1400284-80-1

1400284-80-1 structure

Name: CCT251455
Chemical Name: Tert-Butyl 6-{[2-Chloro-4-(1-Methyl-1h-Imidazol-5-Yl)phenyl]amino}-2-(1-Methyl-1h-Pyrazol-4-Yl)-1h-Pyrrolo[3,2-C]pyridine-1-Carboxylate
CAS Number: 1400284-80-1
Molecular Formula: C₂₆H₂₆ClN₇O₂
Molecular Weight: 503.983
Catalog: Signaling Pathways Cell Cycle/DNA Damage Mps1
Create Date: 2018-06-03 10:32:45
Modify Date: 2024-01-10 08:35:37
CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC50 of 3 nM.

Name	Tert-Butyl 6-{[2-Chloro-4-(1-Methyl-1h-Imidazol-5-Yl)phenyl]amino}-2-(1-Methyl-1h-Pyrazol-4-Yl)-1h-Pyrrolo[3,2-C]pyridine-1-Carboxylate
Synonyms	1H-Pyrrolo[3,2-c]pyridine-1-carboxylic acid, 6-[[2-chloro-4-(1-methyl-1H-imidazol-5-yl)phenyl]amino]-2-(1-methyl-1H-pyrazol-4-yl)-, 1,1-dimethylethyl ester Tert-Butyl 6-{[2-Chloro-4-(1-Methyl-1h-Imidazol-5-Yl)phenyl]amino}-2-(1-Methyl-1h-Pyrazol-4-Yl)-1h-Pyrrolo[3,2-C]pyridine-1-Carboxylate 2-Methyl-2-propanyl 6-{[2-chloro-4-(1-methyl-1H-imidazol-5-yl)phenyl]amino}-2-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,2-c]pyridine-1-carboxylate

Description	CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC50 of 3 nM.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> Mps1 Signaling Pathways >> Cytoskeleton >> Mps1 Research Areas >> Cancer
Target	IC50: 3 nM (MPS1)[1]
In Vitro	CCT251455 is a highly potent inhibitor of MPS1 that demonstrates high selectivity versus kinases tested in a broad kinome profiling panel. CCT251455 inhibits P-MPS1 with an IC50 of 0.04 μM in cell-based assay and has a GI50 of 0.16 μM[1].
In Vivo	CCT251455 demonstrates a good oral pharmacokinetic profile in mouse and rat as well as inhibition of MPS1 activity in vivo following oral administration[1].
Cell Assay	HCT116 cells are treated with 0-20 μM CCT251455 for 72 h. Cell viability is measured using the MTT assay[1].
Animal Admin	Mice[1] [1]Human HCT116 colon carcinoma cells are sc injected bilaterally in the flanks of female CrTac:NCr-Fox1(nu) athymic mice. Once tumors reach a mean diameter of 8 mm (day 15), mice are dosed twice at a 12 h intervals with 50, 75, or 100 mg/kg of CCT251455 in 10% (v/v) DMSO and 5% (v/v) Tween 20 in saline. Mice are culled (n=3 per group) at 2, 10, and 72 h after the second dose. Tumors are snap-frozen and stored at -80 °C until analysis[1].
References	[1]. Naud S, et al. Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). J Med Chem. 2013 Dec 27;56(24):10045-65.