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ALX-380-291

Revised 15-Apr-08

Gatifloxacin
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
ALX-380-291-G005		5 g	240.00 USD

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

Further Categories Containing This Product:

Antibiotics - DNA Replication Inhibitors • Antibiotics - Topoisomerase Inhibitors

ALX-350-006

Revised 05-Apr-08

Genistein (synthetic)
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
ALX-350-006-M025		25 mg	50.00 USD
ALX-350-006-M050		50 mg	90.00 USD
ALX-350-006-M100		100 mg	150.00 USD
ALX-350-006-G001		1 g	480.00 USD

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

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • TNF-alpha & TNF Receptors Other Products • Antitumor Agents (Enzyme Inhibitors) • Cell Cycle Blockers & Inhibitors/Related Products • EGFR Kinase Inhibitors • Antitumor Agents (Anti-proliferative) • Natural Products - Topoisomerase Inhibitors • Natural Products for Angiogenesis Research • Active Substances from Fruit and Vegetables • Flavonoids/Related Products • Natural Products - Antitumor Reagents • Natural Products for Cell Cycle Research • Natural Products - Apoptosis Inducers & Inhibitors • Antitumor Agents (Apoptosis Inducers)

ALX-350-247

Revised 21-May-08

Genistin
SYNONYMS	Genistein-7-O-glucoside
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-350-247-M010		10 mg	180.00 USD

Product Specification

FORMULA:	C₂₁H₂₀O₁₀
MW:	432.4
CAS NUMBER:	529-59-9
MERCK INDEX:	14: 4391
PURITY:	≥98%
APPEARANCE:	Off-white to light yellow powder.
SOLUBILITY:	Soluble in DMSO or dilute aqueous base; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C

Product Description

Glucoside of genistein (Prod. No. ALX-350-006) found in soy beans. Useful as a negative control for genistein and other tyrosine kinase inhibitors. Selective inhibitor of terminal deoxyribonucleotidyltransferase (TdT). Displays antioxidant and anticarcinogenic properties.

Product Specific Literature References

Soybean isoflavones, genistein and genistin, inhibit rat myoblast proliferation, fusion and myotube protein synthesis: S. Ji, et al.; J. Nutr. 129, 1291 (1999) Abstract
Daidzein and genistein but not their glucosides are absorbed from the rat stomach: M.K. Piskula, et al.; FEBS Lett. 447, 287 (1999) Abstract
Inhibition of CYP1A1 enzyme activity in mouse hepatoma cell culture by soybean isoflavones: H.G. Shertzer, et al.; Chem. Biol. Interact. 123, 31 (1999) Abstract
Selective inhibitors of terminal deoxyribonucleotidyltransferase (TdT): baicalin and genistin: Y. Uchiyama, et al.; Biochim. Biophys. Acta 1725, 298 (2005) Abstract
Genistin inhibits UV light-induced plasmid DNA damage and cell growth in human melanoma cells: A. Russo, et al.; J. Nutr. Biochem. 17, 103 (2006) Abstract
Pro-apoptotic effect and cytotoxicity of genistein and genistin in human ovarian cancer SK-OV-3 cells: E.J. Choi, et al.; Life Sci. 80, 1403 (2007) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • Natural Products - Topoisomerase Inhibitors • Natural Products - Chemopreventive Agents • Active Substances from Fruit and Vegetables • Natural Products - Antioxidants • Flavonoids/Related Products

ALX-380-260

Revised 07-Apr-08

Idarubicin . hydrochloride
SYNONYMS	Idamycin DMDR 4-Demethoxydaunorubicin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Apoptosis Inducers & Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-260-M001		1 mg	45.00 USD
ALX-380-260-M005		5 mg	180.00 USD

Product Specification

FORMULA:	C₂₆H₂₇NO₉ . HCl
MW:	497.5 . 36.5
CAS NUMBER:	57852-57-0
MERCK INDEX:	14: 4886
RTECS:	HB7877000
SOURCE/HOST:	Synthetic.
PURITY:	≥98%
APPEARANCE:	Orange crystalline solid.
SOLUBILITY:	Soluble in water or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	VERY TOXIC. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description

More potent, lipophilic and antineoplastic analog of daunorubicin. DNA-damaging effect includes DNA oxidation and methylation, DNA intercalation, inhibition of DNA synthesis, induction of DNA strand breaks and delay of cell cycle progression. Inhibitor of topoisomerase IIα. Produces endonucleolytic cleavage and is a marker of apoptosis.

Product Specific Literature References

Idarubicin (4-demethoxydaunorubicin). A preliminary overview of preclinical and clinical studies: F. Ganzina, et al.; Invest. New Drugs 4, 85 (1986), Review Abstract
Antitumor activity of idarubicin, a derivative of daunorubicin, against drug sensitive and resistant P388 leukemia: T. Tsuruo, et al.; Anticancer Res. 13, 357 (1993) Abstract
Study of apoptosis-related responses of leukemic blast cells to in vitro anthracycline treatment: M.A. Belaud-Rotureau, et al.; Leukemia 14, 1266 (2000) Abstract
A comparison of the in vitro genotoxicity of anticancer drugs idarubicin and mitoxantrone: J. Blasiak, et al.; Acta Biochim. Pol. 49, 145 (2002) Abstract; Full Text
Repair of idarubicin-induced DNA damage: A cause of resistance?: D.C. Dartsch & F. Gieseler; DNA Repair (Amst) 6, 1618 (2007) Abstract

Further Categories Containing This Product:

Antitumor Agents (DNA Interaction & Gene Regulation) • Antitumor Agents (Apoptosis Inducers) • Antitumor Antibiotics • Antibiotics - Topoisomerase Inhibitors

ALX-430-139

Revised 20-Feb-08

Irinotecan . hydrochloride . trihydrate
SYNONYMS	Camptosar 7-ethyl-10-hydroxycamptothecin CPT-11
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Topoisomerase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-430-139-M005		5 mg	90.00 USD
ALX-430-139-M025		25 mg	315.00 USD

Product Specification

FORMULA:	C₃₃H₃₈N₄O₆ . HCl . 3H₂O
MW:	586.7 . 36.4 . 54.0
CAS NUMBER:	100286-90-6; 136572-09-3
MERCK INDEX:	14: 5091
PURITY:	≥98% (HPLC)
APPEARANCE:	Pale yellow powder.
SOLUBILITY:	Slightly soluble in methanol or water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C

Product Description

A member of the camptothecin drug family, and an inhibitor of the nuclear enzyme topoisomerase I, which is involved in cellular DNA replication and transcription. During replication topoisomerase I mediates the relaxation of super coiled DNA, and its inhibition results in breakage of the DNA chain and likely induce apoptosis. Irinotecan is, therefore, an attractive target for anticancer drug development. Currently it is used for the treatment of small cell lung cancer and advanced colorectal cancer.

Product Specific Literature References

Induction of tumor necrosis factor by a camptothecin derivative, irinotecan, in mice and human mononuclear cells: S. Goto, et al.; Anticancer Res. 16, 2507 (1996) Abstract
The role of irinotecan in colorectal cancer: L.B. Saltz; Curr. Oncol. Rep. 1, 155 (1999) Abstract
Therapeutic advances in small cell lung cancer: F.P. Worden and G.P. Kalemkerian; Expert Opin. Investig. Drugs 9, 565 (2000) Abstract
Human DNA-Topoisomerases - Diagnostic and Therapeutic Implications for Cancer: U. Kellner, et al.; Onkologie 23, 424 (2000) Abstract
Irinotecan activates p53 with its active metabolite, resulting in human hepatocellular carcinoma apoptosis: Y. Takeba, et al.; J. Pharmacol. Sci. 104, 232 (2007) Abstract

Further Categories Containing This Product:

Antitumor Agents (Enzyme Inhibitors) • Natural Products - Antitumor Reagents

ALX-380-292

Revised 15-Apr-08

Levofloxacin . hydrochloride
SYNONYMS	(S)-(-)-9-fluoro-2,3-dihydro-3-methyl-10- (4-methyl-1-piperazinyl)-7-oxo-7H-pyrido [1,2,3-de]-1,4-benzoxazine-6-carboxylic acid . hydrochloride S-(-)-Ofloxacin . hydrochloride

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-292-G001		1 g	30.00 USD
ALX-380-292-G005		5 g	70.00 USD

Product Specification

FORMULA:	C₁₈H₂₀FN₃O₄. HCl
MW:	361.4 . 36.5
CAS NUMBER:	177325-13-2
MERCK INDEX:	14: 6771
RTECS:	UU8815550
PURITY:	≥89.5% (Assay)
APPEARANCE:	Slightly yellow crystalline powder.
SOLUBILITY:	Soluble in water (25mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	HARMFUL.

Product Description

Fluoroquinolone with broad spectrum activity against Gram-negative and Gram-positive bacteria. Active enantiomer of ofloxacin with twice its potency. Inhibits bacterial DNA-gyrase (topoisomerase).

Product Specific Literature References

Levofloxacin. A review of its antibacterial activity, pharmacokinetics and therapeutic efficacy: R. Davis & H.M: Bryson; Drugs 47, 677 (1994) Abstract
The clinical pharmacokinetics of levofloxacin: D.N. Fish & A.T. Chow; Clin. Pharmacokinet. 32, 101 (1997) Abstract
Levofloxacin: an updated review of its use in the treatment of bacterial infections: M. Hurst, et al.; Drugs 62, 2127 (2002) Abstract
Levofloxacin : a review of its use as a high-dose, short-course treatment for bacterial infection: V.R. Anderson & C.M. Perry; Drugs 68, 535 (2008) Abstract

Related Products

ALX-380-297

Ofloxacin

Further Categories Containing This Product:

Antibiotics - DNA Replication Inhibitors • Antibiotics - Topoisomerase Inhibitors

ALX-380-293

Revised 04-Aug-08

Lomefloxacin . hydrochloride
SYNONYMS	1-Ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-293-G001		1 g	20.00 USD
ALX-380-293-G005		5 g	80.00 USD

Product Specification

FORMULA:	C₁₇H₁₉F₂N₃O₃ . HCl
MW:	351.4 . 36.5
CAS NUMBER:	98079-52-8
MERCK INDEX:	14: 5562
RTECS:	VB1997500
PURITY:	≥89% (Assay)
APPEARANCE:	White to off-white crystalline powder.
SOLUBILITY:	Soluble in 1M sodium hydroxide (50mg/ml); sparingly soluble in water; insoluble in 100% ethanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
HAZARD:	HARMFUL.

Product Description

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

Product Specific Literature References

Mechanism of action of lomefloxacin: L.J. Piddock, et al.; Antimicrob. Agents Chemother. 34, 1088 (1990) Abstract; Full Text
Antibacterial activity of lomefloxacin in a pharmacokinetic in vitro model: C. Rustige & B. Wiedemann; Antimicrob. Agents Chemother. 34, 1107 (1990) Abstract; Full Text

Further Categories Containing This Product:

Antibiotics - Topoisomerase Inhibitors • Antibiotics - DNA Replication Inhibitors

ALX-400-050

Revised 07-Apr-08

Mitoxantrone . dihydrochloride
SYNONYMS	1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-9,10-anthracenedione . dihydrochloride
PRODUCT LINE	Cancer
PRODUCT CATEGORY	Antitumor Agents (DNA Interaction & Gene Regulation)

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-400-050-M010		10 mg	25.00 USD
ALX-400-050-M050		50 mg	80.00 USD

Product Specification

FORMULA:	C₂₂H₂₈N₄O₆. 2HCl
MW:	444.5 . 73.0
CAS NUMBER:	70476-82-3
MERCK INDEX:	14: 6217
RTECS:	CB5748500
SOURCE/HOST:	Synthetic.
PURITY:	≥97%
APPEARANCE:	Blue to black crystalline solid.
SOLUBILITY:	Soluble in water; slightly soluble in 100% ethanol or methanol; insoluble in acetonitrile or acetone.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	TOXIC. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description

Antiviral, antibacterial, antiprotozoal, immunomodulating, and antineoplastic cytostatic anthraquinone derivative. Induces DNA damage by intercalating into DNA and inhibiting topoisomerase II. Induces interstrand DNA cross-links and DNA-protein cross-links in cellular systems. Has recently been shown to be an inhibitor of DNA methylation.

Product Specific Literature References

Mitoxantrone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the chemotherapy of cancer: D. Faulds, et al.; Drugs 41, 400 (1991) Abstract
Mitoxantrone and ametantrone induce interstrand cross-links in DNA of tumour cells: A. Skladanowski & J. Konopa; Br. J. Cancer 82, 1300 (2000) Abstract
A comparison of the in vitro genotoxicity of anticancer drugs idarubicin and mitoxantrone: J. Blasiak, et al.; Acta Biochim. Pol. 49, 145 (2002) Abstract; Full Text
A molecular understanding of mitoxantrone-DNA adduct formation: effect of cytosine methylation and flanking sequences: B.S. Parker, et al.; J. Biol. Chem. 279, 18814 (2004) Abstract; Full Text

Further Categories Containing This Product:

Topoisomerase Inhibitors Other Products

ALX-804-624

Revised 20-Jun-05

Monoclonal Antibody to Doxorubicin (MAD11)
SYNONYMS	anti-DXR MAb (MAD11) anti-14-Hydroxydaunomycin MAb (MAD11) anti-Adriamycin MAb (MAD11)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antitumor Antibiotics

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-804-624-C100		100 µg	320.00 USD