Ro 48-8071 fumarate

Name: Ro 48-8071 fumarate
Brand: MedChemExpress
SKU: HY-18630A
Rating: 5.0 (11 reviews)

Cat. No.: HY-18630A Purity: 99.42%: FAQs
Data Sheet SDS COA Handling Instructions

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Ro 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC₅₀ of appr 6.5 nM.

For research use only. We do not sell to patients.

Ro 48-8071 fumarate Chemical Structure

CAS No. : 189197-69-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 68	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 68	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 88	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Ro 48-8071 fumarate:

Ro 48-8071 Get quote

10 Publications Citing Use of MCE Ro 48-8071 fumarate

: Ro 48-8071 fumarate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14860-14875. [Abstract]; Cell death in TS600 glioma cells. Dead cells are visualized with SYTOX Orange 24 hours after treatment with DMSO (mock), 1 μM epirubicin, 10 μM clotrimazole, 5 μM ketoconazole, or 1 μM Ro 48-8071.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Ro 48-8071 fumarate is an inhibitor of OSC (Oxidosqualene cyclase) with IC₅₀ of appr 6.5 nM.

IC₅₀ & Target

IC50: appr 6.5 nM (Oxidosqualene cyclase)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	11.3 μM Compound: 2	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 22533316]
Caco-2	IC₅₀	2.99 μM Compound: 2	Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay	[PMID: 22533316]
HCEC	IC₅₀	3.8 μM Compound: 2	Cytotoxicity against human HCEC cells assessed as reduction in cell survival after 72 hrs by MTT assay Cytotoxicity against human HCEC cells assessed as reduction in cell survival after 72 hrs by MTT assay	[PMID: 22533316]
HeLa	IC₅₀	2.89 μM Compound: 2	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 22533316]
KB	IC₅₀	2.88 μM Compound: 2	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 22533316]
LN-18	IC₅₀	6.1 μM Compound: 2	Cytotoxicity against human LN18 cells assessed as reduction in cell survival after 72 hrs by MTT assay Cytotoxicity against human LN18 cells assessed as reduction in cell survival after 72 hrs by MTT assay	[PMID: 22533316]
LN-229	IC₅₀	8.8 μM Compound: 2	Cytotoxicity against human LN229 cells assessed as reduction in cell survival after 72 hrs by MTT assay Cytotoxicity against human LN229 cells assessed as reduction in cell survival after 72 hrs by MTT assay	[PMID: 22533316]
LNCaP	IC₅₀	> 30 μM Compound: 2	Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay	[PMID: 22533316]
MCF7	IC₅₀	6.77 μM Compound: 2	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 22533316]
OVCAR	IC₅₀	> 30 μM Compound: 2	Cytotoxicity against human OVCAR cells after 72 hrs by MTT assay Cytotoxicity against human OVCAR cells after 72 hrs by MTT assay	[PMID: 22533316]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

564.44

Formula

C₂₇H₃₁BrFNO₆

CAS No.

189197-69-1

Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC=C(Br)C=C1)C2=CC=C(OCCCCCCN(C)CC=C)C=C2F.O=C(O)/C=C/C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (177.17 mM; Need ultrasonic)

DMSO : ≥ 55 mg/mL (97.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7717 mL	8.8583 mL	17.7167 mL
5 mM	0.3543 mL	1.7717 mL	3.5433 mL
10 mM	0.1772 mL	0.8858 mL	1.7717 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 12.5 mg/mL (22.15 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.42%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (245 KB) RP-HPLC (247 KB)

Handling Instructions (2659 KB)

References

[1]. Morand OH, et al. Ro 48-8.071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: comparison to simvastatin. J Lipid Res. 1997 Feb;38(2):373-90. [Content Brief]

[2]. Liang Y, et al. Cholesterol biosynthesis inhibitor RO 48-8071 suppresses growth of hormone-dependent and castration-resistant prostate cancer cells. Onco Targets Ther. 2016 May 30;9:3223-32 [Content Brief]

[3]. Liang Y, et al. Cholesterol biosynthesis inhibitors as potent novel anti-cancer agents: suppression of hormone-dependent breast cancer by the oxidosqualene cyclase inhibitor RO 48-8071. Breast Cancer Res Treat. 2014 Jul;146(1):51-62. [Content Brief]

[4]. Chuang JC, et al. Sustained and selective suppression of intestinal cholesterol synthesis by Ro 48-8071, an inhibitor of 2,3-oxidosqualene:lanosterol cyclase, in the BALB/c mouse. Biochem Pharmacol. 2014 Apr 1;88(3):351-63. [Content Brief]

Animal Administration
^[2]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Morand OH, et al. Ro 48-8.071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: comparison to simvastatin. J Lipid Res. 1997 Feb;38(2):373-90. [Content Brief]

[2]. Liang Y, et al. Cholesterol biosynthesis inhibitor RO 48-8071 suppresses growth of hormone-dependent and castration-resistant prostate cancer cells. Onco Targets Ther. 2016 May 30;9:3223-32 [Content Brief]

[3]. Liang Y, et al. Cholesterol biosynthesis inhibitors as potent novel anti-cancer agents: suppression of hormone-dependent breast cancer by the oxidosqualene cyclase inhibitor RO 48-8071. Breast Cancer Res Treat. 2014 Jul;146(1):51-62. [Content Brief]

[4]. Chuang JC, et al. Sustained and selective suppression of intestinal cholesterol synthesis by Ro 48-8071, an inhibitor of 2,3-oxidosqualene:lanosterol cyclase, in the BALB/c mouse. Biochem Pharmacol. 2014 Apr 1;88(3):351-63. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.7717 mL	8.8583 mL	17.7167 mL	44.2917 mL
	5 mM	0.3543 mL	1.7717 mL	3.5433 mL	8.8583 mL
	10 mM	0.1772 mL	0.8858 mL	1.7717 mL	4.4292 mL
	15 mM	0.1181 mL	0.5906 mL	1.1811 mL	2.9528 mL
	20 mM	0.0886 mL	0.4429 mL	0.8858 mL	2.2146 mL
	25 mM	0.0709 mL	0.3543 mL	0.7087 mL	1.7717 mL
	30 mM	0.0591 mL	0.2953 mL	0.5906 mL	1.4764 mL
	40 mM	0.0443 mL	0.2215 mL	0.4429 mL	1.1073 mL
	50 mM	0.0354 mL	0.1772 mL	0.3543 mL	0.8858 mL
	60 mM	0.0295 mL	0.1476 mL	0.2953 mL	0.7382 mL
	80 mM	0.0221 mL	0.1107 mL	0.2215 mL	0.5536 mL
H₂O	100 mM	0.0177 mL	0.0886 mL	0.1772 mL	0.4429 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.