Number:
Molecular Weight:
441.52
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.21
SMILES string
[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
InChI key
IHLVSLOZUHKNMQ-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Related Categories
Application
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.
Biochem/physiol Actions
Orally active, potent and selective TGFβRI/II dual inhibitor with anti-cancer efficacy in in cultures and in vivo.
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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
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
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
Yang Jin et al.
Oncotarget, 8(16), 26090-26099 (2017-02-18)
To confirm that PlncRNA-1 regulates the cell cycle in prostate cancer cells and induces epithelial-mesenchymal transition (EMT) in prostate cancer through the TGF-β1 pathway. PlncRNA-1 and TGF-β1 expression levels were significantly higher in prostate cancer tissues than in normal prostate
Guo Wei et al.
Archives of dermatological research, 310(8), 615-623 (2018-07-27)
Hypertrophic scars (HS) are fibro-hyperproliferative dermal lesions with effusive continuous accumulation of extracellular matrix components, particularly collagen. They usually occur after dermal injury in genetically susceptible individuals and cause both physical and psychological distress for the affected individuals. Transforming growth
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