Pipendoxifene

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

MedKoo CAT#: 202240

CAS#: 198480-55-6

Description: Pipendoxifene, also known as ERA-923, is a new antiestrogen with potential anticancer activity. ERA-923 potently inhibits estrogen binding to ER-alpha (IC50 = 14 nM). In ER-alpha-positive human MCF-7 breast carcinoma cells, ERA-923 inhibits estrogen-stimulated growth (IC50 = 0.2 nM) associated with cytostasis. In vitro, a MCF-7 variant with inherent resistance to tamoxifen (10-fold) or 4-OH tamoxifen (>1000-fold) retains complete sensitivity to ERA-923 . In preclinical models, ERA-923 has an improved efficacy and safety compared with tamoxifen. In the combination with temsirolimus, ERA-923 showed excellent anticancer activity in preclinical models.


Chemical Structure

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Pipendoxifene
CAS# 198480-55-6

Theoretical Analysis

MedKoo Cat#: 202240
Name: Pipendoxifene
CAS#: 198480-55-6
Chemical Formula: C29H32N2O3
Exact Mass: 456.24129
Molecular Weight: 456.58
Elemental Analysis: C, 76.29; H, 7.06; N, 6.14; O, 10.51

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Synonym: ERA923; ERA 923; ERA-923; Pipendoxifene

IUPAC/Chemical Name: 2-(4-hydroxyphenyl)-3-methyl-1-(4-(2-(piperidin-1-yl)ethoxy)benzyl)-1H-indol-5-ol.

InChi Key: JICOGKJOQXTAIP-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H32N2O3/c1-21-27-19-25(33)11-14-28(27)31(29(21)23-7-9-24(32)10-8-23)20-22-5-12-26(13-6-22)34-18-17-30-15-3-2-4-16-30/h5-14,19,32-33H,2-4,15-18,20H2,1H3

SMILES Code: OC1=CC2=C(N(CC3=CC=C(OCCN4CCCCC4)C=C3)C(C5=CC=C(O)C=C5)=C2C)C=C1

Appearance: white 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, not in water

Shelf Life: >2 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

Preparing Stock Solutions

The following data is based on the product molecular weight 456.58 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

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1: Sadler TM, Gavriil M, Annable T, Frost P, Greenberger LM, Zhang Y. Combination therapy for treating breast cancer using antiestrogen, ERA-923, and the mammalian target of rapamycin inhibitor, temsirolimus. Endocr Relat Cancer. 2006 Sep;13(3):863-73. PubMed PMID: 16954435.

2: Conzen SD. Current status of selective estrogen receptor modulators (SERMs). Cancer J. 2003 Jan-Feb;9(1):4-14. Review. PubMed PMID: 12602762.

3: Johnston SR. Endocrine manipulation in advanced breast cancer: recent advances with SERM therapies. Clin Cancer Res. 2001 Dec;7(12 Suppl):4376s-4387s; discussion 4411s-4412s. Review. PubMed PMID: 11916228.

4: Cotreau MM, Stonis L, Dykstra KH, Gandhi T, Gutierrez M, Xu J, Park Y, Burghart PH, Schwertschlag US. Multiple-dose, safety, pharmacokinetics, and pharmacodynamics of a new selective estrogen receptor modulator, ERA-923, in healthy postmenopausal women. J Clin Pharmacol. 2002 Feb;42(2):157-65. PubMed PMID: 11831538.

5: Greenberger LM, Annable T, Collins KI, Komm BS, Lyttle CR, Miller CP, Satyaswaroop PG, Zhang Y, Frost P. A new antiestrogen, 2-(4-hydroxy-phenyl)-3-methyl-1-[4-(2-piperidin-1-yl-ethoxy)-benzyl]-1H-indol-5-o l hydrochloride (ERA-923), inhibits the growth of tamoxifen-sensitive and -resistant tumors and is devoid of uterotropic effects in mice and rats. Clin Cancer Res. 2001 Oct;7(10):3166-77. PubMed PMID: 11595711.

Pipendoxifene

10.0mg / Not available


Additional Information