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[CAS NO. 1811510-56-1] PF-06260933
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-19562 |
| Brand: | MCE |
| CAS: | 1811510-56-1 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 296.75 |
| Molecular Formula | C16H13ClN4 |
| SMILES | NC1=C(C2=CC=C(Cl)C=C2)C=C(C(C=N3)=CC=C3N)C=N1 |
Summary
PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC 50 s of 3.7 and 160 nM for kinase and cell, respectively.
IC50 & Target
|
MAP4K4 3.7 nM (IC 50 ) |
In Vitro
PF-06260933 treatment of human aortic endothelial cell (EC) robustly prevents TNF-α-mediated endothelial permeability in vitro , similar to MAP4K4 knockdown [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 30 mg/mL ( 101.10 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3698 mL | 16.8492 mL | 33.6984 mL |
| 5 mM | 0.6740 mL | 3.3698 mL | 6.7397 mL |
| 10 mM | 0.3370 mL | 1.6849 mL | 3.3698 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.42 mM); Clear solution
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.
- [2] Roth Flach RJ, et al. Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis. Nat Commun. 2015 Dec 21;6:8995.
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