Megestrol Acetate

Catalog No.S1304 Synonyms: BDH1298, SC10363

Megestrol Acetate Chemical Structure

Molecular Weight(MW): 384.51

Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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2 Customer Reviews

  • HEC-1A cells were treated with pterostilbene (75 μM), megestrol acetate (75 μM) or the combination for 24 h. Whole cell lysates were collected and measured for the change of cell cycle and apoptosis pathways by Western blot. Results are representative of 3 or more preparations.

    Sci Rep, 2017, 7(1):12754. Megestrol Acetate purchased from Selleck.

    Kaempferol and ER/PR inhibitor suppress the migration and Rho activity of MCF-7 cells. Notes: (A) MCF-7 ER+/PR+ breast cancer cells were allowed to migrate in response to 20 μmol/L kaempferol and/or 0.1 nmol/L AZD9496 (ER inhibitor) and 200 μmol/L megestrol acetate (PR inhibitor) for 6 h. Results are presented as mean ± SD of 5 independent experiments. (B, C) MCF-7 cells were incubated with 20 μmol/L kaempferol and/or 0.1 nmol/L AZD9496 and 200 μmol/L MA for 1 h, and then subjected to the RhoA (B) and Rac1 (C) activity assays. The relative levels of Rho activity were normalized to the average value of controls. Results are presented as mean ± SD of 3 independent experiments. Abbreviations: AZD, AZD9496; Ctrl, control; ER, estrogen receptor; MA, megestrol acetate; ns, no significance; PR, progesterone receptor.

    Onco Targets Ther, 2017, 10:4809-4819. Megestrol Acetate purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Megestrol acetate is a synthetic progestogen, used to treat breast cancer and loss of appetite.
Targets
progestogen Receptor [1] Androgen Receptor [1]
In vitro

Megestrol acetate inhibits the expression of cytoplasmic aromatase through nuclear C/EBPβ in reperfusion injury-induced ischemic rat hippocampus. [1] Megestrol acetate significantly increases the proliferation, migration, and adipogenic differentiation of adipose-derived stem cells (ASCs) in a dose-dependent manner. Megestrol acetate also upregulates genes downstream of glucocorticoid receptor (GR) in ASCs. [2]

In vivo Megestrol acetate significantly decreases the circulating concentrations of estradiol (E2) and testosterone (T) in female fish or 11-ketotestosterone (11-KT) in male fish. Megestrol acetate exposure significantly downregulates the transcription of certain genes along the hypothalamic-pituitary-gonadal (HPG) axis. [3] Megestrol acetate produces a progressive deterioration in glucose tolerance, with a significant increase in mean fasting plasma glucose concentrations and decrease in mean plasma glucose clearance rates after 6 months and 12 months of treatment in cats. Megestrol acetate also produces a progressive decrease in both resting plasma cortisol concentrations and cortisol concentrations after ACTH stimulation in cats. [4] Megestrol acetate (50 mg/kg/day) for 9 days significantly increases food and water intake compared with untreated controls. Megestrol acetate (50 mg/kg/day) significantly (90-140%) increases in neuropeptide Y concentrations in the arcuate nucleus (where neuropeptide Y is synthesized), in the lateral hypothalamic area (through which arcuate neurones project) and in the medial preoptic area, ventromedial nucleus and dorsomedial nucleus in rats. [5]

Protocol

Solubility (25°C)

In vitro DMSO 33 mg/mL (85.82 mM)
Ethanol 15 mg/mL (39.01 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 384.51
Formula

C24H32O4

CAS No. 595-33-5
Storage powder
Synonyms BDH1298, SC10363

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03024580 Not yet recruiting Breast Neoplasm Instituto Nacional de Cancer, Brazil|Cancer Research UK Cambridge Institute March 2017 Phase 2
NCT02619266 Recruiting Anorexia|Cancer Cachexia Xinqiao Hospital of Chongqing|Chengdu University of Traditional Chinese Medicine December 2015 Phase 2|Phase 3
NCT02595723 Completed Cognitive Impairment University of Texas Southwestern Medical Center|The Rogosin Institute July 2015 Early Phase 1
NCT02980653 Recruiting Head and Neck Cancer TTY Biopharm|Chang Gung Memorial Hospital May 2015 Phase 2
NCT02269670 Active, not recruiting Estrogen Receptor-positive Breast Cancer|HER2-negative Breast Cancer|Progesterone Receptor-positive Breast Cancer|Recurrent Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Emory University|Novartis November 2014 Phase 2
NCT01943058 Withdrawn Atypical Endometrial Hyperplasia|Endometrial Adenocarcinoma|Recurrent Endometrial Carcinoma|Stage IA Endometrial Carcinoma|Stage IB Endometrial Carcinoma|Stage II Endometrial Carcinoma|Stage IIIA Endometrial Carcinoma|Stage IIIB Endometrial Carcinoma|Stage IIIC Endometrial Carcinoma|Stage IVA Endometrial Carcinoma|Stage IVB Endometrial Carcinoma University of Southern California|National Cancer Institute (NCI) March 2014 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID