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Tamoxifen

Catalog No.
B5965
estrogen receptor modulator
Grouped product items
SizePriceStock Qty
1g
$65.00
In stock
5g
$234.00
In stock
10g
$328.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

Tamoxifen (CAS 10540-29-1) is an orally bioavailable selective estrogen receptor modulator (SERM), functioning as an estrogen antagonist in breast tissue and exhibiting agonist activity in bone, liver, and uterine tissues. Additionally, tamoxifen acts as an activator of heat shock protein 90 (Hsp90), enhancing its ATPase chaperone function. In antiviral assays, tamoxifen inhibits Ebola virus (EBOV Zaire) and Marburg virus (MARV) replication with IC50 values of 0.1 μM and 1.8 μM, respectively. It can also induce cellular autophagy and apoptosis. In genetic studies, tamoxifen is widely utilized to trigger CreER-mediated gene knockout in engineered mouse models.

References:
[1] Rohlff C, Blagosklonny MV, Kyle E, Kesari A, Kim IY, Zelner DJ, Hakim F, Trepel J, Bergan RC.  Prostate cancer cell growth inhibition by tamoxifen is associated with inhibition of protein kinase C and induction of p21(waf1/cip1). Prostate. 1998 Sep 15;37(1):51-9.
[2] Jann N.  Sarkaria, David F. C. Gibson, V. Craig Jordan, John F. Fowler, Mary J. Lindstrom, and
R.  Timothy Mulcahy. Tamoxifen-induced Increase in the Potential Doubling Time of MCF-7 Xenografts as Determined by Bromodeoxyuridine Labeling and Flow Cytometry. CANCER RESEARCH 5.1. 4413-1417, September 15, 1993.
[3] Osborne CK.  Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt371.51
Cas No.10540-29-1
FormulaC26H29NO
Solubility≥18.6 mg/mL in DMSO; insoluble in H2O; ≥85.9 mg/mL in EtOH
Chemical Name2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]-N,N-dimethyl-ethanamine
SDFDownload SDF
Canonical SMILESCC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(C)C)C=C2)\C3=CC=CC=C3
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

PC3 and PC3-M prostate carcinoma cells, DU-145 cells

Preparation method

The solubility of this compound in DMSO is >18.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 μM, 3 days

Applications

In PC3-M cells, treatment with tamoxifen for 3days dose-dependently inhibited cell growth. Tamoxifen (10 μM) inhibited protein kinase C activity in PC3-M cells. Tamoxifen and TGF-β showed additive effects upon thymidine uptake in PC3-M cells. Cytosolic Rb protein decreased 12 hr after treatment with tamoxifen, continuing to decline for at least 24 hr. In the nucleus, the phosphorylated form of Rb disappeared between 12–24 hr after treatment with tamoxifen.

Animal experiment [2]:

Animal models

Ovariectomized nude mice bearing MCF-7 xenografts

Dosage form

21 days

Application

Treatment with TAM resulted in a slowing of tumor growth (tumor doubling time, 12 days), a significant increase in Tpot to 6.6 days, and a decrease in %LI to 8% by 23 days posttreatment. TAM treatment significantly decreased tumor cell proliferation in MCF-7 xenografts.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Rohlff C, Blagosklonny M V, Kyle E, et al. Prostate cancer cell growth inhibition by tamoxifen is associated with inhibition of protein kinase C and induction of p21waf1/cip1[J]. The Prostate, 1998, 37(1): 51-59.

[2]. Sarkaria J N, Gibson D F C, Jordan V C, et al. Tamoxifen-induced increase in the potential doubling time of MCF-7 xenografts as determined by bromodeoxyuridine labeling and flow cytometry[J]. Cancer research, 1993, 53(18): 4413-4417.

Quality Control

Quality Control & MSDS

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Chemical structure

Tamoxifen

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