ALEXIS Biochemicals: (Z)-4-Hydroxytamoxifen

Advanced Search

You are here: Product Lines > Cancer > Antitumor Reagents > Antitumor Agents (Hormone-related)

ALX-270-476

Revised 11-Mar-08

Bicalutamide
SYNONYMS	N-(4-Cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methylpropanamide
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	Androgens & Androgen Receptors / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-476-M100		100 mg	40.00 USD
ALX-270-476-M500		500 mg	140.00 USD
ALX-270-476-G001		1 g	220.00 USD

Product Specification

FORMULA:	C₁₈H₁₄F₄N₂O₄S
MW:	430.4
CAS NUMBER:	90357-06-5
SOURCE/HOST:	Synthetic.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in acetone and tetrahydrofuran; slightly soluble in 100% ethanol or methanol; practically insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Nonsteroidal antiandrogen. Effective in the treatment of prostate cancer. Induces cell death by a pathway that is independent of changes in mitochondrial membrane potential and Bcl-2 action.

Product Specific Literature References

Antiproliferative activity of casodex (ICI 176.334) in hormone-dependent tumours: A. Maucher & E. von Angerer; J. Cancer Res. Clin. Oncol. 119, 669 (1993) Abstract
Antiandrogen-induced cell death in LNCaP human prostate cancer cells: E.C. Lee, et al.; Cell Death Differ. 10, 761 (2003) Abstract
Proanthocyanidins from grape seeds inhibit expression of matrix metalloproteinases in human prostate carcinoma cells, which is associated with the inhibition of activation of MAPK and NF kappa B: P.K. Vayalil, et al.; Carcinogenesis 25, 987 (2004) Abstract; Full Text
Wnt3a growth factor induces androgen receptor-mediated transcription and enhances cell growth in human prostate cancer cells: M. Verras, et al.; Cancer Res. 64, 8860 (2004) Abstract; Full Text
Glycogen synthase kinase-3beta activity is required for androgen-stimulated gene expression in prostate cancer: X. Liao, et al.; Endocrinology 145, 2941 (2004) Abstract; Full Text
A phase I pharmacokinetic and pharmacodynamic study of OGX-011, a 2’-methoxyethyl antisense oligonucleotide to clusterin, in patients with localized prostate cancer: K.N. Chi, et al.; J. Natl. Cancer Inst. 97, 1287 (2005) Abstract; Full Text
The mechanisms and managements of hormone-therapy resistance in breast and prostate cancers: K.M. Rau, et al.; Endocr. Relat. Cancer 12, 511 (2005), Review Abstract; Full Text
Signal transduction pathways in androgen-dependent and -independent prostate cancer cell proliferation: P.M. Ghosh, et al.; Endocr. Relat. Cancer 12, 119 (2005) Abstract; Full Text
Recent advances on multiple tumorigenic cascades involved in prostatic cancer progression and targeting therapies: M. Mimeault & S.K. Batra; Carcinogenesis 27, 1 (2006), Review Abstract; Full Text
Bcl-xL is overexpressed in hormone-resistant prostate cancer and promotes survival of LNCaP cells via interaction with proapoptotic Bak: C. Castilla, et al.; Endocrinology 147, 4960 (2006) Abstract; Full Text
Androgen receptor corepressors and prostate cancer: C.J. Burd, et al.; Endocr. Relat. Cancer 13, 979 (2006), Review Abstract; Full Text
Par-4-dependent apoptosis by the dietary compound withaferin A in prostate cancer cells: S. Srinivasan, et al.; Cancer Res. 67, 246 (2006) Abstract; Full Text
Androgen receptor structural and functional elements: role and regulation in prostate cancer: S.M. Dehm & D.J. Tindall; Mol. Endocrinol. 21, 2855 (2007), Review Abstract
Phosphoinositide 3-kinase-independent non-genomic signals transit from the androgen receptor to Akt1 in membrane raft microdomains: B. Cinar, et al.; JBC 282, 29584 (2007) Abstract; Full Text
A novel class of pyranocoumarin anti-androgen receptor signaling compounds: J. Guo, et al.; Mol. Cancer Ther. 6, 907 (2007) Abstract; Full Text
Increased resistance to trail-induced apoptosis in prostate cancer cells selected in the presence of bicalutamide: M. Mitterberger, et al.; Prostate 67, 1194 (2007) Abstract
Interplay of nuclear factor-kappaB and B-myb in the negative regulation of androgen receptor expression by tumor necrosis factor alpha: S. Ko, et al.; Mol. Endocrinol. 22, 273 (2008) Abstract

Further Categories Containing This Product:

Antitumor Agents (Hormone-related)

ALX-550-516

Revised 21-May-08

Compound A
SYNONYMS	CpdA 2-((4-Acetophenyl)-2-chloro-N-methyl)ethylammonium chloride
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Anti-inflammatory Agents

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-550-516-M005		5 mg	40.00 USD
ALX-550-516-M025		25 mg	120.00 USD

Product Specification

FORMULA:	C₁₁H₁₄ClNO₂ . HCl
MW:	227.7 . 36.5
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO, 100% ethanol or water.
SHIPPING:	SHIPPED ON DRY ICE
LONG TERM STORAGE:	-80°C
USE/STABILITY:	Stock solutions in ethanol are stable for up to 1 month when stored at -80°C.
HANDLING:	Protect from moisture. After reconstitution, prepare aliquots and store at -80°C.

Product Description

Cell permeable, nonsteroidal glucocorticoid receptor modulator with high binding affinity. Exerts anti-inflammatory potential by down-modulating TNF-induced pro-inflammatory gene expression, such as IL-6 and E-selectin. Unlike dexamethasone (Prod. No. ALX-370-002) it does not enhance glucocorticoid response element (GRE)-driven gene expression or induce glucocorticoid receptor (GR) binding to GRE-dependent genes in vivo.

Product Specific Literature References

A fully dissociated compound of plant origin for inflammatory gene repression: K. De Bosscher, et al.; PNAS 102, 15827 (2005) Abstract
A plant-derived ligand favoring monomeric glucocorticoid receptor conformation with impaired transactivation potential attenuates collagen-induced arthritis: P. Dewint, et al.; J. Immunol. 180, 2608 (2008) Abstract

Related Products

ALX-550-516

Compound A

Further Categories Containing This Product:

GITR & GITRL Other Products • RANK & RANKL / OPG Other Products • Antitumor Agents (Hormone-related) • NOS Inhibitors (NOS Induction & Enzyme Activity) • Chemopreventive Agents Other Products • DNA & RNA Methyl & Alkyl Transferases / Related Products • Cell Cycle Other Products

ALX-385-032

Revised 16-Jun-08

(R,S)-Equol
SYNONYMS	(±)-Equol 3,4-Dihydro-3-(4-hydroxyphenyl)-2H-1-benzopyran-7-ol 4’,7-Dihydroxyisoflavane
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Flavonoids / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-385-032-M005		5 mg	30.00 USD
ALX-385-032-M025		25 mg	120.00 USD

Product Specification

FORMULA:	C₁₅H₁₄O₃
MW:	242.3
CAS NUMBER:	531-95-3, 94105-90-5
MERCK INDEX:	14: 3644
PURITY:	≥98% (HPLC)
APPEARANCE:	White to light yellow powder.
SOLUBILITY:	Soluble in DMSO, methanol or 100% ethanol; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Flavonoid. Racemic mixture. Urinary metabolite of daidzein. Inhibits 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced neoplastic cell transformation by targeting the MEK/ERK/p90RSK/activator protein-1 signalling pathway. Shows positive effects on the incidence of prostate cancer and physiological changes after menopause. Functions as a DHT blocker. Preferentially activates estrogen receptor β (ERβ).

Product Specific Literature References

Comparisons of percent equol producers between prostate cancer patients and controls: case-controlled studies of isoflavones in Japanese, Korean and American residents: H. Akaza, et al.; Jpn. J. Clin. Oncol. 34, 86 (2004) Abstract; Full Text
Mammographic density in relation to daidzein-metabolizing phenotypes in overweight, postmenopausal women: C.L. Frankenfeld, et al.; Cancer Epidemiol. Biomarkers Prev. 13, 1156 (2004) Abstract; Full Text
Equol is a novel anti-androgen that inhibits prostate growth and hormone feedback: T.D. Lund, et al.; Biol. Reprod. 70, 1188 (2004) Abstract; Full Text
Phytoestrogens and their human metabolites show distinct agonistic and antagonistic properties on estrogen receptor alpha (ERalpha) and ERbeta in human cells: S.O. Mueller, et al.; Toxicol. Sci. 80, 14 (2004) Abstract; Full Text
High concordance of daidzein-metabolizing phenotypes in individuals measured 1 to 3 years apart: C.L. Frankenfeld, et al.; Br. J. Nutr. 94, 873 (2005) Abstract
Equol, a metabolite of the soybean isoflavone daidzein, inhibits neoplastic cell transformation by targeting the MEK/ERK/p90RSK/activator protein-1 pathway: N.J. Kang, et al.; J. Biol. Chem. 282, 32856 (2007) Abstract; Full Text
Isoflavones, equol and cardiovascular disease: pharmacological and therapeutic insights: K.A. Jackman, et al.; Curr. Med. Chem. 14, 2824 (2007) Abstract

Further Categories Containing This Product:

Estrogen & Estrogen Receptors / Related Products • Antitumor Agents (Hormone-related) • Androgens & Androgen Receptors / Related Products • ERK1 & ERK2 / Related Products

ALX-380-092

Revised 03-Jul-08

Radicicol
SYNONYMS	Monorden 1aS-(1aR,2Z,4E,14,15aR*)]-8-Chloro-1a,14,15,15a-tetrahydro-9,11-dihydroxy-14-methyl-6H-oxireno[e][2]benzoxacyclotetradecin-6,12(7H)-dione
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Antifungal

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-092-M001		1 mg	75.00 USD
ALX-380-092-M005		5 mg	295.00 USD

Product Specification

FORMULA:	C₁₈H₁₇ClO₆
MW:	364.8
CAS NUMBER:	12772-57-5
MERCK INDEX:	14: 6253
RTECS:	RR1105000
SOURCE/HOST:	Isolated from Humicola fuscoatra.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to light yellow powder.
SOLUBILITY:	Soluble in DMSO, methanol or acetone.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
HAZARD:	MAY BE CARCINOGENIC. HARMFUL.

Product Description

Antifungal macrocyclic lactone antibiotic with antimalarial activity. Potent inhibitor of HSP90. Binds more strongly to HSP90 (nanomolar affinity) than to Grp94. Also binds to yeast HSP90, E. coli HtpG and TRAP-1. Non-competitive inhibitor of ATP citrate lyase. Anti-angiogenic. Specifically inhibits the interaction between HIF-1α/Arnt heterodimer and the hypoxia-responsive element (HRE), reducing VEGF expression. Protein tyrosine kinase inhibitor, e.g. p60^v-src(IC₅₀=0.27nM). Inhibitor of cyclooxygenase-2 (COX-2) expression (IC₅₀=27nM) without affecting COX-1 expression in LPS-stimulated macrophages. Induces the differentiation of HL-60 cells into macrophages, blocking cell cycle at G1 and G2. Suppressor of NIH 3T3 cell transformation by diverse oncogenes such as mos, ras and src in part by blocking the key signal transduction intermediates such as MAP kinase and GAP-associated p62. Inhibitor of AP-1-, NF-κB- and serum response factor (SRF)-mediated transcription (e.g. expression of iNOS). Represses the transcriptional function of the estrogen receptor. Inhibits archeal growth and DNA topoisomerase VI (a Topo IIB family topoisomerase). Blocks replication of negative-strand RNA viruses.

Product Specific Literature References

Potent and specific inhibition of p60v-src protein kinase both in vivo and in vitro by radicicol: H.J. Kwon, et al.; Cancer Res. 52, 6926 (1992) Abstract
Radicicol, a microbial cell differentiation modulator, inhibits in vivo angiogenesis: T. Oikawa, et al.; Eur. J. Pharmacol. 241, 221 (1993) Abstract
Radicicol, a protein tyrosine kinase inhibitor, suppresses the expression of mitogen-inducible cyclooxygenase in macrophages stimulated with lipopolysaccharide and in experimental glomerulonephritis: P. Chanmugam, et al.; J. Biol. Chem. 270, 5418 (1995) Abstract; Full Text
Suppression of RAS and MOS transformation by radicicol: J.F. Zhao, et al.; Oncogene 11, 161 (1995) Abstract
Induction of differentiation of HL-60 cells by the anti-fungal antibiotic, radicicol: Y. Shimada, et al.; J. Antibiot. 48, 824 (1995) Abstract
Radicicol inhibits tyrosine phosphorylation of the mitotic Src substrate Sam68 and retards subsequent exit from mitosis of Src-transformed cells: I. Pillay, et al.; Cell Growth Differ. 7, 1487 (1996) Abstract
Radicicol leads to selective depletion of Raf kinase and disrupts K-Ras-activated aberrant signaling pathway: S. Soga, et al.; J. Biol. Chem. 273, 822 (1998) Abstract; Full Text
Antimalarial activity of radicicol, heptelidic acid and other fungal metabolites: Y. Tanaka, et al.; J. Antibiot. 51, 153 (1998) Abstract
Targeting of the protein chaperone, HSP90, by the transformation suppressing agent, radicicol: S.V. Sharma, et al.; Oncogene 16, 2369 (1998) Abstract
Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin: S.M. Roe, et al.; J. Med. Chem. 42, 260 (1999) Abstract
T.W. Schulte, et al.; Mol. Endocrinol. 13, 1435 (1999) Abstract; Full Text
Radicicol suppresses expression of inducible nitric-oxide synthase by blocking p38 kinase and nuclear factor-kappaB/Rel in lipopolysaccharide-stimulated macrophages: Y.J. Jeon, et al.; J. Pharmacol. Exp. Ther. 294, 548 (2000) Abstract; Full Text
Radicicol binds and inhibits mammalian ATP citrate lyase: S.W. Ki, et al.; J. Biol. Chem. 275, 39231 (2000) Abstract; Full Text
Radicicol suppresses transformation and restores tropomyosin-2 expression in both ras- and MEK-transformed cells without inhibiting the Raf/MEK/ERK signaling cascade: P.N. Kim, et al.; Cell Growth Differ. 12, 543 (2001) Abstract; Full Text
Radicicol-sensitive peptide binding to the N-terminal portion of GRP94: S. Vogen, et al.; J. Biol. Chem. 277, 40742 (2002) Abstract; Full Text
Reduction of hypoxia-induced transcription through the repression of hypoxia-inducible factor-1alpha/aryl hydrocarbon receptor nuclear translocator DNA binding by the 90-kDa heat-shock protein inhibitor radicicol: E. Hur, et al.; Mol. Pharmacol. 62, 975 (2002) Abstract; Full Text
Radicicol represses the transcriptional function of the estrogen receptor by suppressing the stabilization of the receptor by heat shock protein 90: M.O. Lee, et al.; Mol. Cell Endocrinol. 188, 47 (2002) Abstract
Development of radicicol analogues: S. Soga, et al.; Curr. Cancer Drug Targets 3, 359 (2003) Abstract
Heat shock protein 90 (Hsp90) chaperone complex inhibitor, radicicol, potentiated radiation-induced cell killing in a hormone-sensitive prostate cancer cell line through degradation of the androgen receptor: K. Harashima, et al.; Int. J. Radiat. Biol. 81, 63 (2005) Abstract
Inhibition of archaeal growth and DNA topoisomerase VI activities by the Hsp90 inhibitor radicicol: D. Gadelle, et al.; Nucleic Acid Res. 33, 2310 (2005) Abstract
Geldanamycin, radicicol, and chimeric inhibitors of the Hsp90 N-terminal ATP binding site: M.K. Hadden, et al.; Curr. Top. Med. Chem. 6, 1173 (2006), Review Abstract
The topoisomerase II-Hsp90 complex: a new chemotherapeutic target?: C.R. Barker, et al.; Int. J. Cancer 118, 2685 (2006) Abstract
Structural basis for topoisomerase VI inhibition by the anti-Hsp90 drug radicicol: K.D. Corbett & J.M. Berger; Nucleic Acids Res. 34, 4269 (2006) Abstract
Chemistry and biology of resorcylic acid lactones: N. Winssinger & S. Barluenga; Chem. Commun. (Camb.) 22 (2007) Abstract
Antiviral activity and RNA polymerase degradation following Hsp90 inhibition in a range of negative strand viruses: J.H. Connor, et al.; Virology 362, 109 (2007) Abstract

Further Categories Containing This Product:

NF-kB Pathway Inhibitors • Tyrosine Kinase Inhibitors • Estrogen & Estrogen Receptors / Related Products • Antibiotics - Nitric Oxide Pathway Modulators • Antitumor Agents (Hormone-related) • Malaria / Related Products • Antibiotics - Antimalarial • Antibiotics - Protein Kinase Inhibitors • Antibiotics - NF-kB Inhibitors • Antibiotics for Angiogenesis Research • Antibiotics for Cell Cycle Research • Cell Cycle Blockers & Inhibitors / Related Products • HSP90 / HtpG / Related Products • Antibiotics - Topoisomerase Inhibitors • RNA Polymerases / Related Products

ALX-270-309

Revised 23-Apr-08

T0901317
SYNONYMS	N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide
PRODUCT LINE	DNA Regulation / Transcription
PRODUCT CATEGORY	Nuclear Receptors Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-309-M010		10 mg	30.00 USD
ALX-270-309-M050		50 mg	120.00 USD

Product Specification

FORMULA:	C₁₇H₁₂NF₉O₃S
MW:	481.3
CAS NUMBER:	293754-55-9
PURITY:	≥98% (TLC)
APPEARANCE:	White to off-white crystalline solid.
SOLUBILITY:	50mg/ml soluble in 100% ethanol, DMSO, dimethyl formamide or any organic solvent; also soluble in a 1:1 solution of DMSO:PBS, pH 7.2 (500µg/ml).
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
USE/STABILITY:	We do not recommend storing the aqueous solutions for more than one day.
HAZARD:	HARMFUL.
IDENTITY:	Identity determined by NMR.

Product Description

Potent agonist (EC₅₀=50nM) of the orphan nuclear hormone receptor (liver X receptor; LXR). Inhibitor of human sex hormone-dependent cancer cell lines.

Product Specific Literature References

Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers: J.J. Repa, et al.; Science 289, 1524 (2000) Abstract
Role of LXRs in control of lipogenesis: J.R. Schultz, et al.; Genes Dev. 14, 2831 (2000) Abstract; Full Text
Expression of sterol regulatory element-binding protein 1c (SREBP-1c) mRNA in rat hepatoma cells requires endogenous LXR ligands: R.A. DeBose-Boyd, et al.; PNAS 98, 1477 (2001) Abstract; Full Text
LXRs control lipid-inducible expression of the apolipoprotein E gene in macrophages and adipocytes: B.A. Laffitte, et al.; PNAS 98, 507 (2001) Abstract; Full Text
Antiproliferative effect of liver X receptor agonists on LNCaP human prostate cancer cells: J. Fukuchi, et al.; Cancer Res. 64, 7686 (2004) Abstract
The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells: C.P. Chuu et al.; Biochem. Biophys. Res. Commun. 357, 341 (2007) Abstract

Further Categories Containing This Product:

Antitumor Agents (Hormone-related)

ALX-550-095

Revised 02-May-06

Tamoxifen . citrate
SYNONYMS	(Z)-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethyl-ethanamine . citrate
PRODUCT LINE	Cancer
PRODUCT CATEGORY	Antitumor Agents (Hormone-related)

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-550-095-G001		1 g	85.00 USD

Product Specification

FORMULA:	C₂₆H₂₉NO . C₆H₈O₇
MW:	371.5 . 192.1
CAS NUMBER:	54965-24-1
MERCK INDEX:	14: 9048
RTECS:	KH2387000
PURITY:	≥99%
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in methanol; very slightly soluble in water or acetone.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	TOXIC. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description

Antiestrogen. Selective protein kinase C (PKC) inhibitor. Induces apoptosis.

Product Specific Literature References

Inhibition of protein kinase C by tamoxifen: C.A. O'Brian, et al.; Cancer Res. 45, 2462 (1985) Abstract
Opposite effects of tamoxifen on in vitro protein kinase C activity and endogenous protein phosphorylation in intact MCF-7 cells: M. Issandou, et al.; Cancer Res. 50, 5845 (1990) Abstract
Signalling targets for anticancer drug development: G. Powis; TIPS 12, 188 (1991), (Review) Abstract
Protein kinase C inhibitors induce apoptosis in human malignant glioma cell lines: W.T. Couldwell, et al.; FEBS Lett. 345, 43 (1994) Abstract
Tamoxifen: teaching an old drug new tricks?: D.J. Grainge & J.C. Metcalfe; Nat. Med. 2, 381 (1996), (Review) Abstract
G

FORMULA:	C₂₂H₂₉FO₅
MW:	392.5
CAS NUMBER:	50-02-2
MERCK INDEX:	14: 2943
RTECS:	TU3980000
PURITY:	≥98%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO, 100% ethanol or methanol. Slightly soluble in acetone or chloroform. Insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.
HAZARD:	HARMFUL. MAY BE TERATOGENIC.