ChemicalBook CAS DataBase List 936345-35-6

936345-35-6

Name	PF-2413873
CAS	936345-35-6
Molecular Formula	C18H21N3O3S
MDL Number	MFCD16987601
Molecular Weight	359.44
MOL File	936345-35-6.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)
form	Solid
pka	1.12±0.10(Predicted)
color	White to light yellow

Hazard Information

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 potentselective 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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