Tamoxifen CitrateAn antiestrogen with potent anti-cancer and PKC inhibitory activities

Tamoxifen Citrate (CAS 54965-24-1)

Tamoxifen Citrate | CAS 54965-24-1 is rated 5.0 out of 5 by 1.
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Application: An antiestrogen with potent anti-cancer and PKC inhibitory activities
CAS Number: 54965-24-1
Purity: >99%
Molecular Weight: 563.7
Molecular Formula: C32H37NO8
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Tamoxifen Citrate is a potent and selective inhibitor of PKC (protein kinase C). It is known that Tamoxifen Citrate functions in PKC ε translocation. Studies suggest that Tamoxifen Citrate functions as an estrogen receptor antagonist in breast tissue. Once bound to the estrogen receptor Tamoxifen Citrate will not allow any other ligand to bind to the receptor. In contrast, Tamoxifen Citrate is an agonist towards this receptor in tissues of the endometrium. Studies indicate Tamoxifen Citrate inhibits DNA synthesis and transcription by recruiting co-repressors, which stop estrogen from interacting with genes. When combined with PAX2, Tamoxifen Citrate can inhibit the proliferation of ERBB2. It is also a high affinity activator of the GPR30 receptor. Tamoxifen Citrate is an activator of Estrogen Receptor.


References

1. O'Brian, C.A., et al. 1985. Cancer Res. 45: 2462-2465. PMID: 3157445
2. Issandou, M., et al. 1990. Cancer Res. 50: 5845-5850. PMID: 2393853
3. Maccarrone, M., et al. 1998. FEBS Lett. 434: 421-424. PMID: 9742967
4. Mandlekar, S., et al. 2000. Cancer Res. 60: 5995-6000. PMID: 11085519

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in methanol (50 mg/ml with heat) or ethanol (10 mg/ml with sonication); very slightly soluble in water (0.3 mg/L @ 20°C; the pH is approximately 3.0-3.5), 0.02 N HCl (0.2 mg/ml @ 37°C)4, acetone ,chloroform,and DMSO(100mM)
Storage :
Store at 4° C
Melting Point :
140-142° C
Boiling Point :
482.3° C at 760 mmHg (Predicted)
IC50 :
Ishikawa : IC50 = 12.5 µM (human); DU-145 : IC50 = 15.25 µM (human); MDA-MB-231 : IC50 = 12.3 µM (human); MCF7: IC50 = 10.2 µM (human); PKC : IC50 = 10 µM
pK Values :
pKa: pK1: 8.85, pK2: 6.9 in in Triton® X-100, pKb: 8.69
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
KH2387000
PubChem CID :
2733525
Merck Index :
14: 9048
MDL Number :
MFCD00058321
EC Number :
259-415-2
Beilstein Registry :
5723042
SMILES :
CC/C(=C(\\C1=CC=CC=C1)/C2=CC=C(C=C2)OCCN(C)C)/C3=CC=CC=C3.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

Download SDS (MSDS)

Certificate of Analysis

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Tamoxifen Citrate  Product Citations

See how others have used Tamoxifen Citrate. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 10 total

PMID: # 27814544  Isidori, M. et al. 2016. Environ. Pollut. 219: 275-287.

PMID: # 26971211  Ferre-Aracil, J. et al. 2016. The Science of the total environment. 556: 70-9.

PMID: # 25811655  2015. PLoS ONE. 10: e0121316.

PMID: # 26320721  Negreira, N. et al. 2015. Water Res. 85: 199-207.

PMID: # 25124055  Negreira, N. et al. 2014. Sci. Total Environ. 497-498: 68-77.

PMID: # 24148406  2013. Talanta. 116: 290-9.

PMID: # 23357749  Negreira, N. et al. 2013. J Chromatogr A. 1280: 64-74.

PMID: # 23089292  2012. Eur J Pharm Sci. 47: 842-7.

PMID: # 10402244  Toma, S. et al. 1999. Int. J. Oncol. 15: 321-337.

PMID: # 9042218  Kellen, JA. et al. 1996 Nov-Dec. Anticancer Res. 16: 3537-3541.

Citations 1 to 10 of 10 total
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Rated 5 out of 5 by from Watanabe M; et al Watanabe M; et al. (PubMed: 26423799) determined that Tamoxifen Citrate has less of an effect on CYP2D6 in the bioactivation pathway of TOR. -SCBT Publication Review
Date published: 2015-04-02
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