A mixture of droloxifene isomers
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(E/Z)-Droloxifene

Item No. 33406

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-phenol
CAS Number
165813-01-4
Synonyms
  • 3-Hydroxytamoxifen
Molecular Formula
C26H29NO2
Formula Weight
387.5
Purity
≥98% (mixture of isomers)
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/mlDMSO: 15 mg/mlEthanol: 1 mg/ml
SMILES
CCC(C1=CC=CC=C1)=C(C2=CC(O)=CC=C2)C3=CC=C(C=C3)OCCN(C)C
InChi Code
InChI=1S/C26H29NO2/c1-4-25(20-9-6-5-7-10-20)26(22-11-8-12-23(28)19-22)21-13-15-24(16-14-21)29-18-17-27(2)3/h5-16,19,28H,4,17-18H2,1-3H3
InChi Key
ZQZFYGIXNQKOAV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    (E/Z)-Droloxifene is a mixture of (E)-droloxifene, a selective estrogen receptor modulator (SERM), and (Z)-droloxifene.1 (E)-Droloxifene binds to the estrogen receptor (ER) in rabbit uterine homogenates (IC50 = 24 nM in a radioligand binding assay), increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats.1,2,3 It also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells in a concentration-dependent manner.4 (Z)-Droloxifene binds weakly to ERs and has no estrogenic or antiestrogenic activity.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Robertson, J.F.R. Selective oestrogen receptor modulators/new antioestrogens: A clinical perspective. Cancer Treat. Rev. 30(8), 695-706 (2004).

    2. Löser, R., Seibel, K., Roos, W., et al. In vivo and in vitro antiestrogenic action of 3-hydroxytamoxifen, tamoxifen and 4-hydroxytamoxifen. Eur. J. Cancer Clin. Oncol. 21(8), 985-990 (1985).

    3. Hasmann, M., Rattel, B., and Löser, R. Preclinical data for droloxifene. Cancer Lett. 84(2), 101-116 (1994).

    4. Kawamura, I., Mizota, T., Lacey, E., et al. The estrogenic and antiestrogenic activities of droloxifene in human breast cancers. Jpn. J. Pharmacol. 63(1), 27-34 (1993).

    5. Löser, R., Seibel, K., and Huber, H.J. Pharmacological activities of droloxifene isomers. Anticancer Res. 8(6), 1271-1274 (1988).