Home Other Building Blocks 700874-71-1
700874-71-1,MFCD12923354
Catalog No.:AA00FBGG

700874-71-1 | LY2109761

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
98%
in stock  
$11.00   $8.00
- +
2mg
98%
in stock  
$15.00   $11.00
- +
5mg
98%
in stock  
$28.00   $20.00
- +
10mg
98%
in stock  
$47.00   $33.00
- +
  • Technical Information
  • Properties
  • Upstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Upstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00FBGG
Chemical Name:
LY2109761
CAS Number:
700874-71-1
Molecular Formula:
C26H27N5O2
Molecular Weight:
441.5249
MDL Number:
MFCD12923354
SMILES:
O1CCN(CC1)CCOc1ccc2c(c1)nccc2c1c2CCCn2nc1c1ccccn1
Properties
Computed Properties
 
Complexity:
632  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
33  
Hydrogen Bond Acceptor Count:
6  
Rotatable Bond Count:
6  
XLogP3:
2.8  

Upstream Synthesis Route

[1]Patent:WO2004/48382,2004,A1,.Locationinpatent:Page7

[2]JournalofMedicinalChemistry,2008,vol.51,#7,p.2302-2306

Literature

Title: In vitro and ex vivo anti-fibrotic effects of LY2109761, a small molecule inhibitor against TGF-β.

Journal: Toxicology and applied pharmacology 20180915

Title: Resveratrol suppresses epithelial-to-mesenchymal transition in colorectal cancer through TGF-β1/Smads signaling pathway mediated Snail/E-cadherin expression.

Journal: BMC cancer 20150101

Title: Galangin suppresses HepG2 cell proliferation by activating the TGF-β receptor/Smad pathway.

Journal: Toxicology 20141204

Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.

Journal: Bioorganic & medicinal chemistry letters 20130801

Title: LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-β and BMP-associated proinflammatory and proangiogenic signals.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120701

Title: Effect of transforming growth factor beta (TGF-β) receptor I kinase inhibitor on prostate cancer bone growth.

Journal: Bone 20120301

Title: Trimodal glioblastoma treatment consisting of concurrent radiotherapy, temozolomide, and the novel TGF-β receptor I kinase inhibitor LY2109761.

Journal: Neoplasia (New York, N.Y.) 20110601

Title: Outgrowth of drug-resistant carcinomas expressing markers of tumor aggression after long-term TβRI/II kinase inhibition with LY2109761.

Journal: Cancer research 20110315

Title: Targeting the Transforming Growth Factor-beta pathway inhibits human basal-like breast cancer metastasis.

Journal: Molecular cancer 20100101

Title: Inhibition of transforming growth factor beta receptor I kinase blocks hepatocellular carcinoma growth through neo-angiogenesis regulation.

Journal: Hepatology (Baltimore, Md.) 20091001

Title: Targeting transforming growth factor (TGF)-betaRI inhibits activation of beta1 integrin and blocks vascular invasion in hepatocellular carcinoma.

Journal: Hepatology (Baltimore, Md.) 20090301

Title: Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.

Journal: Journal of medicinal chemistry 20080410

Title: LY2109761, a novel transforming growth factor beta receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis.

Journal: Molecular cancer therapeutics 20080401

Title: Melisi D, 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.

Title: Fransvea E, et al. Blocking transforming growth factor-beta up-regulates E-cadherin and reduces migration and invasion of hepatocellular carcinoma cells. Hepatology, 2008, 47(5), 1557-1566.

Title: Zhang M, et al. Blockade of TGF-β signaling by the TGFβR-I kinase inhibitor LY2109761 enhances radiation response and prolongs survival in glioblastoma. Cancer Res, 2011, 71(23), 7155-7167.

Quotation Request
Company Name:
*
Contact Person:
*
Email:
*
Quantity Required:
*
Country:
Additional Info:
SDS
Tags:700874-71-1 Molecular Formula|700874-71-1 MDL|700874-71-1 SMILES|700874-71-1 LY2109761