Tamoxifen

Biological Activity

Tamoxifen is an orally active, selective estrogen receptor partial agonist/antagonist. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen exhibits antiestrogenic effects in mammary tissue and estrogen-like effects in bone. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.

Product Citations

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  EMBO Mol Med. 2023 Dec.

  MYSM1 acts as a novel co-activator of ERα to confer antiestrogen resistance in breast cancer
  Tamoxifen purchased from AbMole

• 

  Biomater Adv. 2023 Mar;146:213301.

  Breast cancer cells interact with tumor-derived extracellular matrix in a molecular subtype-specific manner
  Tamoxifen purchased from AbMole

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  Nature. 2020 Dec;588(7839):664-669.

  Creation of bladder assembloids mimicking tissue regeneration and cancer
  Tamoxifen purchased from AbMole

Chemical Information

Molecular Weight	371.51
Formula	C26H29NO
CAS Number	10540-29-1
Solubility (25°C)	DMSO 30 mg/mL Ethanol 40 mg/mL
Storage	-20°C, protect from light

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Susanne Feil, et al. Methods Mol Biol. Inducible Cre mice

[2] Forbes, et al. J Med Chem. N-(1-Methyl-5-indolyl)-N'-(3-pyridyl)urea hydrochloride: the first selective 5-HT_1C receptor antagonist.