Synonym
2-MT 63; 2-MT-63; 2-MT63; 2MT 63; 2MT-63; 2MT63;
IUPAC/Chemical Name
N-(2-((3-(dimethylamino)propyl)(methyl)amino)-5-(trifluoromethyl)phenyl)-2-fluoro-5-((3-(4-(methylamino)-1,3,5-triazin-2-yl)pyridin-2-yl)oxy)benzamide
InChi Key
HHKGVQGXRGQBBA-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H30F4N8O2/c1-34-28-37-17-36-25(39-28)20-7-5-12-35-27(20)43-19-9-10-22(30)21(16-19)26(42)38-23-15-18(29(31,32)33)8-11-24(23)41(4)14-6-13-40(2)3/h5,7-12,15-17H,6,13-14H2,1-4H3,(H,38,42)(H,34,36,37,39)
SMILES Code
CNC1=NC=NC(C2=CC=CN=C2OC3=CC=C(F)C(C(NC4=C(N(C)CCCN(C)C)C=CC(C(F)(F)F)=C4)=O)=C3)=N1
Purity
>98% (or refer to the Certificate of Analysis)
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
Shelf Life
>3 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).
HS Tariff Code
2934.99.9001
More Info
2-MT 63 represents a novel inhibitor of the TIE2 receptor. There are multiple kinase inhibitors that have validated activity versus the TIE2 receptor including the advanced clinical agents, Sitravatinib, Glesatinib and Rebastinib. This agent is a useful tool given its unique polypharmacological profile (Rebastinib, for instance, also inhibits VEGFR2, BCR-ABL, LYN and ABL1 kinases while 2-MT 63 does not.) There is a lack of data from cell culture experiments involving this agent in the original publication. It was also shown to inhibit TIE2 autophosphorylation in vivo. However, this outcome was limited - with activity occurring at a high dose (100 mg/kg) and only transiently (positive at 3 hours but the effect was lost by 8 hours).
Preparing Stock Solutions
The following data is based on the
product
molecular weight
598.61
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Bready J,
Caenepeel S, Cee VJ, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y,
Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, Morrison M, Olivieri PR, Patel
VF, Polverino A, Rose P, Tempest P, Wang L, Whittington DA, Zhao H. Evolution of
a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase
inhibitor. J Med Chem. 2007 Feb 22;50(4):611-26. Epub 2007 Jan 25. PubMed PMID:
17253678.
