CYP17 Inhibitor

Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC₅₀s of 2.5 nM and 15 nM, respectively.

Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).

Galeterone (TOK-001) is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone also functions as a CYP17 inhibitor (IC₅₀ = 47 nM). Galeterone induces cell apoptosis. Galeterone inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research^[1][2].

21-Hydroxypregnenolone is a CYP17 inhibitor. 21-Hydroxypregnenolone competitively inhibits CYP17-mediated 17α-hydroxylation activity of progesterone, with a Ki value of 36.4 μM.

Orteronel (TAK-700) is a highly selective inhibitor of human 17,20-lyase (CYP17) with IC₅₀ of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4.

Abiraterone acetate (Standard) is the analytical standard of Abiraterone acetate. This product is intended for research and analytical applications. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).

D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.

Abiraterone decanoate is a potent Abiraterone proagent. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery.

Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC₅₀=69 nM) and an AR antagonist. Seviteronel demonstrates both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.

Lapiteronel (CFG920) is an orally active, nonsteroidal, reversible dual CYP17 and CYP11B2 inhibitor. Lapiteronel has the potential for metastatic castration-resistant prostate cancer research.

Pentacosafluorotridecanoic Acid (PFTrDA) is a long-chain perfluoroalkyl carboxylic acid with strong endocrine-disrupting activity. Pentacosafluorotridecanoic Acid exhibits estrogenic effects and disrupts vtg1 transcription as well as sex hormone homeostasis in male Danio rerio. Pentacosafluorotridecanoic Acid disturbs steroidogenesis and HPG axis function in a sex-dependent pattern. Pentacosafluorotridecanoic Acid inhibits CYP17A and CYP11A1 to reduce testosterone and increase E2/T ratio in H295R cells. Pentacosafluorotridecanoic Acid triggers gender-specific immunomodulation after prenatal exposure. Pentacosafluorotridecanoic Acid correlates with lower eczema risk in female infants. Pentacosafluorotridecanoic Acid can be used for the research of endocrine disruption and eczema.

ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC₅₀s of 80 nM and 22 nM, respectively.

CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC₅₀s of 15.8 and 20.1 nM.

CYP17A1-IN-1 (Compound 14) is the inhibitor for CYP17A1 with an IC₅₀ of 26 nM. CYP17A1-IN-1 exhibits cytotoxicity in androgen-sensitive prostate cancer cell LNCaP, inhibits the migration of cell DU-145.

Galeterone (TOK-001) hydrochloride is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC₅₀ = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research^[1][2].

Pentacosafluorotridecanoic Acid (Standard) is the analytical standard of Pentacosafluorotridecanoic Acid (PFTrDA) (HY-W679754). This product is intended for research and analytical applications.Pentacosafluorotridecanoic Acid is a long-chain perfluoroalkyl carboxylic acid with strong endocrine-disrupting activity. Pentacosafluorotridecanoic Acid exhibits estrogenic effects and disrupts vtg1 transcription as well as sex hormone homeostasis in male Danio rerio. Pentacosafluorotridecanoic Acid disturbs steroidogenesis and HPG axis function in a sex-dependent pattern. Pentacosafluorotridecanoic Acid inhibits CYP17A and CYP11A1 to reduce testosterone and increase E2/T ratio in H295R cells. Pentacosafluorotridecanoic Acid triggers gender-specific immunomodulation after prenatal exposure. Pentacosafluorotridecanoic Acid correlates with lower eczema risk in female infants. Pentacosafluorotridecanoic Acid can be used for the research of endocrine disruption and eczema.