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EGFR Kinase Inhibitors
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ALX-350-256 Revised 07-Oct-08
(+)-Aeroplysinin-1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-256-M001   1 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C9H9Br2NO3
MW: 339.0
CAS NUMBER: 28656-91-9
SOURCE/HOST: Isolated from Aplysina aerophoba.
PURITY: ≥97%
APPEARANCE: Oil.
SOLUBILITY: Soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Displays cytostatic and cytotoxic activity. Inhibitor of EGFR kinase. Shows antiangiogenic activity.
Product Specific Literature References
Aeroplysinin-1, an antibacterial bromo-compound from the sponge Verongia aerophoba: E. Fattorusso, et al.; J. Chem. Soc. 1, 16 (1972) Abstract
Cytostatic activity of aeroplysinin-1 against lymphoma and epithelioma cells: M.H. Kreuter, et al.; Z. Naturforsch. [C] 44, 680 (1989) Abstract
Inhibition of intrinsic protein tyrosine kinase activity of EGF-receptor kinase complex from human breast cancer cells by the marine sponge metabolite (+)-aeroplysinin-1: M.H. Kreuter, et al.; Comp. Biochem. Physiol. B 97, 151 (1990) Abstract
Production of the cytostatic agent aeroplysinin by the sponge Verongia aerophoba in in vitro culture: M.H. Kreuter, et al.; Comp. Biochem. Physiol. 101C, 183 (1992) Abstract
Antibiotic and cytotoxic activity of brominated compounds from the marine sponge Verongia aerophoba: R. Teeyapant, et al.; Z. Naturforsch. [C] 48, 939 (1993) Abstract
Cytotoxicity and mode of action of aeroplysinin-1 and a related dienonefrom the sponge Aplysina aerophoba: A. Koulman, et al.; J. Nat. Prod. 59, 591 (1996) Abstract
Antiangiogenic activity of aeroplysinin-1, a brominated compound isolated from a marine sponge: S. Rodriguez-Nieto, et al.; FASEB J. 16, 261 (2002) Abstract
 
 
ALX-270-313 Revised 03-Mar-05
BPIQ-I
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SYNONYMS 8-[(3-Bromophenyl)amino]-3-methyl-3H-imidazo[4,5-γ]-quinazoline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-313-M001   1 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C16H12BrN5
MW: 354.2
PURITY: ≥95%
APPEARANCE: Off white to yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC50=25 pM).
Product Specific Literature References
Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor: G.W. Rewcastle, et al.; J. Med. Chem. 39, 918 (1996) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-270-338 Revised 03-Mar-05
BPIQ-II
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SYNONYMS 8-[(3-Bromophenyl)amino]-1H-imidazo[4,5-γ]-quinazoline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-338-M001   1 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C15H10BrN5
MW: 340.2
PURITY: ≥98%
APPEARANCE: Pale pink solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC50=8pM).
Product Specific Literature References
Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor: G.W. Rewcastle, et al.; J. Med. Chem. 39, 918 (1996) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-350-246 Revised 07-Oct-08
Butein
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SYNONYMS 2',3,4,4'-Tetrahydroxychalcone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-246-M010   10 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C15H12O5
MW: 272.3
CAS NUMBER: 487-52-5
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (>50mg/ml) or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Keep cool and dry under inert gas.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Plant polyphenol. Specific tyrosine kinase inhibitor. Potently inhibits the tyrosine kinase activity of the EGF receptor and p60c-src. Potent antioxidant and anti-inflammatory agent. Inhibits glutathione reductase and rat liver glutathione S-transferase. Activator of human deacetylase SIRT1. Inhibits aromatase, showing chemopreventive properties. Directly inhibits IKK.
Product Specific Literature References
Inhibition of 12-O-tetradecanoylphorbol-13-acetate-mediated epidermal ornithine decarboxylase induction and skin tumor promotion by new lipoxygenase inhibitors lacking protein kinase C inhibitory effects: E. Aizu, et al.; Carcinogenesis 7, 1809 (1986) Abstract
Protective effects of hydroxychalcones on free radical-induced cell damage: S. Sogawa, et al.; Biol. Pharm. Bull. 17, 251 (1994) Abstract
Cytotoxic effect of butein on human colon adenocarcinoma cell proliferation: C.C. Yit & N.P. Das; Cancer Lett. 82, 65 (1994) Abstract
Inhibitory effects of plant polyphenols on rat liver glutathione S-transferase: K. Zhang & N.P. Das; Biochem. Pharmacol. 47, 2063 (1994) Abstract
Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor: S.M. Yu, et al.; Eur. J. Pharmacol. 280, 69 (1995) Abstract
Butein (3,4,2',4'-tetrahydroxychalcone) ameliorates experimantal anti-glomerular basement membrane antibody-associated glomerulonephritis (3): K. Hayashi, et al.; Eur. J. Pharmacol. 316, 297 (1996) Abstract
Inhibition of glutathione reductase by plant polyphenols: K. Zhang, et al.; Biochem. Pharmacol 54, 1047 (1997) Abstract
Butein, a specific protein tyrosine kinase inhibitor: E.-B. Yang, et al.; BBRC 245, 435 (1998) Abstract
Antioxidant properties of butein isolated from Dalbergia odorifera: Z.J. Cheng, et al.; Biochim. Biophys. Acta 1392, 291 (1998) Abstract
Flavonoids inhibit cell growth and induce apoptosis in B16 melanoma 4A5 cells: K. Iwashita, et al.; Biosci. Biotechnol. Biochem. 64, 1813 (2000) Abstract
Butein, a plant polyphenol, induces apoptosis concomitant with increased caspase-3 activity, decreased Bcl-2 expression and increased Bax expression in HL-60 cells: N.Y. Kim, et al.; Pharmacol. Toxicol. 88, 261 (2001) Abstract
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003) Abstract
The plant polyphenol butein inhibits testosterone-induced proliferation in breast cancer cells expressing aromatase: Y. Wang, et al.; Life Sci. 77, 39 (2005) Abstract
Butein, a tetrahydroxychalcone, inhibits nuclear factor (NF)-kappaB and NF-kappaB-regulated gene expression through direct inhibition of IkappaBalpha kinase beta on cysteine 179 residue: M.K. Pandey, et al.; J. Biol. Chem. 282, 17340 (2007) Abstract
 
 
ALX-270-314 Revised 04-Dec-07
CL-387,785
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SYNONYMS EKI-785
N-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-butynamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-314-M001   1 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C18H13BrN4O
MW: 381.2
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic. Protect from light. Packaged under inert gas.

Product Description
Irreversibly inhibits EGF-stimulated autophosphorylation of tyrosine residues in the epidermal growth factor receptor (EGFR) in vivo (IC50=250-490pM) and blocks EGF-mediated growth.
Product Specific Literature References
Irreversible inhibition of epidermal growth factor receptor tyrosine kinase with in vivo activity by N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide (CL-387,785): C.M. Discafani, et al.; Biochem. Pharmacol. 57, 917 (1999) Abstract
 
 
ALX-270-316 Revised 12-Jan-07
Compound 56
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SYNONYMS 4-[(3-Bromophenyl)amino]-6,7-diethoxyquinazoline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-316-C500   500 µg 135.00 USD Add To Cart
Product Specification
FORMULA: C18H18BrN3O2
MW: 388.3
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: MAY BE MUTAGENIC. HARMFUL.

Product Description
Potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC50=6pM).
Product Specific Literature References
Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor: A.J. Bridges, et al.; J. Med. Chem. 39, 267 (1996) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-350-028 Revised 12-Sep-08
Curcumin (high purity)
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SYNONYMS 1,7-bis(4-Hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione
Diferuloylmethane
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
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ALX-350-028-M010   10 mg 15.00 USD Add To Cart
ALX-350-028-M050   50 mg 60.00 USD Add To Cart
ALX-350-028-M250   250 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C21H20O6
MW: 368.4
CAS NUMBER: 458-37-7
MERCK INDEX: 14: 2673
SOURCE/HOST: Isolated from turmeric (Curcuma longa).
PURITY: ≥98.5% (Note: This highly purified product is free of demethoxy- and bis-demethoxycurcumin and does not contain 30-40% bioactive impurities)
APPEARANCE: Orange-yellow crystalline powder.
SOLUBILITY: Soluble in acetic acid or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Protect from light.

Product Description
Dual inhibitor of cyclooxygenase (COX) and 5-lipoxygenase. Also inhibits glutathione S-transferase, induction of nitric oxide (NO) in activated macrophages and inhibits EGF-induced tyrosine phosphorylation of EGF receptors. Antioxidant. Inhibitor of NAD(P)H:quinone oxidoreductase 1 (NQO1), disrupting the binding of NQO1 to wild type p53 inducing ubiquitin-independent degradation of p53 and inhibits p53-mediated apoptosis in normal thymocytes and myeloid leukemic cells.
Product Specific Literature References
Modification of certain inflammation-induced biochemical changes by curcumin: R. Srivastava & R.C. Srimal; Indian J. Med. Res. 81, 215 (1985) Abstract
Inhibition of 5-hydroxy-eicosatetraenoic acid (5-HETE) formation in intact human neutrophils by naturally-occurring diarylheptanoids: inhibitory activities of curcuminoids and yakuchinones: D.L. Flynn, et al.; Prostagl. Leukotr. Med. 22, 357 (1986) Abstract
Inhibitory effect of curcumin on epidermal growth factor receptor kinase activity in A431 cells: L. Korutla & R. Kumar; Biochim. Biophys. Acta 1224, 597 (1994) Abstract
Curcumin, an anti-tumour promoter and anti-inflammatory agent, inhibits induction of nitric oxide synthase in activated macrophages: I. Brouet & H. Okshima; BBRC 206, 533 (1995) Abstract
Cytotoxicity and cytoprotective activities of natural compounds. The case of curcumin: J.N. Commandeur & N.P. Vermeulen; Xenobiotica 26, 667 (1996) Abstract
Nitric oxide scavenging by curcuminoids: Sreejayan & M.N. Rao; J. Pharm. Pharmacol. 49, 105 (1997) Abstract
Inhibitory effects of curcumin on tumorigenesis in mice: M.T. Huang, et al.; J. Cell. Biochem. (Suppl.) 27, 26 (1997) Abstract
In vivo inhibition of nitric oxide synthase gene expression by curcumin, a cancer preventive natural product with anti-inflammatory properties: M.M. Chan, et al.; Biochem. Pharmacol. 55, 1955 (1998) Abstract
Effect of curcumin on the production of nitric oxide by cultured rat mammary gland: M. Onoda & H. Inano; Nitric Oxide 4, 505 (2000) Abstract
Suppression of nitric oxide oxidation to nitrite by curcumin is due to the sequestration of the reaction intermediate nitrogen dioxide, not nitric oxide: B.D. Johnston & E.G. DeMaster; Nitric Oxide 8, 231 (2003) Abstract
Biological properties of curcumin-cellular and molecular mechanisms of action: B. Joe, et al.; Crit. Rev. Food Sci. Nutr. 44, 97 (2004), (Review) Abstract
Curcumin, a major constituent of turmeric, corrects cystic fibrosis defects: M.E. Egan, et al.; Science 304, 600 (2004) Abstract
Inhibition of NAD(P)H:quinone oxidoreductase 1 activity and induction of p53 degradation by the natural phenolic compound curcumin: P. Tsvetkov, et al.; PNAS 102, 5535 (2005) Abstract
Immunomodulatory effects of curcumin: V.S. Yadav, et al.; Immunopharmacol. Immunotoxicol. 27, 485 (2005) Abstract
Curcumin, an atoxic antioxidant and natural NFkappaB, cyclooxygenase-2, lipooxygenase, and inducible nitric oxide synthase inhibitor: a shield against acute and chronic diseases: S. Bengmark; JPEN J. Parenter. Enteral. Nutr. 30, 45 (2006), (Review) Abstract
Curcumin is an inhibitor of p300 histone acetylatransferase: M.G. Marcu, et al.; Med. Chem. 2, 169 (2006) Abstract
Multiple biological activities of curcumin: a short review: R.K. Maheshwari, et al.; Life Sci. 78, 2081 (2006), (Review) Abstract
Curcumin inhibits hypoxia-induced angiogenesis via down-regulation of HIF-1: M.K. Bae, et al.; Oncol. Rep. 15, 1557 (2006) Abstract
Notch-1 down-regulation by curcumin is associated with the inhibition of cell growth and the induction of apoptosis in pancreatic cancer cells: Z. Wang, et al.; Cancer 106, 2503 (2006) Abstract
Curcumin improves wound healing by modulating collagen and decreasing reactive oxygen species: M. Panchatcharam, et al.; Mol. Cell Biochem. 290, 87 (2006) Abstract
Inhibitory effect of curcumin on nitric oxide production from lipopolysaccharide-activated primary microglia: K.K. Jung, et al.; Life Sci. 79, 2022 (2006) Abstract
The dietary compound curcumin inhibits p300 histone acetyltransferase activity and prevents heart failure in rats: T. Morimoto, et al.; J. Clin. Invest. 118, 868 (2008) Abstract; Full Text
 
 
ALX-270-281 Revised 28-Sep-06
Daphnetin
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SYNONYMS 7,8-Dihydroxycoumarin
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-281-M005   5 mg 25.00 USD Add To Cart
ALX-270-281-M025   25 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C9H6O4
MW: 178.1
CAS NUMBER: 486-35-1
RTECS: GN6382600
PURITY: ≥97%
APPEARANCE: White to rose powder.
SOLUBILITY: Soluble in 100% ethanol, methanol or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Inhibitor of protein kinases. EGF receptor tyrosine kinase (IC50=7.87µM), PKA (IC50=9.33µM), PKC (IC50=25.01µM). Antioxidant. Antimalarial agent.
Product Specific Literature References
Daphnetin: a novel antimalarial agent with in vitro and in vivo activity: Y.Z. Yang, et al.; Am. J. Trop. Med. Hyg. 46, 15 (1992) Abstract
Daphnetin, one of coumarin derivatives, is a protein kinase inhibitor: E.B. Yang, et al.; BBRC 260, 682 (1999) Abstract
 
 
ALX-270-263 Revised 03-Apr-08
(-)-Epigallocatechin gallate
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SYNONYMS EGCG
(2R,3R)-2-(3,4,5-Trihydroxyphenyl)-3,4-dihydro-1[2H]-benzopyran-3,5,7-triol 3-(3,4,5-trihydroxybenzoate)
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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ALX-270-263-M010   10 mg 20.00 USD Add To Cart
ALX-270-263-M050   50 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C22H18O11
MW: 458.4
CAS NUMBER: 989-51-5
MERCK INDEX: 14: 3526
SOURCE/HOST: Isolated from green tea.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to yellow powder.
SOLUBILITY: Soluble in 100% ethanol, dimethyl formamide or DMSO; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions in DMSO are stable for up to 3 months when stored at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Keep under inert gas. Protect from light.

Product Description
Antitumor reagent. Antioxidant. Protects cells from lipid peroxidation and DNA damage induced by reactive free radicals. Inhibits inducible nitric oxide synthase (iNOS; NOS II). Chemopreventive anticancer agent. Induces apoptosis in human cancer cell lines. Inhibits MAP kinase mediated signalling pathways. Inhibits angiogenesis. Inhibits telomerase and DNA methyltransferase. Anti-inflammatory agent.
Product Specific Literature References
Inhibitory effect of topical application of a green tea polyphenol fraction on tumor initiation and promotion in mouse skin: M.T. Huang, et al.; Carcinogenesis 13, 947 (1992) Abstract
Inhibition of 12-O-tetradecanoylphorbol-13-acetate and other skin tumor-promoter-caused induction of epidermal interleukin-1 alpha mRNA and protein expression in SENCAR mice by green tea polyphenols: S.K. Katiyar, et al.; J. Invest. Dermatol. 105, 394 (1995) Abstract
Growth inhibition and regression of human prostate and breast tumors in athymic mice by tea epigallocatechin gallate: S. Liao, et al.; Cancer Lett. 96, 239 (1995) Abstract
Inhibition of N-methyl-N'-nitro-N-nitrosoguanidine-induced carcinogenesis by (-)-epigallocatechin gallate in the rat glandular stomach: T. Yamane, et al.; Cancer Res. 55, 2081 (1995) Abstract
(-)-Epigallocatechin gallate, a polyphenolic tea antioxidant, inhibits peroxynitrite-mediated formation of 8-oxodeoxyguanosine and 3-nitrotyrosine: E.S. Fiala, et al.; Experientia 52, 922 (1996) Abstract
Green tea constituent epigallocatechin-3-gallate and induction of apoptosis and cell cycle arrest in human carcinoma cells: N. Ahmad, et al.; J. Natl. Cancer Inst. 89, 1881 (1997) Abstract
Inhibition of inducible nitric oxide synthase gene expression and enzyme activity by epigallocatechin gallate, a natural product from green tea: M.M. Chan, et al.; Biochem. Pharmacol. 54, 1281 (1997) Abstract
(-)-Epigallocatechin-3-gallate blocks the induction of nitric oxide synthase by down-regulating lipopolysaccharide-induced activity of transcription factor nuclear factor-kappaB: Y.L. Lin & J.K. Lin; Mol. Pharmacol. 52, 465 (1997) Abstract
Telomerase inhibition, telomere shortening, and senescence of cancer cells by tea catechins: I. Naasani, et al.; BBRC 249, 391 (1998) Abstract
Epigallocatechin suppression of proliferation of vascular smooth muscle cells: correlation with c-jun and JNK: L.H. Lu, et al.; Br. J. Pharmacol. 124, 1227 (1998) Abstract
ESR study on the structure-antioxidant activity relationship