Ro 48-8071 fumarate
Modify Date: 2024-01-02 17:00:14
Ro 48-8071 fumarate structure
|
Common Name | Ro 48-8071 fumarate | ||
|---|---|---|---|---|
| CAS Number | 189197-69-1 | Molecular Weight | 564.44 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 522.8±50.0 °C at 760 mmHg | |
| Molecular Formula | C27H31BrFNO6 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 270.0±30.1 °C | |
Use of Ro 48-8071 fumarateRo 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM. |
| Name | Ro 48-8071 |
|---|---|
| Synonym | More Synonyms |
| Description | Ro 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM. |
|---|---|
| Related Catalog | |
| Target |
IC50: appr 6.5 nM (Oxidosqualene cyclase)[1] |
| In Vitro | In HepG2 cells, Ro 48-8071 reduces cholesterol synthesis dose dependently with an IC50 value of appr 1.5 nM[1]. Ro 48-8071 (10 μM) significantly reduces the viability of PC-3 prostate cancer cells, but not normal prostate cells. Ro 48-8071 (10-30 μM) induces apoptosis of both LNCaP and C4-2 cell lines in a dose-dependent manner. And castration-resistant PC-3 and DU145 cells also demonstrate significant levels of apoptosis following 24-hour treatment with Ro 48-8071. Ro 48-8071 (10-25 μM) reduces AR protein expression in a dose-dependent manner. Ro 48-8071 (0.1-1 μM) increases ERβ protein expression dose-dependently in both hormone-dependent LNCaP and castration-resistant PC-3 cells[2]. Using mammalian cells engineered to express human ERα or ERβ protein, together with an ER-responsive luciferase promoter, Ro 48-8071 dose-dependently inhibits 17β-estradiol (E2)-induced ERα responsive luciferase activity (IC50, appr 10 µM), under conditions that are non-toxic to the cells[3]. |
| In Vivo | Ro 48-8071 lowers LDL-C maximally appr 60% at 150 μmol/kg per day, with no further reduction up to 300 μmol/kg per day, leaving HDL-C unchanged at all doses in hamsters. Ro 48-8071 (≥00 μmol/kg per day) increases the amount of MOS in liver of hamsters. Ro 48-8071 (300 μmol/kg per day) remarkedly and significantly reduces VLDL secretion of hamsters[1]. Ro 48-8071 (5 or 20 mg/kg) significantly reduces in vivo tumor growth in mice, without weight loss of the mice. Furthermore, Ro 48-8071 at a concentration of 20 mg/kg, completely eradicates two of the 12 tumors being monitored in the mice in the timeframe tested[2]. Ro 48-8071 (20 mg/day/kg body weight) leads to a rapid and sustained inhibition (>50%) of cholesterol synthesis in the whole small intestine of BALB/c mice. Sterol synthesis is also reduced in the large intestine and stomach[4]. |
| Animal Admin | Six-week-old male athymic nude mice (nu/nu) weighing 20-22 g are used in the assay. Castration-resistant PC-3 cells (5×106 in 0.15 mL solution) are mixed with matrigel and RPMI-1640 medium (1/1, v/v) and injected subcutaneously into both flanks of each mouse (n=6 animals/group) and tumors allowed to develop. The tumors are measured twice per week with a digital caliper. Tumor volumes are calculated by the formula (L × W × H) × π/6. Drug treatment is started when tumor volumes reach appr 100 mm3. Mice are given daily tail vein injections of 0.1 mL solution of either 5 or 20 mg/kg Ro 48-8071 for 5 days. This is followed by an injection every other day for six additional treatments and then a final injection 2 hours prior to sacrifice. Control mice receive the same volume of phosphate-buffered saline on the same schedule. The animals are weighed and tumor volumes are measured twice weekly throughout the drug treatment period. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 522.8±50.0 °C at 760 mmHg |
| Molecular Formula | C27H31BrFNO6 |
| Molecular Weight | 564.44 |
| Flash Point | 270.0±30.1 °C |
| LogP | 6.24 |
| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
| Index of Refraction | 1.550 |
| Storage condition | 2-8℃ |
| Methanone, (4-bromophenyl)(2-fluoro-4-((6-(methyl-2-propenylamino)hexyl)oxy)phenyl)- |
| [4-({6-[Allyl(methyl)amino]hexyl}oxy)-2-fluorophenyl](4-bromophenyl)methanone |
| Methanone, (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]- |
| Ro 48-8071 fumarate |
| Ro 48-8071 (fumarate) |