PF 04449913 maleate

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Description: Potent Smo antagonist
Alternative Names: glasdegib,PF-913
Chemical Name: 1-((2R,4R)-2-(1H-Benzimidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate salt
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for PF 04449913 maleate

PF 04449913 maleate is a potent Smo antagonist (IC50 = 5 nM). Attenuates the leukemia-initiation potential of AML cells in a serial transplantation mouse model. Also eliminates self-propagation capacity of AML cells.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 04449913 maleate

PF 04449913 maleate is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen FDA-Approved Drugs and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 04449913 maleate

M. Wt 490.51
Formula C21H22N6O.C4H4O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 2030410-25-2
PubChem ID 122640033
Smiles OC(/C=C\C(O)=O)=O.CN1CC[C@@H](NC(NC2=CC=C(C#N)C=C2)=O)C[C@@H]1C3=NC4=CC=CC=C4N3

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 04449913 maleate

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 49.05 100

Preparing Stock Solutions for PF 04449913 maleate

The following data is based on the product molecular weight 490.51. 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 2.04 mL 10.19 mL 20.39 mL
5 mM 0.41 mL 2.04 mL 4.08 mL
10 mM 0.2 mL 1.02 mL 2.04 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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Product Datasheets for PF 04449913 maleate

References for PF 04449913 maleate

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

Munchhof et al (2011) Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened. ACS Med.Chem.Lett. 3 106 PMID: 24900436

Fukushima et al (2016) Small-molecule Hedgehog inhibitor attenuates the leukemia-initiation potential of acute myeloid leukemia cells. Cancer Sci. 107 1422 PMID: 27461445

Giordani et al (2016) The human Smoothened inhibitor PF-04449913 induces exit from quiescence and loss of multipotent Drosophila hematopoietic progenitor cells. Oncotarget 7 55313 PMID: 27486815

If you know of a relevant reference for PF 04449913 maleate, please let us know.

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Citations for PF 04449913 maleate

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Stem Cell Research Product Guide

Stem Cell Research Product Guide

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