Name | PF-6260933 |
Synonyms | PF6260933 PF-6260933 PF06260933 PF 6260933 PF 06260933 1811510-56-1 [3,3'-Bipyridine]-6,6'-diamine, 5-(4-chlorophenyl)- |
CAS | 1811510-56-1 |
Molecular Formula | C16H13ClN4 |
Molar Mass | 296.75 |
Density | 1.330±0.06 g/cm3(Predicted) |
Boling Point | 483.8±40.0 °C(Predicted) |
Solubility | DMSO : 30 mg/mL (101.10 mM; Need ultrasonic and warming) |
pKa | 5.04±0.13(Predicted) |
Storage Condition | -20°C |
Use | PF-06260933 is an orally active, highly selective MAP4K4 small molecule inhibitor with IC50 values of 3.7 and 160 nM in kinase and cell experiments, respectively. |
In vitro study | PF-06260933 treatment of human aortic endothelial cell (EC) robustly prevents TNF-α-mediated endothelial permeability in vitro , similar to MAP4K4 knockdown. |
In vivo study | In the mice model, PF-06260933 treatment does not alter plasma lipid content, although reductions in glucose levels are observed, which is consistent with whole-body-inducible Map4k4 knockout animals. PF-06260933 administration ameliorates further plaque development and/or promotes plaque regression in this animal model (46.0% versus 25.5%), and a reduction in plasma glucose as well as lipid content is also observed. |
Reference Show more | 1: Roth Flach RJ, Skoura A, Matevossian A, Danai LV, Zheng W, Cortes C, Bhattacharya SK, Aouadi M, Hagan N, Yawe JC, Vangala P, Menendez LG, Cooper MP, Fitzgibbons TP, Buckbinder L, Czech MP. Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis. Nat Commun. 2015 Dec 21;6:8995. doi: 10.1038/ncomms9995. PubMed PMID: 26688060; PubMed Central PMCID: PMC4703891. 2: Ammirati M, Bagley SW, Bhattacharya SK, Buckbinder L, Carlo AA, Conrad R, Cortes C, Dow RL, Dowling MS, El-Kattan A, Ford K, Guimarães CR, Hepworth D, Jiao W, LaPerle J, Liu S, Londregan A, Loria PM, Mathiowetz AM, Munchhof M, Orr ST, Petersen DN, Price DA, Skoura A, Smith AC, Wang J. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33. doi: 10.1021/acsmedchemlett.5b00215. eCollection 2015 Nov 12. PubMed PMID: 26617966; PubMed Central PMCID: PMC4645242. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.37 ml | 16.849 ml | 33.698 ml |
5 mM | 0.674 ml | 3.37 ml | 6.74 ml |
10 mM | 0.337 ml | 1.685 ml | 3.37 ml |
5 mM | 0.067 ml | 0.337 ml | 0.674 ml |