Ro 48-8071 free base
Based on 13 publication(s) in Google Scholar
Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
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- CAS No.: 161582-11-2
- Formule: C23H27BrFNO2
- Masse moléculaire:448.37
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Stockage:
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Ro 48-8071 free base
More- Cancer Cell. 2023 Jul 10;41(7):1276-1293.e11. [Abstract]
- Nat Commun. 2023 Jul 17;14(1):4267. [Abstract]
- Mol Cell. 2021 Jul 1;81(13):2736-2751.e8. [Abstract]
- Cell Death Dis. 2021 May 13;12(5):482. [Abstract]
- Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]
- Sci China Life Sci. 2022 Feb;65(2):341-361. [Abstract]
- Cell Rep. 2022 Dec 13;41(11):111827. [Abstract]
- Mol Med Rep. 2021 Dec;24(6):828. [Abstract]
- Neoplasia. 2025 Oct 27:70:101243. [Abstract]
- ACS Synth Biol. 2023 May 19;12(5):1408-1414. [Abstract]
- Cancer Res Commun. 2024 Sep 1;4(9):2427-2443. [Abstract]
- Immunomedicine. 2022 Dec;2(2):e1041. [Abstract]
- Oncotarget. 2017 Feb 28;8(9):14860-14875. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
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In Vivo Efficacy Study
Activité biologique
Description
IC50 & Target
IC50: appr 6.5 nM (Oxidosqualene cyclase)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
0.092 μM
Compound: Ro 48-8071
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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
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[PMID: 26745812] |
| HL-60 | IC50 |
8 μM
Compound: Ro 48-8071
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Cytotoxicity against human HL60 cells after 24 hrs by MTT assay
Cytotoxicity against human HL60 cells after 24 hrs by MTT assay
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[PMID: 23583910] |
| HL-60 | IC50 |
8 μM
Compound: Ro 48-8071
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Cytotoxicity against human HL60 cells after 24 hrs by MTT assay
Cytotoxicity against human HL60 cells after 24 hrs by MTT assay
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[PMID: 26745812] |
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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 161582-11-2
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Masse moléculaire 448.37
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Formule C23H27BrFNO2
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SMILES
O=C(C1=CC=C(Br)C=C1)C2=CC=C(OCCCCCCN(C)CC=C)C=C2F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (13)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Exhaustion-associated cholesterol deficiency dampens the cytotoxic arm of antitumor immunity. [Abstract]2023 Jul 10;41(7):1276-1293.e11. PMID: 37244259 -
Nat Commun
A polycistronic system for multiplexed and precalibrated expression of multigene pathways in fungi. [Abstract]2023 Jul 17;14(1):4267. PMID: 37460548 -
Mol Cell
The ZMYND8-regulated mevalonate pathway endows YAP-high intestinal cancer with metabolic vulnerability. [Abstract]2021 Jul 1;81(13):2736-2751.e8. PMID: 33932349 -
Cell Death Dis
Targeting epigenetic modulation of cholesterol synthesis as a therapeutic strategy for head and neck squamous cell carcinoma. [Abstract]2021 May 13;12(5):482. PMID: 33986254 -
Cell Death Discov
Inhibition of lanosterol synthase linking with MAPK/JNK signaling pathway suppresses endometrial cancer. [Abstract]2025 Feb 8;11(1):55. PMID: 39922821
Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]
The results of CCK8 reflected the IC50 of Ro 48-8071 (0-2 μM) in EC cells and that Ro 48-8071 significantly inhibited the proliferation of EC cells.
Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]
Clone formation and Transwell experiments showed that the activity of EC cells was significantly inhibited by Ro 48-8071 (0-1 μM).
Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]
Flow cytometry analysis found that Ro 48-8071 (0-1 μM) can promote the apoptosis of EC cells.
Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]
Ro 48-8071 (0-1 μM) reduces the expression of phosphorylated JNK protein.
Ro 48-8071 free base purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]
Images of isolated tumors from the subcutaneous tumor nude mice model established using Ishikawa cells treated with Ro 48-8071 or SP600125(n = 6 mice per group).
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Sci China Life Sci
2022 Feb;65(2):341-361. PMID: 34047913 -
Cell Rep
EGFR-phosphorylated GDH1 harmonizes with RSK2 to drive CREB activation and tumor metastasis in EGFR-activated lung cancer. [Abstract]2022 Dec 13;41(11):111827. PMID: 36516759 -
Mol Med Rep
Cholesterol biosynthesis inhibitor RO 48‑8071 inhibits pancreatic ductal adenocarcinoma cell viability by deactivating the JNK and ERK/MAPK signaling pathway. [Abstract]2021 Dec;24(6):828. PMID: 34590153 -
Neoplasia
Cholesterol biosynthesis as a drug-induced vulnerability in diffuse large B cell lymphoma insensitive to EZH2 inhibition. [Abstract]2025 Oct 27:70:101243. PMID: 41151153 -
ACS Synth Biol
2023 May 19;12(5):1408-1414. PMID: 36853024 -
Cancer Res Commun
2024 Sep 1;4(9):2427-2443. PMID: 39028932 -
Immunomedicine
Metabolic inhibitor screening identifies dihydrofolate reductase as an inducer of the tumor immune escape mediator CD24. [Abstract]2022 Dec;2(2):e1041. PMID: 36816458 -
Oncotarget
Disabled cell density sensing leads to dysregulated cholesterol synthesis in glioblastoma. [Abstract]2017 Feb 28;8(9):14860-14875. PMID: 28118603
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.
Protocole
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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