PF-02413873
CAS No. : 936345-35-6
(Synonyms: PF-2413873)
| Size | Price | Stock |
|---|---|---|
| 5mg | $100 | In-stock |
| 10mg | $160 | In-stock |
| 25mg | $320 | In-stock |
| 50mg | $510 | In-stock |
| 100mg | $820 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-11028 |
| M.Wt: | 359.44 |
| Formula: | C18H21N3O3S |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic;warming;heat to 60°C) |
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].
IC50 & Target: Ki: 2.6 nM (progesterone receptor)[1]
In Vitro: PF-02413873 shows potent PR antagonist activity with a derived Ki of 9.7 nM in the T47D native functional assay[1].
PF-02413873 (1 nM-10 μM) induces nuclear translocation only at high concentrations (>3 μM)[1].
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 t1/2 (4.2 h), Cmax (162 ng/mL) and CL/F (41 mL/min/kg)[1].
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