. LY2801653 | LY-2801653 | CAS#1206799-15-6 | c-Met inhibitor | MedKoo Biosciences

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MedKoo product information:

  

  LY2801653

  

Description of LY2801653: LY2801653 is an orally available, small molecule inhibitor of the proto-oncogene c-Met (mesenchymal-epithelial transition, also known as hepatocyte growth factor receptor [HGFR]) with potential antineoplastic activity. c-Met inhibitor LY2801653 selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. This agent has potent anti-tumor efficacy in mono- and combination therapy in a broad range of cancers. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays key roles in tumor cell proliferation, survival, invasion, metastasis, and tumor angiogenesis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). (last updated: 10/20/2014).

  

Current developer:    Eli Lilly.

  

MedKoo Cat#: 205526

Name: LY2801653

CAS#: 1206799-15-6

Synonym: LY2801653; LY-2801653; LY 2801653.

IUPAC/Chemical name: 

N-(3-fluoro-4-((1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide

Chemical structure

Theoretical analysis

LY2801653

 MedKoo Cat#:  205526
Name:  LY2801653
CAS#:  1206799-15-6

Chemical Formula: C30H22F2N6O3
Exact Mass: 552.17215
Molecular Weight: 552.53
Elemental Analysis: C, 65.21; H, 4.01; F, 6.88; N, 15.21; O, 8.69  

  

Availability and price:

LY2801653, purity > 98%, may be available through custom synthesis. Minimum 1 gram order is requested. Lead time is usually 2-3 months. Please email us to ask quote. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee:  from $30.00 (USA); $45.00 (Canada); $70.00 (international).

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200mg / Not Available

500mg / Not Available

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2.0g / Ask price

5.0g / Ask price

   

   

Technical data

Appearance:

Solid powder

Purity:

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

View current batch of CoA

QC data:

View NMR, View HPLC, View MS

Safety Data Sheet (MSDS):

View Material Safety Data Sheet (MSDS)

Shipping condition:

Shipped under ambient temperature as non-hazardous chemical.  This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage condition:

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:

Soluble in DMSO, not in water

Shelf life:

>2 years if stored properly

Drug formulation:

This drug may be formulated in DMSO

Stock solution storage:

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Note: The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

 

Protocols from literature

In vitro protocol::

XXX

In vivo protocol:

XXX

Clinical study:

XXX

Review papers:

XXX 

 

Information about this agent

 LY2801653 was identified and developed as a novel, potent, and orally active small molecule inhibitor of human c-Met. It demonstrated dose dependent inhibition of c-Met phosphorylation in xenograft tumors with a long lasting PD effect.  LY2801653 displayed potent anti-tumor efficacy in a number of non small cell lung, renal, pancreatic, and breast tumor models. Examination of c-Met expression in these tumors by immunohistochemistry (IHC) revealed a good correlation between response and c-Met expression in the tumor tissue.  LY2801653 treatment led to increase in functional vessel areas, and decrease in tumor hypoxia. Enhanced anti-tumor efficacy was achieved when Erlotinib was combined with LY2801653. . (source: http://cancerres.aacrjournals.org/cgi/content/meeting_abstract/70/8_MeetingAbstracts/3611).

   

 

References

1: Yan SB, Peek VL, Ajamie R, Buchanan SG, Graff JR, Heidler SA, Hui YH, Huss KL, Konicek BW, Manro JR, Shih C, Stewart JA, Stewart TR, Stout SL, Uhlik MT, Um SL,  Wang Y, Wu W, Yan L, Yang WJ, Zhong B, Walgren RA. LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and  other oncoproteins, and displays anti-tumor activities in mouse xenograft models. Invest New Drugs. 2012 Dec 29. [Epub ahead of print] PubMed PMID: 23275061.

  

 

 

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