WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407976
Description: 2-MT 63 is a novel TIE-2 kinase inhibitor that demonstrates unique and improved kinase selectivity compared to other inhibitors known to interact with TIE-2. 2-MT 63 has a good kinase selectivity profile in enzyme assays with >30-fold selectivity (typically much greater) against the tested kinases. Importantly, the profile includes selectivity against other targets of relevance for angiogenesis (KDR, PDGFR, EPHB4).
MedKoo Cat#: 407976
Chemical Formula: C29H30F4N8O2
Exact Mass: 598.2428
Molecular Weight: 598.6066
Elemental Analysis: C, 58.19; H, 5.05; F, 12.70; N, 18.72; O, 5.35
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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
Appearance: Solid powder
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
The following data is based on the product molecular weight 598.6066 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:
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).