PF 04449913 maleate

Name: PF 04449913 maleate
Brand: Tocris Bioscience
SKU: 6538

Tocris Bioscience, part of Bio-Techne | Catalog # 6538

COA / SDS

Potent Smo antagonist

Key Product Details

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)
Molecular Weight:	490.51

View Full Technical Details for PF 04449913 maleate

Technical Data
Citations

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
InChi Key	VJCVKWFBWAVYOC-UIXXXISESA-N
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 for PF 04449913 maleate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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	0.20 mL	1.02 mL	2.04 mL
50 mM	0.04 mL	0.20 mL	0.41 mL

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References for PF 04449913 maleate

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

Fukushima Small-molecule Hedgehog inhibitor attenuates the leukemia-initiation potential of acute myeloid leukemia cells. Cancer Sci. 2016 PMID: 27461445
Giordani The human Smoothened inhibitor PF-04449913 induces exit from quiescence and loss of multipotent Drosophila hematopoietic progenitor cells. Oncotarget 2016 PMID: 27486815
Munchhof Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened. ACS Med.Chem.Lett. 2011 PMID: 24900436