2-MT-63 | CAS#870225-11-9

MedKoo Cat#: 407976 | Name: 2-MT-63

Description:

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

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).

Chemical Structure

2-MT-63

CAS#870225-11-9

Theoretical Analysis

MedKoo Cat#: 407976

Name: 2-MT-63

CAS#: 870225-11-9

Chemical Formula: C29H30F4N8O2

Exact Mass: 598.2428

Molecular Weight: 598.61

Elemental Analysis: C, 58.19; H, 5.05; F, 12.70; N, 18.72; O, 5.35

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

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

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).

Instruction

View handling instruction

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.