MGCD-265-analog
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 201841

CAS#: 875337-44-3

Description: MGCD265-analog, CAS#875337-44-3, is structurally related to MGCD-265 (Glesatinib). MGCD-265-analog is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity. MGCD-265-analog was introduced to the research community due to the wrong structure published in some database and publications. MGCD-265-analog has been sold as MGCD-265 by many reagent vendors since 2012. As of 4/28/2016, many drug-related database and suppliers still listed a wrong structure for MGCD-265. MGCD-265 (Glesatinib) has CAS#936694-12-1.


Price and Availability

Size
Price

25mg
Not available
200mg
Not available
2g
USD 3850
Size
Price

50mg
Not available
500mg
Not available
5g
USD 6950
Size
Price

100mg
Not available
1g
USD 2850
10g
Ask price

MGCD-265-analog is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 201841
Name: MGCD-265-analog
CAS#: 875337-44-3
Chemical Formula: C26H20FN5O2S2
Exact Mass: 517.10424
Molecular Weight: 517.6
Elemental Analysis: C, 60.33; H, 3.89; F, 3.67; N,13.53; O, 6.18; S, 12.39


Synonym: MGCD-265-analog; MGCD 265-analog; MGCD265-analog. Glesatinib-analog.

IUPAC/Chemical Name: N-((3-fluoro-4-((2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)carbamothioyl)-2-phenylacetamide

SMILES Code: O=C(NC(NC1=CC=C(OC2=C3C(C=C(C4=CN(C)C=N4)S3)=NC=C2)C(F)=C1)=S)CC5=CC=CC=C5


Technical Data

Appearance:
Solid powder

Purity:
>98%

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time sent 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:
>5 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

MGCD265 is a novel targeted cancer therapeutic discovered by MethylGene that inhibits the Met and VEGF receptor tyrosine kinases. The abnormal activation of Met is involved in tumor development, metastasis and survival and the VEGF kinase is responsible for the inappropriate formation of blood vessels (angiogenesis) that nourish the tumor. In preclinical studies, MGCD265 demonstrated nanomolar potency in enzyme and cellular assays and up to 100% of tumor growth inhibition in a broad range of xenograft models.
 
Development Status of MGCD265: In the ongoing Phase 1 program, MGCD265 is being administered orally in patients with advanced cancers. The compound has demonstrated a favorable safety profile and can be combined safely with other cancer therapeutics such as docetaxel (Taxotere®) and erlotinib (Tarceva®). These therapeutics were selected for combination studies based on preclinical data that demonstrated the combination of MGCD265 and erlotinib and of MGCD265 and docetaxel showed greater anti-tumor activity compared to each drug administered alone. To date, the Company has initiated three clinical studies. (source: http://methylgene.com, accessed date: 2/1/2012)
   
 


References

J. M. Besterman, M. Fournel, I. Dupont, C. Bonfils, M. Dubay, H. Ste-Croix, C. R. Maroun; MethylGene, Inc., Montreal, QC, Canada, Potent preclinical antitumor activity of MGCD265, an oral Met/VEGFR kinase inhibitor in phase II clinical development, in combination with taxanes or erlotinib, J Clin Oncol 28, 2010 (suppl; abstr e13595).