Megestrol
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 584778

CAS#: 3562-63-8

Description: Megestrol is a progestational hormone used most commonly as the acetate ester in the palliative treatment of breast cancer..


Chemical Structure

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Megestrol
CAS# 3562-63-8

Theoretical Analysis

MedKoo Cat#: 584778
Name: Megestrol
CAS#: 3562-63-8
Chemical Formula: C22H30O3
Exact Mass: 342.22
Molecular Weight: 342.479
Elemental Analysis: C, 77.16; H, 8.83; O, 14.01

Price and Availability

Size Price Availability Quantity
100mg USD 150 2 Weeks
200mg USD 250 2 Weeks
500mg USD 450 2 Weeks
1g USD 750 2 Weeks
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Related CAS #: 595-33-5 (acetate)   3562-63-8  

Synonym: Megestrol

IUPAC/Chemical Name: Pregna-4,6-diene-3,20-dione, 17-hydroxy-6-methyl-

InChi Key: VXIMPSPISRVBPZ-NWUMPJBXSA-N

InChi Code: InChI=1S/C22H30O3/c1-13-11-16-17(20(3)8-5-15(24)12-19(13)20)6-9-21(4)18(16)7-10-22(21,25)14(2)23/h11-12,16-18,25H,5-10H2,1-4H3/t16-,17+,18+,20-,21+,22+/m1/s1

SMILES Code: CC([C@@]1(O)CC[C@@]2([H])[C@]3([H])C=C(C)C4=CC(CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 342.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Sharifzadeh F, Aminimoghaddam S, Kashanian M, Fazaeli M, Sheikhansari N. A comparison between the effects of metformin and megestrol on simple endometrial hyperplasia. Gynecol Endocrinol. 2017 Feb;33(2):152-155. doi: 10.1080/09513590.2016.1223285. Epub 2016 Sep 30. PubMed PMID: 27690687.

2: Stiles J, Coster M. Use of an ophthalmic formulation of megestrol acetate for the treatment of eosinophilic keratitis in cats. Vet Ophthalmol. 2016 Jul;19 Suppl 1:86-90. doi: 10.1111/vop.12371. Epub 2016 Mar 3. PubMed PMID: 26938779.

3: Nanjappa S, Thai C, Shah S, Snyder M. Pharmacy Report: Megestrol Acetate-Induced Adrenal Insufficiency. Cancer Control. 2016 Apr;23(2):167-9. PubMed PMID: 27218795.

4: Guk J, Son H, Chae DW, Park K. Quantitative Assessment of Food Effect on the Pharmacokinetics of Nano-Crystallized Megestrol Acetate. Basic Clin Pharmacol Toxicol. 2017 Mar;120(3):270-277. doi: 10.1111/bcpt.12677. Epub 2016 Nov 4. PubMed PMID: 27639080.

5: Smith CS, Logomarsino JV. Using megestrol acetate to ameliorate protein-energy wasting in chronic kidney disease. J Ren Care. 2016 Mar;42(1):53-9. doi: 10.1111/jorc.12138. Epub 2015 Nov 5. Review. PubMed PMID: 26537025.

6: Guida M, Di Carlo C, Troisi J, Gallo A, Cibarelli F, Martini E, Tiranini L, Nappi RE. The sexuological impact of hormonal contraceptives based on their route of administration. Gynecol Endocrinol. 2017 Mar;33(3):218-222. doi: 10.1080/09513590.2016.1249841. Epub 2016 Dec 2. PubMed PMID: 27908210.

7: Chae DW, Son H, Guk J, Park C, Park K. Pharmacokinetics of a nanocrystal-containing megestrol acetate formulation: a single-dose, randomized, open-label, 2-part, 2-period crossover study in healthy Korean subjects. Int J Clin Pharmacol Ther. 2016 Sep;54(9):698-704. doi: 10.5414/CP202574. PubMed PMID: 27191767.

8: Ha ES, Kim JS, Baek IH, Yoo JW, Jung Y, Moon HR, Kim MS. Development of megestrol acetate solid dispersion nanoparticles for enhanced oral delivery by using a supercritical antisolvent process. Drug Des Devel Ther. 2015 Aug 4;9:4269-77. doi: 10.2147/DDDT.S90706. eCollection 2015. PubMed PMID: 26345723; PubMed Central PMCID: PMC4531043.

9: Seo YD, Jin SE, Kim D, Lee DH, Yang SG. Fabrication of Eudragit polymeric nanoparticles using ultrasonic nebulization method for enhanced oral absorption of megestrol acetate. Pharm Dev Technol. 2018 Apr;23(4):407-413. doi: 10.1080/10837450.2017.1400049. Epub 2017 Nov 20. PubMed PMID: 29095656.

10: Jang K, Yoon S, Kim SE, Cho JY, Yoon SH, Lim KS, Yu KS, Jang IJ, Lee H. Novel nanocrystal formulation of megestrol acetate has improved bioavailability compared with the conventional micronized formulation in the fasting state. Drug Des Devel Ther. 2014 Jun 25;8:851-8. doi: 10.2147/DDDT.S62176. eCollection 2014. PubMed PMID: 25028536; PubMed Central PMCID: PMC4077389.

11: Greig CA, Johns N, Gray C, MacDonald A, Stephens NA, Skipworth RJ, Fallon M, Wall L, Fox GM, Fearon KC. Phase I/II trial of formoterol fumarate combined with megestrol acetate in cachectic patients with advanced malignancy. Support Care Cancer. 2014 May;22(5):1269-75. doi: 10.1007/s00520-013-2081-3. Epub 2014 Jan 4. PubMed PMID: 24389826.

12: Zoely: a new combined oral contraceptive. Drug Ther Bull. 2014 Aug;52(8):90-3. doi: 10.1136/dtb.2014.8.0270. Epub 2014 Aug 7. Review. PubMed PMID: 25104773.

13: Nair SG, Patel DP, Sanyal M, Singhal P, Shrivastav PS. Ultra-performance liquid chromatography-tandem mass spectrometry assay for determination of plasma nomegestrol acetate and estradiol in healthy postmenopausal women. Biomed Chromatogr. 2018 Feb;32(2). doi: 10.1002/bmc.4086. Epub 2017 Sep 19. PubMed PMID: 28869284.

14: Li F, Zou XJ, Zheng H, Xiang Y. LC-MS/MS method for determination of megestrol in human plasma and its application in bioequivalence study. J Huazhong Univ Sci Technolog Med Sci. 2013 Dec;33(6):912-916. doi: 10.1007/s11596-013-1221-9. Epub 2013 Dec 13. PubMed PMID: 24337858.

15: Kim YH, Choi HY, Jin S, Noh YH, Kim MJ, Park HJ, Lim HS, Bang K, Lee SH, Bae KS. Tolerability and pharmacokinetics of two formulations of megestrol acetate under fed conditions in healthy volunteers. Clin Ther. 2015 Feb 1;37(2):439-47. doi: 10.1016/j.clinthera.2014.09.022. Epub 2014 Oct 23. PubMed PMID: 25450470.

16: Li Y, Song CK, Kim MK, Lim H, Shen Q, Lee DH, Yang SG. Nanomemulsion of megestrol acetate for improved oral bioavailability and reduced food effect. Arch Pharm Res. 2015 Oct;38(10):1850-6. doi: 10.1007/s12272-015-0604-9. Epub 2015 Apr 18. PubMed PMID: 25893430.

17: Lachowicz M, Kołodziejczyk M, Lukosek M, Kosno J, Olszewska P, Szyma Nski P. New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate. Molecules. 2016 Feb 6;21(2). pii: E197. doi: 10.3390/molecules21020197. PubMed PMID: 26861275; PubMed Central PMCID: PMC6273346.

18: Loprinzi CL, Johnson PA, Jensen M. Megestrol acetate for anorexia and cachexia. Oncology. 1992;49 Suppl 2:46-9. PubMed PMID: 1461628.

19: Greenberg M, Lawler D, Zawistowski S, Jöchle W. Low-dose megestrol acetate revisited: a viable adjunct to surgical sterilization in free roaming cats? Vet J. 2013 Jun;196(3):304-8. doi: 10.1016/j.tvjl.2013.01.038. Epub 2013 Mar 14. Review. PubMed PMID: 23499239.

20: Canetta R, Florentine S, Hunter H, Lenaz L. Megestrol acetate. Cancer Treat Rev. 1983 Sep;10(3):141-57. Review. PubMed PMID: 6352021.