1. MAPK/ERK Pathway
  2. MAP4K
  3. PF-06260933

PF-06260933 

Cat. No.: HY-19562 Purity: 99.69%
Handling Instructions

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.

For research use only. We do not sell to patients.

PF-06260933 Chemical Structure

PF-06260933 Chemical Structure

CAS No. : 1811510-56-1

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
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10 mg USD 228 In-stock
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25 mg USD 468 In-stock
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50 mg USD 660 In-stock
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100 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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.

IC50 & Target[1]

MAP4K4

3.7 nM (IC50)

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].

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].

Molecular Weight

296.75

Formula

C₁₆H₁₃ClN₄

CAS No.

1811510-56-1

SMILES

NC1=C(C2=CC=C(Cl)C=C2)C=C(C(C=N3)=CC=C3N)C=N1

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
In Vitro: 

DMSO : 30 mg/mL (101.10 mM; Need ultrasonic and warming)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.42 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

HUVECs are maintained in EGM2 media at 37°C and 5% CO2. HUVECs or peritoneal macrophages are treated with vehicle or PF-06260933 in vitro to determine whether pharmacological inhibition of MAP4K4 alteres MAPK signalling in response to TNF-α[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Compound PF-06260933 (10 mg/kg, dissolved in dH2O) is orally administered to 8 to 10-week-old male Apoe-/- mice twice daily for 6 weeks. Ldlr-/- male mice are placed on high-fat diet (HFD) for 10 weeks before drug administration. Compound PF-06260933 is administered to male 8 to 10-week-old Ldlr-/- mice as above for 10 weeks. Oral administration of water is used as vehicle control in all studies. Mice are euthanized by CO2 inhalation followed by bilateral pneumothorax[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

PF-06260933PF06260933PF 06260933MAP4KMAPK Kinase Kinase KinaseInhibitorinhibitorinhibit

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Product name:
PF-06260933
Cat. No.:
HY-19562
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