PF 06260933 dihydrochloride

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Description: MAP4K4 (HGK) inhibitor; also inhibits MINK and TNIK
Chemical Name: 5-(4-Chlorophenyl)-[3,3'-bipyridine]-6,6'-diamine dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (1)

Biological Activity for PF 06260933 dihydrochloride

PF 06260933 dihydrochloride is a MAP4K4 (HGK) inhibitor (IC50 = 140 nM). Also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). Improves fasting hyperglycemia in mice. Orally active.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 06260933 dihydrochloride

PF 06260933 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 06260933 dihydrochloride

M. Wt 369.68
Formula C16H13ClN4.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1883548-86-4
PubChem ID 118701007
InChI Key VRQXEOPUAQLBQI-UHFFFAOYSA-N
Smiles NC1=NC=C(C3=CN=C(N)C=C3)C=C1C2=CC=C(Cl)C=C2.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PF 06260933 dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 36.97 100
DMSO 7.39 20

Preparing Stock Solutions for PF 06260933 dihydrochloride

The following data is based on the product molecular weight 369.68. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.71 mL 13.53 mL 27.05 mL
5 mM 0.54 mL 2.71 mL 5.41 mL
10 mM 0.27 mL 1.35 mL 2.71 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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Product Datasheets for PF 06260933 dihydrochloride

References for PF 06260933 dihydrochloride

References are publications that support the biological activity of the product.

Ammirati et al (2015) Discovery of an in vivo tool to establish proof-of-concept for MAP4K4-based antidiabetic treatment. ACS Med.Chem.Lett. 6 1128 PMID: 26617966


If you know of a relevant reference for PF 06260933 dihydrochloride, please let us know.

View Related Products by Product Action

View all Other MAPK Inhibitors

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2 Citations for PF 06260933 dihydrochloride

Citations are publications that use Tocris products. Selected citations for PF 06260933 dihydrochloride include:

Sebastian et al (2019) Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents. Cell Chem Biol 26 1703-1715.e37 PMID: 31676236

Gao et al (2017) MAP4K4 is a novel MAPK/ERK pathway regulator required for lung adenocarcinoma maintenance. Mol Oncol 11 628 PMID: 28306189


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


MAPK Signaling Scientific Review

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.