Loading... Please wait...

Our Newsletter


LY210976 | TGF-β receptor type I/II inhibitor

  • LY210976.jpg
  • LY210976, 400x400px, png
Price:
$159.00
Catalog #:
C5210-2s
Quantity:


Product Description

LY-2109761 is an orally-bioavailable pyrrolopyrazole inhibitor of the TGF-b1/2 kinase subtypes in Phase I and II clinical studies for malignant malignancies. With Ki potencies of 38 nM and 300 nM, respectively, LY-2109761 has been studied in metastatic pancreatic cancer cells and completely inhibits basal and TGF-b1-stimulated migration and invasion of L3.6pl/GLT cells. [1] LY-2109761 treatment suppresses Smad2 phosphorylation and the Smad-dependent downstream pathway. [2]

LY-2109761 is synergistic with gemcitabine, significantly prolonging survival times and reducing tumor volume and metastatic events. [1] Additionally, LY2109761 enhances radiation response and prolongs survival in glioblastomas. Prolliferation assays displayed a reduction of NMA-23 cell viability and inhibited self-renewal of glioblastoma cancer stem-like cells (CSLC). [3]


Technical information:

Chemical Formula:   C26H27N5O2
CAS #:   700874-71-1
Molecular Weight:   441.52
Purity:   > 98%
Appearance:   Pale Brown
Chemical Name:   7-(2-morpholinoethoxy)-4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline
Solubility:   Up to 100 mM in DMSO
Synonyms:   LY-2109761, LY 2109761, LY2109761

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Melisi et al., LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Mol. Cancer Ther. 2008, 7(4), 829-840. Pubmed ID: 1841379
2. Connolly et al., Complexities of TGF-? targeted cancer therapy. Int. J. Biol. Sci. 2012, 8(7), 964-978. Pubmed ID: 22811618
3. Zhang et al., Blockade of TGF-? signaling by the TGF?R-I kinase inhibitor LY2109761 enhances radiation response and prolongs survival in glioblastoma. Cancer Res. 2011, 71, 7155-7167. Pubmed ID: 22006998

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

Write your own product review

Product Reviews

This product hasn't received any reviews yet. Be the first to review this product!

Add to Wish List

Click the button below to add the LY210976 | TGF-β receptor type I/II inhibitor to your wish list.

You Recently Viewed...