PF-2413873

Product NamePF-2413873
CAS936345-35-6
MFC18H21N3O3S
MW359.44
EINECS
MOL File936345-35-6.mol

Chemical Properties

Melting point	163-164 °C
Boiling point	548.9±50.0 °C(Predicted)
Density	1.31±0.1 g/cm3(Predicted)
storage temp.	room temp
solubility	DMSO : 100 mg/mL (278.21 mM; Need ultrasonic)
pka	1.12±0.10(Predicted)
form	Solid
color	White to light yellow
InChI	1S/C18H21N3O3S/c1-11-7-15(8-12(2)16(11)9-19)24-18-13(3)21(10-25(4,22)23)20-17(18)14-5-6-14/h7-8,14H,5-6,10H2,1-4H3
InChIKey	QSFGZNVRVZHUGV-UHFFFAOYSA-N
SMILES	CC1=C(C#N)C(C)=CC(OC2=C(C)N(CS(=O)(C)=O)N=C2C3CC3)=C1

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo[1][2].

Biological Activity

PF-02413873 is a potent, selective and fully competitive non-steroidal progesterone receptor (PR) antagonist th at blocks progesterone binding and PR nuclear translocation. PF-02413873 suppresses endometrial growth in the macaque and human.

in vivo

PF-02413873 (2.5 and 10 mg/kg; p.o. twice daily for 10 days) induces a statistically significant reduction in endometrial thickness in cynomolgus macaques^[1].
PF-02413873 (3 mg/kg; a single p.o.) exhibits t_1/2 (4.2 h), C_max (162 ng/mL) and CL/F (41 mL/min/kg)^[1].

Animal Model:	Cynomolgus macaques (3.7-5.7 kg; 5-6 years)^[1]
Dosage:	2.5, 10 mg/kg
Administration:	P.o. twice daily for 10 days
Result:	Reduced the endometrial thickness of 43 and 56% at the dose of 2.5 and 10 mg/kg, respectively.

Animal Model:	Cynomolgus macaques (3.7-5.7 kg; 5-6 years)^[1]
Dosage:	3 mg/kg (Pharmacokinetic Analysis)
Administration:	A single p.o.
Result:	t_1/2=4.2 h, C_max=162 ng/mL, CL/F=41 mL/min/kg.

References

[1] Howe DC, et, al. The translational efficacy of a nonsteroidal progesterone receptor antagonist, 4-[3-cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile (PF-02413873), on endometrial growth in macaque and human. J Pharmacol Exp Ther. 2011 Nov;339(2):642-53. DOI:10.1124/jpet.111.183848
[2] Bungay PJ, et, al. Preclinical and clinical pharmacokinetics of PF-02413873, a nonsteroidal progesterone receptor antagonist. Drug Metab Dispos. 2011 Aug;39(8):1396-405. DOI:10.1124/dmd.110.037234

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