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RIP2 kinase inhibitor 2

Names

[ CAS No. ]:
1581270-11-2

[ Name ]:
RIP2 kinase inhibitor 2

[Synonym ]:
4-Quinolinamine, 6-[(1,1-dimethylethyl)sulfonyl]-N-(4,5-dimethyl-1H-pyrazol-3-yl)-7-(2-methoxyethoxy)-
N-(4,5-Dimethyl-1H-pyrazol-3-yl)-7-(2-methoxyethoxy)-6-[(2-methyl-2-propanyl)sulfonyl]-4-quinolinamine

Biological Activity

[Description]:

RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.

[Related Catalog]:

Signaling Pathways >> Apoptosis >> RIP kinase
Research Areas >> Cancer

[Target]

RIP2 Kinase[1]


[In Vitro]

RIP2 kinase inhibitor 2 is a novel prodrug of a quinazolyl amine that inhibits RIP2 kinase. Receptor interacting protein-2 (RIP2) kinase is a TKL family serine/threonine protein kinase involved in innate immune signaling. Following activation, RIP2 kinase associates with NODI or NOD2 and appears to function principally as a molecular scaffold to bring together other kinases (TAK1, ΙΚΚα/β/γ) involved in NF-κΒ and mitogen-activated protein kinase activation[1].

[Animal admin]

Rats[1] Rats are orally pre-dosed with the RIP2 kinase inhibitor 2, at doses of 0.016, 0.16 and 1.6 mg/kg (n=8 rats/group), followed by dosing with L18-MDP (50 μg/rat) 0.25 hours after pre-dosing with the compound. The IL8 cytokine levels and percentage levels are calculated as the mean±standard error of the mean (n=8 rats/group).

[References]

[1]. Linda N. Casillas, et al. Amino-quinolines as kinase inhibitors. PCT Int. Appl. (2014), WO 2014043437 A1 20140320.


[Related Small Molecules]

Necrostatin-1 | GSK872 | GSK2982772 | WEHI-345 | RIPA-56 | GSK 583 | RIP2 kinase inhibitor 1 | GSK'481 | Nec-4

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
670.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C21H28N4O4S

[ Molecular Weight ]:
432.536

[ Flash Point ]:
359.0±31.5 °C

[ Exact Mass ]:
432.183136

[ LogP ]:
3.27

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.595

[ Storage condition ]:
2-8℃


Related Compounds