Tamoxifen citrate salt

SKU: T0201

Category: Antibiotics

Synonyms: (Z)-1-(p-Dimethylaminoethoxyphenyl)-1,2-diphenyl-1-butene; 54965-24-1
CAS-Number: C₂₆H₂₉NO · C₆H₈O₇
Molecular Formula: 563.64
Molecular Weight

Product Data
Handling
Safety Information
Details

Specifications

Purity: ≥98% (Titration)
Identity: 1H-NMR
Appearance: White powder

Properties

Melting Point: approx. 142° C
Solvents: methanol

Downloads

Safety Data Sheet: CDX T0201 MSDS.pdf

Handling Advice: Protect from light and moisture.
Use / Stability: Stable for at least 2 years after receipt when stored at +4°C.
Long Term Storage: +4°C
Short Term Storage: RT
Shipping: AMBIENT

Transportation: Not dangerous goods
Signal word: Danger
GHS Symbol: GHS07+GHS08
Precautionary statements: P201-P308 + P313
Hazard statements: H302-H350-H360

Description: Selective estrogen receptor modulator (SERM) used as adjuvant therapy for estrogen-dependent breast cancer. Antagonist of ER action in breast tissue and breast cancer cells and ER agonist in bone, uterus, and the cardiovasculature system. This prodrug is metabolized by cytochrome P450 (CYP450) enzymes to the active metabolites N-desmethyl-TMX, 4-hydroxy-N-desmethyl-TMX (endoxifen) and 4-hydroxy-TMX (afimoxifene). N,N-Didesmethyl-4-hydroxytamoxifen (norendoxifen), another active metabolite has been found to act as a potent competitive aromatase inhibitor and may also be involved in its antiestrogenic activity. Binds microsomal antiestrogen binding sites, altering cholesterol esterification at therapeutic doses and impacting breast cancer cell differentiation, apoptosis, and autophagy. Protein kinase C (PKC) inhibitor and anti-angiogenetic factor.
InChi: InChI=1S/C26H29NO.C6H8O7/c1-4-25(21-11-7-5-8-12-21)26(22-13-9-6-10-14-22)23-15-17-24(18-16-23)28-20-19-27(2)3,7-3(8)1-6(13,5(11)12)2-4(9)10/h5-18H,4,19-20H2,1-3H3,13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/b26-25-,
References: K. B. Horwitz & W. L. McGuire, J. Biol. Chem. 253, 8185 (1978) , V.C. Jordan, et al., Cancer Treat. Rep. 64, 745 (1980) , C.A. O'Brian, et al., Cancer Res. 45, 2462 (1985) , K.J. Edwards, et al., J. Med. Chem. 35, 2753 (1992) , M. Clarke, et al., Lancet 351, 1451 (1998) , D.A. Tonetti & V.C. Jordan, Mol. Med. Today 2, 218 (1996) , J.M. Hall, et al., J. Biol. Chem. 276, 36869 (2001) , P. Thomas, et al., Endocrinol. 146, 624 (2005) , M.S. Singh, et al., Breast 20, 111 (2011) , P. de Medina, et al., Chem. Phys. Lip. 164, 432 (2011) , V.K. Todorova, et al., Cancer Chemother. Pharmacol. 67, 285 (2011)
InChi Key: FQZYTYWMLGAPFJ-OQKDUQJOSA-N
Smiles: CN(CCOC1=CC=C(/C(C2=CC=CC=C2)=C(C3=CC=CC=C3)/CC)C=C1)C.OC(CC(O)(C(O)=O)CC(O)=O)=O

Selective estrogen receptor modulator (SERM) used as adjuvant therapy for estrogen-dependent breast cancer. Antagonist of ER action in breast tissue and breast cancer cells and ER agonist in bone, uterus, and the cardiovasculature system. This prodrug is metabolized by cytochrome P450 (CYP450) enzymes to the active metabolites N-desmethyl-TMX, 4-hydroxy-N-desmethyl-TMX (endoxifen) and 4-hydroxy-TMX (afimoxifene). N,N-Didesmethyl-4-hydroxytamoxifen (norendoxifen), another active metabolite has been found to act as a potent competitive aromatase inhibitor and may also be involved in its antiestrogenic activity. Binds microsomal antiestrogen binding sites, altering cholesterol esterification at therapeutic doses and impacting breast cancer cell differentiation, apoptosis, and autophagy. Protein kinase C (PKC) inhibitor and anti-angiogenetic factor.

SKU: T0201 Category: Antibiotics

Additional information

Additional information

Synonyms	(Z)-1-(p-Dimethylaminoethoxyphenyl)-1,2-diphenyl-1-butene
Purity	≥98% (Titration)
Appearance	White powder
CAS-Number	54965-24-1
Molecular Formula	C26H29NO · C6H8O7
Molecular Weight	563.64
Identity	1H-NMR
Solvents	methanol
Melting Point	approx. 142° C
Smiles	CN(CCOC1=CC=C(/C(C2=CC=CC=C2)=C(C3=CC=CC=C3)/CC)C=C1)C.OC(CC(O)(C(O)=O)CC(O)=O)=O
InChi Key	FQZYTYWMLGAPFJ-OQKDUQJOSA-N
Shipping	AMBIENT
Short Term Storage	RT
Long Term Storage	+4°C
Handling Advice	Protect from light and moisture.
Use / Stability	Stable for at least 2 years after receipt when stored at +4°C.
Hazard statements	H302-H350-H360
Precautionary statements	P201-P308 + P313
GHS Symbol	GHS07+GHS08
Signal word	Danger
Transportation	Not dangerous goods
References	K. B. Horwitz & W. L. McGuire, J. Biol. Chem. 253, 8185 (1978), V.C. Jordan, et al., Cancer Treat. Rep. 64, 745 (1980), C.A. O'Brian, et al., Cancer Res. 45, 2462 (1985), K.J. Edwards, et al., J. Med. Chem. 35, 2753 (1992), M. Clarke, et al., Lancet 351, 1451 (1998), D.A. Tonetti & V.C. Jordan, Mol. Med. Today 2, 218 (1996), J.M. Hall, et al., J. Biol. Chem. 276, 36869 (2001), P. Thomas, et al., Endocrinol. 146, 624 (2005), M.S. Singh, et al., Breast 20, 111 (2011), P. de Medina, et al., Chem. Phys. Lip. 164, 432 (2011), V.K. Todorova, et al., Cancer Chemother. Pharmacol. 67, 285 (2011)
InChi	InChI=1S/C26H29NO.C6H8O7/c1-4-25(21-11-7-5-8-12-21)26(22-13-9-6-10-14-22)23-15-17-24(18-16-23)28-20-19-27(2)3,7-3(8)1-6(13,5(11)12)2-4(9)10/h5-18H,4,19-20H2,1-3H3,13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/b26-25-,
Quantity	1 g, 5 g, Bulk