RALOXIFENE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C28H27NO4S
Molecular Weight	473.583
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC1=CC=C(C=C1)C2=C(C(=O)C3=CC=C(OCCN4CCCCC4)C=C3)C5=C(S2)C=C(O)C=C5

InChI

InChIKey=GZUITABIAKMVPG-UHFFFAOYSA-N

InChI=1S/C28H27NO4S/c30-21-8-4-20(5-9-21)28-26(24-13-10-22(31)18-25(24)34-28)27(32)19-6-11-23(12-7-19)33-17-16-29-14-2-1-3-15-29/h4-13,18,30-31H,1-3,14-17H2

HIDE SMILES / InChI

Molecular Formula	C28H27NO4S
Molecular Weight	473.583
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.drugbank.ca/drugs/DB00481 | https://www.drugs.com/pro/raloxifene-hydrochloride-tablets.html | https://www.ncbi.nlm.nih.gov/pubmed/11836973 | http://reference.medscape.com/drug/evista-raloxifene-342794

Raloxifene (marketed as Evista by Eli Lilly and Company) is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. Raloxifene binds to estrogen receptors, resulting in differential expression of multiple estrogen-regulated genes in different tissues. Raloxifene produces estrogen-like effects on bone, reducing resorption of bone and increasing bone mineral density in postmenopausal women, thus slowing the rate of bone loss. The maintenance of bone mass by raloxifene and estrogens is, in part, through the regulation of the gene-encoding transforming growth factor-β3 (TGF-β3), which is a bone matrix protein with antiosteoclastic properties. Raloxifene activates TGF-β3 through pathways that are estrogen receptor-mediated but involve DNA sequences distinct from the estrogen response element. The drug also binds to the estrogen receptor and acts as an estrogen agonist in preosteoclastic cells, which results in the inhibition of their proliferative capacity. This inhibition is thought to contribute to the drug's effect on bone resorption. Other mechanisms include the suppression of the activity of the bone-resorbing cytokine interleukin-6 promoter activity. Raloxifene also antagonizes the effects of estrogen on mammary tissue and blocks uterotrophic responses to estrogen. By competing with estrogens for the estrogen receptors in reproductive tissue, raloxifene prevents the transcriptional activation of genes containing the estrogen response element. As well, raloxifene inhibits the estradiol-dependent proliferation of MCF-7 human mammary tumor cells in vitro. The mechanism of action of raloxifene has not been fully determined, but evidence suggests that the drug's tissue-specific estrogen agonist or antagonist activity is related to the structural differences between the raloxifene-estrogen receptor complex (specifically the surface topography of AF-2) and the estrogen-estrogen receptor complex. Also, the existence of at least 2 estrogen receptors (ERα, ERβ) may contribute to the tissue specificity of raloxifene. Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women. It is also used for reduction of risk and treatment of invasive breast cancer, and it also reduces breast density. For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate. Common adverse events considered to be drug-related were hot flashes and leg cramps.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Estrogen receptor alpha 127 Target ID: CHEMBL206 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18457385	Agonist 2678	22.0 nM [EC50]
Estrogen receptor beta 110 Target ID: CHEMBL242 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11906280	Agonist 2678	260.0 nM [EC50]
Estrogen receptor 75 Target ID: CHEMBL2093866 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12749898	Agonist 2678

Conditions

Condition	Modality	Highest Phase	Product
Osteoporosis in postmenopausal women 6 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Primary	Approved 8429	EVISTA Approved Use EVISTA® is an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. (1.1) Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (1.2) Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. (1.3) Important Limitations: EVISTA is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer. (1.3) 1.1 Treatment and Prevention of Osteoporosis in Postmenopausal Women EVISTA is indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1, 14.2) Launch Date 1997
Breast cancer in postmenopausal women with osteoporosis 3 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Primary	Approved 8429	EVISTA Approved Use EVISTA® is an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. (1.1) Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (1.2) Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. (1.3) Important Limitations: EVISTA is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer. (1.3) 1.1 Treatment and Prevention of Osteoporosis in Postmenopausal Women EVISTA is indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1, 14.2) Launch Date 1997
Breast cancer in postmenopausal women at high risk for invasive breast cancer 3 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Primary	Approved 8429	EVISTA Approved Use EVISTA® is an estrogen agonist/antagonist indicated for: Treatment and prevention of osteoporosis in postmenopausal women. (1.1) Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (1.2) Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. (1.3) Important Limitations: EVISTA is not indicated for the treatment of invasive breast cancer, reduction of the risk of recurrence of breast cancer, or reduction of risk of noninvasive breast cancer. (1.3) 1.1 Treatment and Prevention of Osteoporosis in Postmenopausal Women EVISTA is indicated for the treatment and prevention of osteoporosis in postmenopausal women [see Clinical Studies (14.1, 14.2) Launch Date 1997

C_max

Value	Dose	Co-administered	Analyte	Population
0.5 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:		RALOXIFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
27.2 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:		RALOXIFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
27.7 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:		RALOXIFENE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
180 mg 1 times / day single, oral Studied dose Dose: 180 mg, 1 times / day Route: oral Route: single Dose: 180 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	healthy, 18 months n = 2 Health Status: healthy Age Group: 18 months Population Size: 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Other AEs: Ataxia, Dizziness... Other AEs: Ataxia Dizziness Vomiting Rash Diarrhea Tremor Flushing Alkaline phosphatase increased Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf
600 mg 1 times / day multiple, oral Highest studied dose Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/8725181/	healthy, Mean age 53.2 years n = 63 Health Status: healthy Age Group: Mean age 53.2 years Sex: F Population Size: 63 Sources: https://pubmed.ncbi.nlm.nih.gov/8725181/	Other AEs: Hot flashes... Other AEs: Hot flashes Sources: https://pubmed.ncbi.nlm.nih.gov/8725181/
60 mg 1 times / day multiple, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf	unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf	Other AEs: Deep vein thrombosis, Pulmonary embolism... Other AEs: Deep vein thrombosis Pulmonary embolism Stroke Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf
60 mg 1 times / day multiple, oral Recommended Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf https://pubmed.ncbi.nlm.nih.gov/12450599/	unhealthy, Mean age 68 years n = 10101 Health Status: unhealthy Age Group: Mean age 68 years Sex: F Population Size: 10101 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf https://pubmed.ncbi.nlm.nih.gov/12450599/	Disc. AE: Vomiting, Nausea... AEs leading to discontinuation/dose reduction: Vomiting (0.3%) Nausea (0.6%) Oedema (0.6%) Muscle spasms (0.7%) Muscle related signs and symptoms NEC (1.6%) Headache (0.3%) Paralysis (0.1%) Hot flush (1.4%) Peripheral vascular disorder (1.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022042s000_MedR_P3.pdf https://pubmed.ncbi.nlm.nih.gov/12450599/
180 mg multiple, oral Studied dose Dose: 180 mg Route: oral Route: multiple Dose: 180 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Other AEs: Leg cramps, Dizziness... Other AEs: Leg cramps Dizziness Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf
1.5 g 1 times / day single, oral Studied dose Dose: 1.5 g, 1 times / day Route: oral Route: single Dose: 1.5 g, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	unhealthy Health Status: unhealthy Sex: F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 1587			inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A5 73 KCNQ1/KCNE1 3	UGT1A1 418 UGT1A8 283 UGT1A9 380 UGT1A 7 UGT1A3 422 UGT1A4 347 UGT1A6 307 UGT1A7 236 UGT2B7 389 UGT2B15 203 SULT1A3 27 BCRP 561 MRP4 77

Drug as perpetrator

Target	Modality	Activity
CYP3A5 130	inhibitor 3277 Sources: https://pubs.acs.org/doi/pdf/10.1021/tx700207u Page: 1.0	yes [IC50 2.4 uM]
CYP3A4 1925	inhibitor 3277 Sources: https://pubs.acs.org/doi/pdf/10.1021/tx700207u Page: 1.0	yes [IC50 3.7 uM]
KCNQ1/KCNE1 3	inhibitor 3277 Sources: https://www.sciencedirect.com/science/article/pii/S1043661810001611 Page: 1.0	yes [IC50 4.8 uM]

Drug as victim

Target	Modality	Activity	Metabolite
UGT1A3 422	substrate 3367 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
UGT1A4 347	substrate 3367 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
UGT1A6 307	substrate 3367 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
UGT1A7 236	substrate 3367 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
UGT2B15 203	substrate 3367 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
UGT2B7 389	substrate 3367 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	no
SULT1A3 27	substrate 3367 Sources: https://www.sciencedirect.com/science/article/pii/S1347436715000580 Page: 1.0	yes [Km 0.33 uM]
BCRP 561	substrate 3367 Sources: https://www.sciencedirect.com/science/article/pii/S1347436715000580 Page: 1.0	yes	RALOXIFENE-4'-Sulfate 3
BCRP 561	substrate 3367 Sources: https://www.sciencedirect.com/science/article/pii/S1347436715000580 Page: 1.0	yes	RALOXIFENE-6-Sulfate 3
MRP4 77	substrate 3367 Sources: https://www.sciencedirect.com/science/article/pii/S1347436715000580 Page: 1.0	yes	RALOXIFENE-4'-Sulfate 3
MRP4 77	substrate 3367 Sources: https://www.sciencedirect.com/science/article/pii/S1347436715000580 Page: 1.0	yes	RALOXIFENE-6-Sulfate 3
UGT1A 7	substrate 3367 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	yes
UGT1A1 418	substrate 3367 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	yes
UGT1A8 283	substrate 3367 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	yes
UGT1A9 380	substrate 3367 Sources: https://reader.elsevier.com/reader/sd/pii/S0378517309003536?token=C5EF4CE2F71D78CFD787CA2FAC57B1E30092D604FB48B94AE8D7DBA7256401EEA08F7693A3CD048482E0D78C463EC866#page=2 Page: 2.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.sciencedirect.com/science/article/pii/S1043661810001611 Page: 1.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:8772	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:8772
ChemicalBook	CB1290431	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1290431
ZINC	ZINC000000538275	http://zinc15.docking.org/substances/ZINC000000538275
eMolecules	902386	https://www.emolecules.com/cgi-bin/more?vid=902386

PubMed

Title	Date	PubMed
Raloxifene and prevention of vertebral fracture (cont'd): mainly when oestrogen is contraindicated.	2000 Dec	11475503
Chemoprevention of breast cancer with fenretinide.	2001	11434448
[Modern approaches to hormone therapy of breast cancer as a reflection of pathogenesis of the disease].	2001	11383456
Update on endocrine aspects of breast cancer: report from the 23rd San Antonio Breast Cancer Symposium, San Antonio, Texas, USA, 6-9 December 2000.	2001	11305952
Raloxifene.	2001	11281162
[An alternative to postmenopausal Hormone Replacement Therapy? Selective Estrogens Receptors Modulators (SERMs)].	2001 Apr	11319506
Suggested rationale for prevention and treatment of glucocorticoid-induced bone loss in dermatologic patients.	2001 Apr	11295929
Can estrogen or selective estrogen-receptor modulators preserve cognitive function in elderly women?	2001 Apr 19	11309641
Raloxifene fails to slow cognitive decline in older women.	2001 Apr 21	11418160
Raloxifene for breast cancer prevention.	2001 Apr 25	11311092
[SERM--selective estrogen receptor modulators].	2001 Apr 9	11332210
Bone builders: preventing and treating osteoporosis.	2001 Aug	11481213
Familiar drugs may prevent cancer.	2001 Aug	11470927
Estrogen-like activity of tamoxifen and raloxifene on NMDA receptor binding and expression of its subunits in rat brain.	2001 Aug	11425508
Neuroprotective properties of 17beta-estradiol, progesterone, and raloxifene in MPTP C57Bl/6 mice.	2001 Aug	11400179
An update on glucocorticoid-induced osteoporosis.	2001 Feb	11285998
Treatment of osteoporosis with bisphosphonates.	2001 Feb	11285996
The role of selective estrogen receptor modulators in the prevention and treatment of osteoporosis.	2001 Feb	11285993
Paradoxical interactions among estrogen receptors, estrogens and SERMS: mutual annihilation and synergy.	2001 Jan-Mar	11384866
Control of the estrogen-like actions of the tamoxifen-estrogen receptor complex by the surface amino acid at position 351.	2001 Jan-Mar	11384864
Raloxifene effect on frequency of surgery for pelvic floor relaxation.	2001 Jul	11430963
Gonadotropins at menopause: the influence of obesity, insulin resistance, and estrogens.	2001 Jul	11322964
Rheumatology: 15. Osteoporosis.	2001 Jul 10	11468955
2-Amino-4,6-diarylpyridines as novel ligands for the estrogen receptor.	2001 Jul 23	11459665
Effects of raloxifene and hormone replacement therapy on markers of serum atherogenicity in healthy postmenopausal women.	2001 Jul 25	11451623
Tamoxifen and contralateral breast cancer: the other side.	2001 Jul 4	11438553
Estradiol regulates monocyte chemotactic protein-1 in human coronary artery smooth muscle cells: a mechanism for its antiatherogenic effect.	2001 Jul-Aug	11449089
Tamoxifen, screening and new oestrogen receptor modulators.	2001 Jun	11476559
A non-calcemic analog of 1 alpha,25 dihydroxy vitamin D(3) (JKF) upregulates the induction of creatine kinase B by 17 beta estradiol in osteoblast-like ROS 17/2.8 cells and in rat diaphysis.	2001 Jun	11457658
Estrogenic and antiestrogenic effects of raloxifene on collagen metabolism in breast cancer MCF-7 cells.	2001 Jun	11447735
Tibolone and its effects on bone: a review.	2001 Jun	11428176
Osteoporosis.	2001 Jun	11402788
Effect of physicians opinion on patients' choice of treatment.	2001 Jun	11384811
Oestrogenic effects of neonatal administration of raloxifene on hypothalamic-pituitary-gonadal axis in male and female rats.	2001 Jun	11373178
Chemoprevention of breast cancer. A joint guideline from the Canadian Task Force on Preventive Health Care and the Canadian Breast Cancer Initiative's Steering Committee on Clinical Practice Guidelines for the Care and Treatment of Breast Cancer.	2001 Jun 12	11450210
Systemic therapy for older women with breast cancer.	2001 Mar	11301828
Selective estrogen receptor modulators. An aid in unraveling the links between estrogen and breast cancer.	2001 Mar	11296736
SERMs and cardiovascular disease in women. How do these agents affect risk?	2001 Mar	11296735
Effects of estrogen deficiency on brain function. Implications for the treatment of postmenopausal women.	2001 Mar	11296734
Therapy for osteoporosis.	2001 Mar	11285883
Prevention and treatment of osteoporosis.	2001 Mar-Apr	11333463
Effects of the selective oestrogen receptor modulator-raloxifene-on calcium and PTH secretory dynamics in women with osteoporosis.	2001 May	11380487
Differential SERM activation of the estrogen receptors (ERalpha and ERbeta) at AP-1 sites.	2001 May	11358690
Silencing and reactivation of the selective estrogen receptor modulator-estrogen receptor alpha complex.	2001 May 1	11325832
Flexible alignment of small molecules.	2001 May 10	11334559
Effect of tibolone and raloxifene on the tail temperature of oestrogen-deficient rats.	2001 May 4	11348629
From adjuvant therapy to breast cancer prevention: BCPT and STAR.	2001 May-Jun	11469927
Estrogen receptor (ER)-alpha, but not ER-beta, mediates regulation of the insulin-like growth factor I gene by antiestrogens.	2001 Sep 21	11457856
Cardiovascular effects of raloxifene hydrochloride.	2001 Spring	11314601
Regression to the mean: what does it mean? Using bone density results to monitor treatment of osteoporosis.	2001 Spring	11309514

Patents

Sample Use Guides

In Vivo Use Guide

60 mg tablet orally once daily

Route of Administration: Oral

In Vitro Use Guide

MCF-7 cells were obtained from the ATCC and grown in Growth Medium (GM). The cells are grown to 80% confluency and trypsinized and washed to remove phenol red, then plated at 10,000 cells/well in Starve Medium (SM). After 2 days, the medium is removed from the cells and either fresh SM or SM plus Raloxifene is added (100 mL total volume). The next day the bDNA assay is started by adding Capture Hybridization Buffer to each capture well of the bDNA plate (all solutions supplied with QuantiGene kit). Subsequently, medium is removed from the 96-well plate containing cells and then the solution of lysis buffer and oligomers (designed by ProbeDesigner 1.0 for the gene of interest) is added to the 96-well plate (100 mL/well). The cell and lysis/ oligomer mixture is incubated for 15 min at 53 C and then vortexed for 1 min. The lysate is then transferred to the bDNA capture plate and mixed. The plate is then sealed and incubated at 53 C for 16 h. The next day, the plate is cooled for 10 min at room temperature and the Amplifier Reagent mixture is prepared. The wells are then washed twice with 200 mkL of Wash Solution A. Amplifier Reagent is added (50 mkL/well) and the plate is sealed again and incubated at 53 C for 30 min. The plate is then cooled for 10 min at room temperature (rt) and the Label Probe Reagent is prepared. The plate is washed twice with 200 mkL of Wash Solution A and 50 mkL/well of Label Probe Reagent is added. The plate is sealed and incubated at 53 C for 15 min. The plate is cooled for 10 min at rt and the Substrate Mixture is prepared. The plate is again washed twice with 200 mkL Wash Solution A and then twice with Wash Solution D. The Substrate Mixture is then added (50 mkL) and the plate is sealed. The plate is incubated at 37 C for 30 min and then read on the Quantiplex luminometer. Raloxifene is used as a positive control in this assay, and behaves as a full antagonist of estrogen-induced pS2 expression.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:46:25 GMT 2023` Edited by `admin` on `Fri Dec 15 15:46:25 GMT 2023`
Record UNII	YX9162EO3I
Record Status	`Validated (UNII)`
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Name

Type

Language

RALOXIFENE

Official Name

English

EVIDEN

Brand Name

English

RALOXIFENE [HSDB]

Common Name

English

Raloxifene [WHO-DD]

Common Name

English

RAXETO

Brand Name

English

NSC-747974

Code

English

LY-139481

Code

English

RALOXIFENE [VANDF]

Common Name

English

RALOXIFENE [MI]

Common Name

English

RALOXIPHENE

Common Name

English

raloxifene [INN]

Common Name

English

J22.982B

Code

English

KEOXIFENE

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000175826