ChemicalBook > CAS DataBase List > PF-6260933

PF-6260933

Product Name: PF-6260933
CAS No.: 1811510-56-1
Chemical Name: PF-6260933
Synonyms: PF06260933;PF-6260933;PF-06260933 (PF 6260933;PF-06260933, 10 mM in DMSO;5-(4-Chlorophenyl)-[3,3'-bipyridine]-6,6'-diamine;[3,3'-Bipyridine]-6,6'-diamine, 5-(4-chlorophenyl)-;PF 06260933;PF06260933;PF6260933;PF 6260933;PF-6260933;inhibit,MAP4K,MAPK Kinase Kinase Kinase,PF 06260933,PF06260933,Inhibitor,PF-06260933
CBNumber: CB53344890
Molecular Formula: C16H13ClN4
Formula Weight: 296.75
MOL File: 1811510-56-1.mol

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PF-6260933 Property

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

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Safety

HS Code: 2933998090

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-8001
Product name: PF-06260933
Purity: 98.41%
Packaging: 5mg
Price: $144
Updated: 2021/12/16

ChemScene

Product number: CS-8001
Product name: PF-06260933
Purity: 98.41%
Packaging: 10mg
Price: $228
Updated: 2021/12/16

ChemScene

Product number: CS-8001
Product name: PF-06260933
Purity: 98.41%
Packaging: 25mg
Price: $468
Updated: 2021/12/16

ChemScene

Product number: CS-8001
Product name: PF-06260933
Purity: 98.41%
Packaging: 50mg
Price: $660
Updated: 2021/12/16

ChemScene

Product number: CS-8001
Product name: PF-06260933
Purity: 98.41%
Packaging: 100mg
Price: $1020
Updated: 2021/12/16

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PF-6260933 Chemical Properties,Usage,Production

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.

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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.

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

PF-6260933 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF 06260933;PF06260933;PF6260933;PF 6260933;PF-6260933

PF-6260933

PF06260933

[3,3'-Bipyridine]-6,6'-diamine, 5-(4-chlorophenyl)-

inhibit,MAP4K,MAPK Kinase Kinase Kinase,PF 06260933,PF06260933,Inhibitor,PF-06260933

5-(4-Chlorophenyl)-[3,3'-bipyridine]-6,6'-diamine

PF-06260933, 10 mM in DMSO

PF-06260933 (PF 6260933

1811510-56-1