| Identification | Back Directory | [Name]
PF-6260933 | [CAS]
1811510-56-1 | [Synonyms]
PF-6260933
PF06260933
[3,3'-Bipyridine]-6,6'-diamine, 5-(4-chlorophenyl)-
PF 06260933;PF06260933;PF6260933;PF 6260933;PF-6260933 | [Molecular Formula]
C16H13ClN4 | [MDL Number]
MFCD30532622 | [MOL File]
1811510-56-1.mol | [Molecular Weight]
296.75 |
| Chemical Properties | Back Directory | [Boiling point ]
483.8±40.0 °C(Predicted) | [density ]
1.330±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 1 mg/ml; DMSO: 1 mg/ml; Ethanol: insol; PBS (pH 7.2): insol | [form ]
A solid | [pka]
5.04±0.13(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively. | [Biological Activity]
PF-6260933 is a MAP4K4 inhibitor with IC50 of 3.7 nM and good kinome selectivity. | [in vitro]
PF-06260933 treatment of human aortic endothelial cell (EC) robustly prevents TNF-α-mediated endothelial permeability in vitro , similar to MAP4K4 knockdown. < b> | [in vivo]
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. p> | [target]
| Target | Value | MAP4K4
() | 3.7 nM |
| [IC 50]
MAP4K4: 3.7 nM (IC50) | [References]
[1] Ammirati M, et al. 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
[2] Roth Flach RJ, et al. Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis. Nat Commun. 2015 Dec 21;6:8995. DOI:10.1038/ncomms9995 |
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| Company Name: |
Twochem Co.Ltd.
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| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
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