Telapristone acetate

Telapristone acetate (CDB-4124) is a potent progesterone receptor (PR) modulator. Telapristone acetate inhibits the proliferation of ovarian cancer cells by inducing cell cycle arrest and apoptosis. Telapristone effectively inhibits the occurrence and development of spontaneous and chemically induced mammary tumors in rats. Telapristone acetate can be used for breast and ovarian cancer research^[1][2]. IC50 & Target:IC50：35.5±3.9,21.3±1.8,43.6±5.1,47.4±3.9 μM of IGROV-1, IGROV-1 PTES, SKOV-3, SKOV-3 PTES cells, respectively^[1]. In Vitro:Telapristone acetate (0-60 μM, 96 h) inhibits the growth of ovarian cancer cells resistant to Cisplatin (CDDP) (HY-17394) and Paclitaxel (PTX) (HY-B0015), with IC₅₀ values of 35.5 μM (IGROV-1), 21.3 μM (IGROV-1 PTES), 43.6 μM (SKOV-3) and 47.4 μM (SKOV-3 PTES)^[1].
Telapristone acetate (30 μM, 48 h) induces cell cycle arrest and apoptosis in IGROV-1 and IGROV-1 PTES cells, as evidenced by the upregulation of p21^Cip1/p27^Kip1 and PARP cleavage, respectively^[1].
Telapristone acetate (0-10 μmol/L, 3-6 days) induces G1/S cell cycle arrest and thereby inhibits cell growth by downregulating CDK2 and CDK4 in human T47D cells^[2]. In Vivo:Telapristone acetate (20, 70, and 200 mg/kg, i.g., daily for 24 months) inhibits spontaneous mammary carcinogenesis by reducing lobular hyperplasia and development of benign tumors in rats^[2].
Telapristone acetate (3 and 30 mg/pellet, s.c., over 84 days, initiated 6 days post-MNU) suppresses the development of precancerous lesions and carcinogen-induced estrogen receptor (ER)⁺ mammary tumors in rats^[2].