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25mg |
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Purity: ≥98%
PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 (Mitogen-activated protein kinase kinase kinase kinase 4) with IC50 values of 3.7 and 160 nM for cell-freel assay (kinase) and cell assay, respectively. It also inhibits MINK and TNIK with IC50 values of 8 and 13 nM, respectively. PF-06260933 has been reported to improve fasting hyperglycemia in mice. Recent studies in adipose tissue, pancreas, muscle, and macrophages suggest that MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic drugs. As part of the evaluation of MAP4K4 as a novel antidiabetic target, PF-6260933.
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References |
ACS Med Chem Lett.2015 Oct 6;6(11):1128-33;Nat Commun.2015 Dec 21;6:8995.
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Molecular Formula |
C16H15CL3N4
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Molecular Weight |
369.67610001564
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CAS # |
1883548-86-4
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Related CAS # |
1883548-86-4 (2HCl);1811510-56-1;2118243-34-6 (HCl);
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SMILES |
ClC1C=CC(=CC=1)C1C(N)=NC=C(C2C=NC(=CC=2)N)C=1.Cl.Cl
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Synonyms |
PF-06260933 2HCl; PF 06260933 2HCl; PF06260933 2HCl;PF-06260933 dihydrochloride; PF 06260933 dihydrochloride; PF06260933dihydrochloride
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7050 mL | 13.5252 mL | 27.0504 mL | |
5 mM | 0.5410 mL | 2.7050 mL | 5.4101 mL | |
10 mM | 0.2705 mL | 1.3525 mL | 2.7050 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Pharmacological MAP4K4 inhibition ameliorates atherosclerosis.Nat Commun.2015 Dec 21;6:8995. th> |
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(a) Effects of16 (PF-06260933 )on LPS-induced TNFα levels in C57-BL/6J mice). (b) Effects of16on glycemic control inob/obmice.ACS Med Chem Lett.2015 Oct 6;6(11):1128-33. td> |
Total and free plasma concentration of16(PF-06260933 )after PO dosing (10 mg/kg) to mice.ACS Med Chem Lett.2015 Oct 6;6(11):1128-33. td> |
Heat map obtained from an Invitrogen selectivity panel (% inhibition of kinases tested @1 μM).ACS Med Chem Lett.2015 Oct 6;6(11):1128-33. th> |
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ACS Med Chem Lett.2015 Oct 6;6(11):1128-33. td> |