| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In HepG2 cells, Ro 48-8071 dose-dependently decreases cholesterol production with an IC50 value of around 1.5 nM [1]. Ro 48-8071 (10 μM) dramatically lowers the viability of PC-3 prostate cancer cells but not of normal prostate cells. Ro 48-8071 (10-30 μM) causes apoptosis in LNCaP and C4-2 cell lines in a dose-dependent manner. Castration-resistant PC-3 and DU145 cells also demonstrated considerable levels of apoptosis following 24 hours of treatment with Ro 48-8071. Ro 48-8071 (10-25 μM) decreases AR protein expression in a dose-dependent manner. Ro 48-8071 (0.1-1 μM) stimulates ERβ protein expression in a dose-dependent manner in hormone-dependent LNCaP and castration-resistant PC-3 cells [2]. Using mammalian cells designed to express human ERα or ERβ proteins, coupled with the ER-responsive luciferase promoter, Ro 48-8071 dose-dependently suppresses 17β-estradiol (E2)-induced ERα-responsive luciferase activity (IC50, around 10 µM), lower than non-toxic circumstances for cells [3].
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|---|---|
| ln Vivo |
In hamsters, Ro 48-8071 decreased HDL-C at all doses but decreased LDL-C by about 60% at 150 μmol/kg per day and up to 300 μmol/kg per day. The amount of MOS in hamster liver is increased by Ro 48-8071 (≥00 μmol/kg daily). In hamsters, Ro 48-8071 (300 μmol/kg daily) dramatically lowers VLDL secretion [1]. Without causing weight loss, Ro 48-8071 (5 or 20 mg/kg) dramatically slowed the growth of tumors in mice. Additionally, two of the twelve tumors that were observed in mice during the testing period were totally eradicated by Ro 48-8071 at a dosage of 20 mg/kg [2]. In the entire small intestine of BALB/c mice, Ro 48-8071 (20 mg/day/kg body weight) rapidly and sustainably inhibits cholesterol synthesis (>50%). Additionally, the stomach and large intestine produce less cholesterol [4].
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| References |
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| Additional Infomation |
Ro 48-8071 is an aromatic ketone that is 2-fluoro-4'-bromobenzophenone in which the hydrogen at position 4 (meta to the fluoro group) is replaced by a 6-[methyl(prop-2-en-1-yl)amino]hexyl}oxy group. An inhibitor of lanosterol synthase. It has a role as an EC 5.4.99.7 (lanosterol synthase) inhibitor and an antineoplastic agent. It is an aromatic ketone, an aromatic ether, a member of monofluorobenzenes, a member of bromobenzenes, a tertiary amino compound and an olefinic compound. It is functionally related to a benzophenone. It is a conjugate base of a Ro 48-8071(1+).
|
| Molecular Formula |
C23H27NO2FBR
|
|---|---|
| Molecular Weight |
448.36838
|
| Exact Mass |
447.12
|
| CAS # |
161582-11-2
|
| Related CAS # |
Ro 48-8071 fumarate;189197-69-1
|
| PubChem CID |
1949
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
522.8±50.0 °C at 760 mmHg
|
| Flash Point |
270.0±30.1 °C
|
| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.550
|
| LogP |
6.24
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
28
|
| Complexity |
468
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=CC=C(Br)C=C1)C2=CC=C(OCCCCCCN(C)CC=C)C=C2F
|
| InChi Key |
CMYCCJYVZIMDFU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H27BrFNO2/c1-3-14-26(2)15-6-4-5-7-16-28-20-12-13-21(22(25)17-20)23(27)18-8-10-19(24)11-9-18/h3,8-13,17H,1,4-7,14-16H2,2H3
|
| Chemical Name |
(4-bromophenyl)-[2-fluoro-4-[6-[methyl(prop-2-enyl)amino]hexoxy]phenyl]methanone
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2303 mL | 11.1515 mL | 22.3030 mL | |
| 5 mM | 0.4461 mL | 2.2303 mL | 4.4606 mL | |
| 10 mM | 0.2230 mL | 1.1152 mL | 2.2303 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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