Merestinib (LY2801653)
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MedKoo CAT#: 205526

CAS#: 1206799-15-6 (free base)

Description: Merestinib, also known as LY2801653, is a n 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.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 650
1g
USD 2850
Size
Price

25mg
USD 250
200mg
USD 950
2g
USD 3650
Size
Price

50mg
USD 450
500mg
USD 1650
5g
USD 5650

Merestinib, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 1g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205526
Name: Merestinib (LY2801653)
CAS#: 1206799-15-6 (free base)
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


Related CAS #: 1206799-15-6 (free base)   1206801-37-7 (HCl)    

Synonym: LY-2801653; LY 2801653; LY2801653; Merestinib

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

InChi Key: QHADVLVFMKEIIP-UHFFFAOYSA-N

InChi Code: InChI=1S/C30H22F2N6O3/c1-17-3-9-23(30(40)38(17)22-7-4-20(31)5-8-22)29(39)36-21-6-10-27(25(32)12-21)41-28-11-18-16-35-37(2)26(18)13-24(28)19-14-33-34-15-19/h3-16H,1-2H3,(H,33,34)(H,36,39)

SMILES Code: O=C(C1=CC=C(C)N(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=CC5=C(N(C)N=C5)C=C4C6=CNN=C6)C(F)=C3


Technical Data

Appearance:
White to off-white solid powder

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

Certificate of Analysis:

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).

Harmonized System Code:
293490


Additional Information

  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).
 
(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.