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 fumarate

Ro 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	Signaling Pathways >> Others >> Others Research Areas >> Cancer
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	[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. [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. [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. [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.

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)

DC Chemicals Limited
China
Product Name: Ro 48-8071 fumarate
Price: $420.0/100mg $825.0/250mg $1500.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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Price: $75/10mM*1mLinDMSO

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Ro 48-8071 fumarate

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