Ro 48-8071 free base

製品番号: HY-18630: Data Sheet 取扱説明書
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Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC₅₀ of appr 6.5 nM.

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CAS 番号 : 161582-11-2

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Other 在庫あり Forms of Ro 48-8071 free base:

Ro 48-8071

Other Forms of Ro 48-8071 free base:

Ro 48-8071 在庫あり

顧客検証

: Ro 48-8071 free base 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.

Estrogen Receptor/ERR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

生物活性
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純度とドキュメンテーション
参考文献
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製品説明

Ro 48-8071 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
HL-60	IC₅₀	0.092 μM Compound: Ro 48-8071	Inhibition of total cholesterol biosynthesis in human HL60 cells assessed as incorporation of 2-13C-acetate by GC-MS analysis Inhibition of total cholesterol biosynthesis in human HL60 cells assessed as incorporation of 2-13C-acetate by GC-MS analysis	[PMID: 26745812]
HL-60	IC₅₀	8 μM Compound: Ro 48-8071	Cytotoxicity against human HL60 cells after 24 hrs by MTT assay Cytotoxicity against human HL60 cells after 24 hrs by MTT assay	[PMID: 23583910]
HL-60	IC₅₀	8 μM Compound: Ro 48-8071	Cytotoxicity against human HL60 cells after 24 hrs by MTT assay Cytotoxicity against human HL60 cells after 24 hrs by MTT assay	[PMID: 26745812]

体外実験

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.

体内実験

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.

分子量

448.37

分子式

C₂₃H₂₇BrFNO₂

CAS 番号

161582-11-2

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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]

動物実験
^[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.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。

参考文献

[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]