Exemestane (FCE 24304) - Moligand™, 10mM in DMSO , Cytochrome P450 19A1 inhibitor, CAS No.107868-30-4, Cytochrome P450 19A1 inhibitor

CAS: 107868-30-4 Cat. No.: E409085 Fórmula: C₂₀H₂₄O₂ Peso molecular: 296.403 Número EC: 643-090-2

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

PNU155971 | 6-​methylene-androsta-​1,​4-​diene-​3,​17-​dione

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Exemestane (FCE 24304) Exemestane (FCE24304, PNU155971) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
In vitro

Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [³H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM. Exemestane (1 μM) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells. Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells.

In vivo

Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats. Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors.
Cell Data

cell lines：

Concentrations：1 μM

Incubation Time：24 hours

Powder Purity:≥99%

Specifications

Sinónimos

PNU155971 | 6-​methylene-androsta-​1,​4-​diene-​3,​17-​dione

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Exemestane (FCE24304, PNU155971) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Cytochrome P450 19A1 inhibitor

Propiedades del producto

• ALogP: 3.1

Nombres e identificadores

• Isómeros SMILES: C[C@]12CC[C@H]3[C@H]([C@@H]1CCC2=O)CC(=C)C4=CC(=O)C=C[C@]34C
• WGK Alemania: 3
• Peso molecular: 296.403
• Reaxy-Rn: 14613973
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14613973&ln=

Objetivos asociados (humanos)

CYP19A1 Tclin Aromatase (11 Activities)

Discover Target: CYP19A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)