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TGF-beta&Smad

LY2109761 (700874-71-1)

LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1/type II kinases (IC50 = 69 nM).1 It has been used to study the role of TGF-β signaling in tumor cell migration and metastasis in pancreatic tumor cell lines

Not Intended for Therapeutic Use. For research use only.

CAS: 700874-71-1 Category

LY2109761 (700874-71-1) Description:

LY2109761 is a novel transforming growth factor beta receptor type I and type II dual inhibitor. The effect of LY2109761 has been evaluated on soft agar growth, migration, invasion using a fibroblast coculture model, and detachment-induced apoptosis (anoikis) by Annexin V flow cytometric analysis. The efficacy of LY2109761 on tumor growth, survival, and reduction of spontaneous metastasis have been evaluated in an orthotopic murine model of metastatic pancreatic cancer expressing both luciferase and green fluorescence proteins (L3.6pl/GLT). In vivo, LY2109761 , in combination with gemcitabine, significantly reduced the tumor burden, prolonged survival, and reduced spontaneous abdominal metastases.

LY2109761 (700874-71-1) Specifications:

Product Name LY2109761
Synonyms LY 2109761; LY-2109761
Chemical Name 4-[2-[4-(2-pyridin-2-yl-5,6-dihydro-4~{H}-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl]oxyethyl]morpholine
Purity >98%
CAS Number 700874-71-1
Molecular Formula C26H27N5O2
Molecular Weight 441.535 g/mol
Monoisotopic Mass 441.216 g/mol
MDL number MFCD12923354
InChIKey IHLVSLOZUHKNMQ-UHFFFAOYSA-N
InChi Code 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
SMILES C1CC2=C(C(=NN2C1)C3=CC=CC=N3)C4=C5C=CC(=CC5=NC=C4)OCCN6CCOCC6
Form powder
Color White to off-white solid
Solubility  Soluble in DMSO
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Shelf life >5 years if stored properly
Handling Protect from air and light
Application A small molecule inhibitor of the TGF-β receptor type 1/type II kinases; TβRI/II kinase inhibitor

 


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RIDADR NONH for all modes of transport

References:

  • LY2109761 inhibits metastasis and enhances chemosensitivity in osteosarcoma MG-63 cells. Ren XF et al. Eur Rev Med Pharmacol Sci. (2015)
  • LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Melisi D et al. Mol Cancer Ther. (2008)
  • LY2109761 enhances cisplatin antitumor activity in ovarian cancer cells. Gao Y et al. Int J Clin Exp Pathol. (2015)

1 review for LY2109761 (700874-71-1)

  1. Cofttek

    Never had such good experience before,The LY2109761 (700874-71-1) is high purity,also customer service is pretty nice !gotta try!!

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