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DNA Metabolism
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ALX-380-290 Revised 15-Apr-08 New product
Enrofloxacin
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SYNONYMS 1,4-Dihydro-1-cyclopropyl-7-(4-ethyl-1-piperazinyl)-6-fluoro-4-oxo-3-quinolinecarboxylic acid
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-290-G005   5 g 30.00 USD Add To Cart
ALX-380-290-G025   25 g 120.00 USD Add To Cart
Product Specification
FORMULA: C19H22FN3O3
MW: 359.4
CAS NUMBER: 93106-60-6
MERCK INDEX: 14: 3592
RTECS: VB1993650
PURITY: ≥98% (Assay)
APPEARANCE: White to light yellow crystalline powder.
SOLUBILITY: Slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Fluoroquinolone with broad spectrum activity against Gram-negative and Gram-positive bacteria as well as against Mycoplasma spp. Inhibits bacterial DNA-gyrase (topoisomerase).

Product Specific Literature References
Enrofloxacin: a new antimicrobial agent: J. Schroder; J. S. Afr. Vet. Assoc. 60, 122 (1989) Abstract
 
 
ALX-270-209 Revised 05-Apr-08
Etoposide
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SYNONYMS 4-Desmethylepipodophyllotoxin 9-(4,6-O-ethylidene)-β-D-glucopyranoside
VP-16-213
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Topoisomerase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-209-M025   25 mg 30.00 USD Add To Cart
ALX-270-209-M100   100 mg 65.00 USD Add To Cart
ALX-270-209-M500   500 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C29H32O13
MW: 588.6
CAS NUMBER: 33419-42-0
MERCK INDEX: 14: 3886
RTECS: KC0190000
SOURCE/HOST: Semisynthetic derivative of podophyllotoxin.
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO, dimethyl formamide, ethyl ether or chloroform:methanol (1:1); slightly soluble in methanol or acetone; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Store solutions in DMSO at 4°C. For long term storage prepare aliquots and store at -20°C.
HANDLING: Protect from light and moisture.
HAZARD: MAY BE CARCINOGENIC. TOXIC.

Product Description
Antitumor reagent. Topoisomerase II inhibitor. Induces apoptosis by FasL. Activates p53 resulting in upregulated expression of TRAIL-R2 (DR5) and Bak to overcome TRAIL resistance in Bax-deficient human colon carcinoma cancer cells.
Product Specific Literature References
The podophyllotoxin derivatives VP16-213 and VM26: B.F. Issell; Cancer Chemother. Pharmacol. 7, 73 (1982) Abstract
Etoposide: four decades of development of a topoisomerase II inhibitor: K.R. Hande; Eur. J. Cancer 34, 1514 (1998) Abstract
Etoposide sensitivity of human prostatic cancer cell lines PC-3, DU 145 and LNCaP: M. Salido, et al.; Histol. Histopathol. 14, 125 (1999) Abstract
A systematic review of the role of etoposide and cisplatin in the chemotherapy of small cell lung cancer with methodology assessment and meta-analysis: C. Mascaux, et al.; Lung Cancer 30, 23 (2000) Abstract
Distinct pathways for stimulation of cytochrome c release by etoposide: J.D. Robertson, et al.; J. Biol. Chem. 275, 32438 (2000) Abstract; Full Text
Ordering of ceramide formation, caspase activation, and Bax/Bcl-2 expression during etoposide-induced apoptosis in C6 glioma cells: M. Sawada, et al.; Cell Death Differ. 7, 761 (2000) Abstract
Etoposide-induced apoptosis is not associated with the fas pathway in acute myeloblastic leukemia cells: T. Siitonen, et al.; Leuk. Res. 24, 281 (2000) Abstract
Early caspase activation in leukemic cells subject to etoposide-induced G2-M arrest: evidence of commitment to apoptosis rather than mitotic cell death: R.J. Sleiman & B.W. Stewart; Clin. Cancer Res. 6, 3756 (2000) Abstract; Full Text
Cell cycle phase specificity in the potentiation of etoposide-induced DNA damage and apoptosis by KN-62, an inhibitor of calcium-calmodulin- dependent enzymes: M. Aoyama, et al.; Biochem Pharmacol 61, 49 (2001) Abstract
Deacetylase activity associates with topoisomerase II and is necessary for etoposide-induced apoptosis: C.A. Johnson, et al.; J. Biol. Chem. 276, 4539 (2001) Abstract; Full Text
In vitro topo II-DNA complex accumulation and cytotoxicity of etoposide in leukaemic cells from patients with acute myelogenous and chronic lymphocytic leukaemia: Y. Wang, et al.; Leuk. Res. 25, 133 (2001) Abstract
Etoposide: discovery and medicinal chemistry: P. Meresse, et al.; Curr. Med. Chem. 11, 2443 (2004), Review Abstract
Etoposide, topoisomerase II and cancer: E.L. Baldwin & N. Osheroff; Curr. Med. Chem. Anticancer Agents 5, 363 (2005), Review Abstract
 
 
ALX-480-100 Revised 27-Mar-08 New product
Fludarabine
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SYNONYMS 2-Fluoroadenine-9-β-D-arabinofuranoside
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Apoptosis Inducers)
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ALX-480-100-M005   5 mg 45.00 USD Add To Cart
ALX-480-100-M025   25 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C10H12FN5O4
MW: 285.2
CAS NUMBER: 21679-14-1
MERCK INDEX: 14: 4126
RTECS: AU6207000
PURITY: ≥98% (HPLC)
APPEARANCE: White to pale yellow crystalline powder.
SOLUBILITY: Sparingly soluble in water or organic solvents.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
IDENTITY: Determined by IR.

Product Description

Prodrug converted to the free nucleoside 9-β-D-arabinosyl-2-fluoroadenine (F-ara-A). F-ara-A enters cells and accumulates as the 5’-triphosphate. Interferes with DNA synthesis and repair. Induces apoptosis of cancer cells. Inhibits RNA transcription.

Product Specific Literature References
Fludarabine: a new agent with major activity against chronic lymphocytic leukemia: M.J. Keating, et al.; Blood 74, 19 (1989) Abstract; Full Text
Termination of DNA synthesis by 9-beta-D-arabinofuranosyl-2-fluoroadenine. A mechanism for cytotoxicity: P. Huang, et al.; J. Biol. Chem. 265, 16617 (1990) Abstract; Full Text
Action of 9-beta-D-arabinofuranosyl-2-fluoroadenine on RNA metabolism: P. Huang & W. Plunkett; Mol. Pharmacol. 39, 449 (1991) Abstract
Inhibition of RNA transcription: a biochemical mechanism of action against chronic lymphocytic leukemia cells by fludarabine: P. Huang, et al.; Leukemia 14, 1405 (2000) Abstract
Role of fludarabine in hematological malignancies: M. Montillo, et al.; Expert Rev. Anticancer Ther. 6, 1141 (2006) Abstract
Fludarabine-mediated suppression of the excision repair enzyme ERCC1 contributes to the cytotoxic synergy with the DNA minor groove crosslinking agent SJG-136 (NSC 694501) in chronic lymphocytic leukaemia cells: C. Pepper, et al.; Br. J. Cancer 97, 253 (2007) Abstract
Fludarabine induces apoptosis of human T-cell leukemia virus type 1-infected T cells via inhibition of the nuclear factor-kappaB signal pathway: C. Nishioka, et al.; Leukemia 21, 1044 (2007) Abstract
 
 
ALX-480-099 Revised 25-Mar-08 New product
5-Fluorouracil
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SYNONYMS 5-FU
2,4-Dioxo-5-fluoropyrimidine
5-Fluoro-2,4(1H,3H)-pyrimidinedione
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Apoptosis Inducers)
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-480-099-G001   1 g 15.00 USD Add To Cart
ALX-480-099-G005   5 g 60.00 USD Add To Cart
Product Specification
FORMULA: C4H3FN2O2
MW: 130.1
CAS NUMBER: 51-21-8
MERCK INDEX: 14: 4181
RTECS: YR0350000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white crystalline powder.
SOLUBILITY: Soluble in DMSO (5mg/ml), dimethyl formamide (5mg/ml), methanol (1mg/ml) or hot water (1mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.
IDENTITY: Determined by IR and UV.

Product Description

Potent antitumor agent. Inhibits thymidylate synthetase. Induces p53-dependent apoptosis.

Product Specific Literature References
Apoptosis of human primary and metastatic colon adenocarcinoma cell lines in vitro induced by 5-fluorouracil, verapamil, and hyperthermia: I.B. Shchepotin, et al.; Anticancer Res. 14, 1027 (1994) Abstract
Modulation of the equilibrative nucleoside transporter by inhibitors of DNA synthesis: J. Pressacco, et al.; Br. J. Cancer 72, 939 (1995) Abstract
Nucleoside-mediated mitigation of 5-fluorouracil-induced toxicity in synchronized murine erythroleukemic cells: K.H. Elstein, et al.; Toxicol. Appl. Pharmacol. 146, 29 (1997) Abstract
Effects of perturbations of pools of deoxyribonucleoside triphosphates on expression of ribonucleotide reductase, a G1/S transition state enzyme, in p53-mutated cells: S. Wadler, et al.; Biochem. Pharmacol. 55, 1353 (1998) Abstract
Chemically-induced apoptosis: p21 and p53 as determinants of enterotoxin activity: D.M. Pritchard, et al.; Toxicol. Lett. 102, 19 (1998) Abstract
Effect of 5-fluorouracil on cell cycle regulatory proteins in human colon cancer cell line: H. Takeda, et al.; Jpn. J. Cancer Res. 90, 677 (1999) Abstract
5-fluorouracil sensitivity and dihydropyrimidine dehydrogenase activity in advanced gastric cancer: T. Inada, et al.; Anticancer Res. 20, 2457 (2000) Abstract
Further Categories Containing This Product:
DNA Replication Other Products
 
 
ALX-380-065 Revised 21-Feb-08
Fostriecin
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SYNONYMS Phosphotrienin
CI-920
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Topoisomerase Inhibitors
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ALX-380-065-C010   10 µg 150.00 USD Add To Cart
Product Specification
FORMULA: C19H26O9PNa
MW: 452.4
CAS NUMBER: 87860-39-7
RTECS: UQ0600000
SOURCE/HOST: Isolated from Streptomyces pulveraceous subsp. fostreus.
PURITY: ≥98% (HPLC)
APPEARANCE: Colorless solid.
SOLUBILITY: Soluble in water (50 mg/ml), methanol (10 mg/ml) or 100 % ethanol (10 mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year when stored at -20°C. Use fresh solution.
HANDLING: Protect from light. Hygroscopic. Packaged under inert gas.

Product Description
Antitumor antibiotic. Catalytic inhibitor of topoisomerase II. Strong protein phosphatase 2A (PP2A) inhibitor (IC50=3.2nM). Weak inhibitor for PP1 (IC50=131µM). No apparent effect on PP2B. The binding site for fostriecin on PP2A is different from that of okadaic acid (see Prod. No. ALX-350-003).
Product Specific Literature References
Novel antitumor agents CI-920, PD 113,270 and PD 113,271. II. Isolation and characterization: S.S. Stampwala, et al.; J. Antibiot. (Tokyo) 36, 1601 (1983) Abstract
Novel antitumor agents CI-920, PD 113,270 and PD 113,271. I. Taxonomy, fermentation and biological properties: J.B. Tunac, et al.; J. Antibiot. (Tokyo) 36, 1595 (1983) Abstract
Studies on the biochemical mechanism of the novel antitumor agent, CI- 920: D.W. Fry, et al.; Cancer Chemother. Pharmacol. 13, 171 (1984) Abstract
Anticancer activity of the structurally novel antibiotic Cl-920 and its analogues: W.R. Leopold, et al.; Cancer Res. 44, 1928 (1984) Abstract
Inhibition of type II topoisomerase by fostriecin: T.J. Boritzki, et al.; Biochem. Pharmacol. 37, 4063 (1988) Abstract
Comparison of effects of fostriecin, novobiocin, and camptothecin, inhibitors of DNA topoisomerases, on DNA replication and repair in human cells: C.M. Gedik & A.R. Collins; Nucl. Acids Res. 18, 1007 (1990) Abstract
The cell cycle related differences in susceptibility of HL-60 cells to apoptosis induced by various antitumor agents: W. Gorczyca, et al.; Cancer Res. 53, 3186 (1993) Abstract
Induction of DNA strand breaks associated with apoptosis during treatment of leukemias: W. Gorczyca, et al.; Leukemia 7, 659 (1993) Abstract
Antitumor drug fostriecin inhibits the mitotic entry checkpoint and protein phosphatases 1 and 2A: M. Roberge, et al.; Cancer Res. 54, 6115 (1994) Abstract
Fostriecin: a review of the preclinical data: R.S. de Jong, et al.; Anticancer Drugs 8, 413 (1997) Abstract
Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A: A.H. Walsh, et al.; FEBS Lett. 416, 230 (1997) Abstract
Fostriecin, an inhibitor of protein phosphatase 2A, limits myocardial infarct size even when administered after onset of ischemia: C. Weinbrenner, et al.; Circulation 98, 899 (1998) Abstract
Phase I and pharmacokinetic study of the topoisomerase II catalytic inhibitor fostriecin: R.S. de Jong, et al.; Br. J. Cancer 79, 882 (1999) Abstract
Fostriecin: chemistry and biology: D.S. Lewy, et al.; Curr. Med. Chem. 9, 2005 (2002) Abstract
 
 
ALX-380-291 Revised 15-Apr-08 New product
Gatifloxacin
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SYNONYMS AM-1155
1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-291-G001   1 g 60.00 USD Add To Cart
ALX-380-291-G005   5 g 240.00 USD Add To Cart
Product Specification
FORMULA: C19H22FN3O4
MW: 375.4
CAS NUMBER: 112811-59-3
MERCK INDEX: 14: 4376
PURITY: ≥98% (Assay)
APPEARANCE: White to yellow crystalline powder.
SOLUBILITY: Soluble in water at pH 2-5 (40-60mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Fluoroquinolone with broad spectrum activity against Gram-negative and Gram-positive bacteria. Inhibits bacterial DNA-gyrase and topoisomerase IV. May cause dysglycemia.

Product Specific Literature References
Comparison of the antibacterial activities of the quinolones Bay 12-8039, gatifloxacin (AM 1155), trovafloxacin, clinafloxacin, levofloxacin and ciprofloxacin: A. Bauernfeind; J. Antimicrob. Chemother. 40, 639 (1997) Abstract; Full Text
Activities of gatifloxacin compared to those of seven other agents against anaerobic organisms: L.M. Ednie, et al.; Antimicrob. Agents Chemother. 42, 2459 (1998) Abstract; Full Text
Inhibitory activities of gatifloxacin (AM-1155), a newly developed fluoroquinolone, against bacterial and mammalian type II topoisomerases: M. Takei, et al.; Antimicrob. Agents Chemother. 42, 2678 (1998) Abstract; Full Text
Primary targets of fluoroquinolones in Streptococcus pneumoniae: H. Fukuda & K. Hiramatsu; Antimicrob. Agents Chemother. 43, 410 (1999) Abstract; Full Text
Gatifloxacin: C.M. Perry, et al.; Drugs 58, 683 (1999), (Review) Abstract
Contributions of the 8-methoxy group of gatifloxacin to resistance selectivity, target preference, and antibacterial activity against Streptococcus pneumoniae: H. Fukuda, et al.; Antimicrob. Agents Chemother. 45, 1649 (2001) Abstract; Full Text
Gatifloxacin affects GLUT1 gene expression and disturbs glucose homeostasis in vitro: T.F. Ge, et al.; Eur. J. Pharmacol. 573, 70 (2007) Abstract
Gatifloxacin-associated hypoglycemia: T. Ali, et al.; J. Okla. State Med. Assoc. 100, 425 (2007) Abstract
Gatifloxacin produces both hypoglycemia and hyperglycemia: a retrospective study: H. Haerian, et al.; Am. J. Med. Sci. 335, 95 (2008) Abstract
 
 
ALX-350-006 Revised 05-Apr-08
Genistein (synthetic)
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SYNONYMS 4',5,7-Trihydroxyisoflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-006-M010   10 mg 25.00 USD Add To Cart
ALX-350-006-M025   25 mg 50.00 USD Add To Cart
ALX-350-006-M050   50 mg 90.00 USD Add To Cart
ALX-350-006-M100   100 mg 150.00 USD Add To Cart
ALX-350-006-G001   1 g 480.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 446-72-0
MERCK INDEX: 14: 4391
RTECS: NR2392000
SOURCE/HOST: Synthetic.
PURITY: ≥99% (HPLC)
APPEARANCE: White to yellow crystalline powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Tyrosine protein kinase inhibitor. Inhibits phosphorylation of EGFR kinase. Inhibits tumor cell proliferation and induces tumor cell differentiation. Inhibits topoisomerase II activity in vivo. Produces cell cycle arrest and apoptosis. Direct inhibitor of insulin-induced glucose uptake in adipocytes (IC50=20µM).
Product Specific Literature References
Genistein, a specific inhibitor of tyrosine-specific protein kinases: T. Akiyama, et al.; J. Biol. Chem. 262, 5592 (1987) Abstract; Full Text
Erbstatin blocks platelet activating factor-induced protein-tyrosine phosphorylation, polyphosphoinositide hydrolysis, protein kinase C activation, serotonin secretion and aggregation of rabbit platelets: H. Salari, et al.; FEBS Lett. 263, 104 (1990) Abstract
Mechanisms of cancer chemoprevention by soy isoflavone genistein: F.H. Sarkar & Y. Li; Cancer Metastasis Rev. 21, 265 (2002) Abstract
Soy isoflavone phyto-pharmaceuticals in interleukin-6 affections. Multi-purpose nutraceuticals at the crossroad of hormone replacement, anti-cancer and anti-inflammatory therapy: N. Dijsselbloem, et al.; Biochem. Pharmacol. 68, 1171 (2004), Review Abstract
Genistein affects testosterone secretion by Leydig cells in roosters (Gallus gallus domesticus): M. Opalka, et al.; Reprod. Biol. 4, 185 (2004) Abstract
Genistein directly inhibits GLUT4-mediated glucose uptake in 3T3-L1 adipocytes: M. Bazuine, et al.; BBRC 325, 511 (2005) Abstract
Decreased circulating levels of tumor necrosis factor-alpha in postmenopausal women during consumption of soy-containing isoflavones: Y. Huang, et al.; J. Clin. Endocrinol. Metab. 90, 3956 (2005) Abstract
Phytoestrogens and lipoproteins in women: C.N. Bairey Merz, et al.; J. Clin. Endocrinol. Metab. 91, 2209 (2006) Abstract
Clinical review: a critical evaluation of the role of soy protein and isoflavone supplementation in the control of plasma cholesterol concentrations: A. Dewell, et al.; J. Clin. Endocrinol. Metab. 91, 772 (2006), Review Abstract
The role of genistein and synthetic derivatives of isoflavone in cancer prevention and therapy: F.H. Sarkar, et al.; Mini Rev. Med. Chem. 6, 401 (2006), Review Abstract
 
 
ALX-350-247 Revised 21-May-08
Genistin
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SYNONYMS Genistein-7-O-glucoside
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-247-M010   10 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C21H20O10
MW: 432.4
CAS NUMBER: 529-59-9
MERCK INDEX: 14: 4391
PURITY: ≥98%