PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that can inhibit the effects of PAX3-FOXO1. PFI-90 causes apoptosis and myogenic differentiation, leading to increased cell death. PFI-90 has potential anti-tumor activity and is from patent WO2021101929A1.

Physicochemical Properties

Molecular Formula	C11H10N4O
Molecular Weight	214.223
Exact Mass	214.085
CAS #	53995-62-3
PubChem CID	12499590
Appearance	Light yellow to yellow solid powder
LogP	1.697
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Heavy Atom Count	16
Complexity	234
Defined Atom Stereocenter Count	0
InChi Key	GCZPXNWBXDWHKM-UHFFFAOYSA-N
InChi Code	InChI=1S/C11H10N4O/c16-11(9-5-1-3-7-12-9)15-14-10-6-2-4-8-13-10/h1-8H,(H,13,14)(H,15,16)
Chemical Name	N'-pyridin-2-ylpyridine-2-carbohydrazide
HS Tariff Code	2934.99.9001
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)

Biological Activity

ln Vitro	In RH4, RH30, OSA-CL, and TC-32 cells, PFI-90 displays defined responses with IC50 values of 812, 3200, 1895, and 1113 nM, respectively [1]. Addition of PFI-90 (3 μM; 24 hours) to RH4 and
Cell Assay	Western Blot analysis [1] Cell Types: RH4 and SCMC Cell Tested Concentrations: 3 μM Incubation Duration: 24 hrs (hours) Experimental Results: Increased apoptosis in RH4 and SCMC cells.
References	[1]. Inhibitors of histone demethylases (pfi-63 and pfi-90) for the treatment of cancer and for the inhibition of histone demethylase in cells. WO2021101929A1.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~466.81 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (11.67 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.6681 mL	23.3405 mL	46.6810 mL
	5 mM	0.9336 mL	4.6681 mL	9.3362 mL
	10 mM	0.4668 mL	2.3340 mL	4.6681 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.