| Chemical Properties | Back Directory | [Boiling point ]
731.0±70.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
7.86±0.30(Predicted) | [color ]
Light yellow to brown |
| Hazard Information | Back Directory | [Description]
CCT251455 is a potent and selecltive MSP1 inhibitor with potential anticancer activitiy. The protein kinase MPS1 is a crucial component of the spindle assembly checkpoint signal and is aberrantly overexpressed in many human cancers. MPS1 is one of the top 25 genes overexpressed in tumors with chromosomal instability and aneuploidy. PTEN-deficient breast tumor cells are particularly dependent upon MPS1 for their survival, making it a target of significant interest in oncology. CCT251455 stabilizes an inactive conformation of MPS1 with the activation loop ordered in a manner incompatible with ATP and substrate-peptide binding; it displays a favorable oral pharmacokinetic profile, shows dose-dependent inhibition of MPS1 in an HCT116 human tumor xenograft model, and is an attractive tool compound to elucidate further the therapeutic potential of MPS1 inhibition. | [Uses]
CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC50 of 3 nM. | [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]. | [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. DOI:10.1021/jm401395s |
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| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
| Company Name: |
ABBIOCHEM
|
| Tel: |
18964309092 18964309092 |
| Website: |
http://www.abbiochemical.com |
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