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Antibiotics - Topoisomerase Inhibitors
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ALX-380-119 Revised 21-May-08
Becatecarin
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SYNONYMS 6-N-[2-(Diethylamino)ethyl]rebeccamycin
NSC 655649
BMY-27557-14
BMS-181176
XL 119
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-119-C250   250 µg 155.00 USD Add To Cart
ALX-380-119-M001   1 mg 465.00 USD Add To Cart
Product Specification
FORMULA: C33H34Cl2N4O7
MW: 669.6
CAS NUMBER: 119673-08-4
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in water (pH-dependent) or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Semisynthetic water-soluble derivative of rebeccamycin (ALX-380-079). Antitumor antibiotic. Topoisomerase II inhibitor. DNA intercalating agent.
Product Specific Literature References
Water soluble derivatives of rebeccamycin: T. Kaneko, et al.; J. Antibiot. 43, 125 (1990) Abstract
Discovery of antitumor indolocarbazoles: rebeccamycin, NSC 655649, and fluoroindolocarbazoles: B.H. Long, et al.; Curr. Med. Chem. Anticancer Agents 2, 255 (2002) Abstract
Becatecarin (Helsinn Healthcare): G.W. Rewcastle; IDrugs 8, 838 (2005) Abstract
Phase I and pharmacokinetic study of sequences of the rebeccamycin analogue NSC 655649 and cisplatin in patients with advanced solid tumors: A.D. Ricart, et al.; Clin. Cancer Res. 11, 8728 (2005) Abstract; Full Text
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Further Categories Containing This Product:
Antitumor Agents (DNA Interaction & Gene Regulation) • DNA Intercalators & Crosslinkers • Antibiotics - Topoisomerase Inhibitors
 
 
ALX-380-073 Revised 12-Oct-07
Chartreusin
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SYNONYMS Lambdamycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-073-M005   5 mg 50.00 USD Add To Cart
ALX-380-073-M025   25 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C32H32O14
MW: 640.6
CAS NUMBER: 6377-18-0
MERCK INDEX: 14: 2045
SOURCE/HOST: Isolated from Streptomyces chartreusis.
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in acetone; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: TOXIC.
Product Description
Antitumor antibiotic which inhibits topoisomerase II. Induces single-strand scission in DNA in the presence of reducing agents.
Product Specific Literature References
Chartreusin, a New Antibiotic Produced by Streptomyces chartreusis, a New Species: B. E. Leach, et al.; J. Am. Chem. Soc. 75, 4011 (1953)
Chartreusin, a glycosidic antitumour antibiotic from Streptomyces: J.A. Beisler; Prog. Med. Chem. 19, 247 (1982), (Review) Abstract
Biochemical characterisation of elsamicin and other coumarin-related antitumour agents as potent inhibitors of human topoisomerase II: A. Lorico & B.H. Long; Eur. J. Cancer 14, 1985 (1993) Abstract
Chartreusin, elsamicin A and related anti-cancer antibiotics: J. Portugal; Curr. Med. Chem. Anticancer Agents 3, 411 (2003), Review Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (DNA Interaction & Gene Regulation) • Antibiotics - Topoisomerase Inhibitors
 
 
ALX-380-112 Revised 03-Apr-08
Chrysomycin A
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SYNONYMS Chrysomycin V
Virenomycin V
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Topoisomerase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-112-C250   250 µg 140.00 USD Add To Cart
ALX-380-112-M001   1 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C28H28O9
MW: 508.5
CAS NUMBER: 82196-88-1
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow to greenish solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; slightly soluble in 100% ethanol or methanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for at least 3 months when stored at -20°C.
HANDLING: Protect from light also when in solution.

Product Description
Antibiotic. Inhibits topoisomerase II in human. Mediates a unique cross-linking reaction between DNA and histidine H3. Antineoplastic and photosensitizing compound. Exhibits antitumor activity against human cell lines.
Product Specific Literature References
Chrysomycin: a new antibiotic substance for bacterial viruses: F. Strelitz, et al.; J. Bacteriol. 69, 280 (1955) Abstract
The chemistry of the antibiotics chrysomycin A and B. Antitumor activity of chrysomycin A: U. Weiss, et al.; J. Antibiot. (Tokyo) 35, 1194 (1982) Abstract
Biochemical characterisation of elsamicin and other coumarin-related antitumour agents as potent inhibitors of human topoisomerase II: A. Lorico and B.H. Long; Eur. J. Cancer 29A, 1985 (1993) Abstract
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Further Categories Containing This Product:
Antitumor Antibiotics • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-380-114 Revised 03-Apr-08
Chrysomycin B
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SYNONYMS Chrysomycin M
Virenomycin M
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Topoisomerase Inhibitors
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ALX-380-114-C250   250 µg 140.00 USD Add To Cart
ALX-380-114-M001   1 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C27H28O9
MW: 496.5
CAS NUMBER: 83852-56-6
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; slightly soluble in 100% ethanol or methanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for at least 3 months when stored at -20°C.
HANDLING: Protect from light.

Product Description
Antibiotic. Inhibits topoisomerase II in human. Mediates a unique cross-linking reaction between DNA and histidine H3. Antineoplastic and photosensitizing compound. Exhibits antitumor activity against human cell lines. Less potent than Chrysomycin A (Prod. No. ALX-380-112).
Product Specific Literature References
Chrysomycin: a new antibiotic substance for bacterial viruses: F. Strelitz, et al.; J. Bacteriol. 69, 280 (1955) Abstract
The chemistry of the antibiotics chrysomycin A and B. Antitumor activity of chrysomycin A: U. Weiss, et al.; J. Antibiot. (Tokyo) 35, 1194 (1982) Abstract
Biochemical characterisation of elsamicin and other coumarin-related antitumour agents as potent inhibitors of human topoisomerase II: A. Lorico and B.H. Long; Eur. J. Cancer 29A, 1985 (1993) Abstract
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Further Categories Containing This Product:
Antitumor Agents (DNA Interaction & Gene Regulation) • Antitumor Antibiotics
 
 
ALX-380-287 Revised 15-Apr-08
Ciprofloxacin
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SYNONYMS 1-Cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1- piperazinyl)-3-quinolinecarboxylic acid
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ALX-380-287-G005   5 g 20.00 USD Add To Cart
ALX-380-287-G025   25 g 60.00 USD Add To Cart
Product Specification
FORMULA: C17H18FN3O3
MW: 331.3
CAS NUMBER: 85721-33-1
MERCK INDEX: 14: 2314
RTECS: VB1993800
PURITY: ≥98% (Assay)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in dilute hydrochloric acid; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Fluoroquinolone antibacterial agent. Inhibits bacterial DNA gyrase (topoisomerase). Inhibits cell division and causes double-strand breaks in the bacterial chromosome. Broad-spectrum antibiotic effective against Gram-positive, Gram-negative and anaerobic bacteria. Effective against Mycobacterium tuberculosis. Potentially anxiogenic.
Product Specific Literature References
Is ciprofloxacin active against clinically important anaerobes?: B. Watt & F.V. Brown; J. Antimicrob. Chemother. 17, 605 (1986) Abstract
Ciprofloxacin and norfloxacin, two fluoroquinolone antimicrobials: D.E. Nix & J.M DeVito; Clin. Pharm. 6, 105 (1987) Abstract
Mechanisms of action of and resistance to ciprofloxacin: D.C. Hooper, et al.; Am. J. Med. 82, 12 (1987) Abstract
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy: R.K. Shandil, et al.; Antimicrob. Agents Chemother. 51, 576 (2007) Abstract; Full Text
Anxiogenic potential of ciprofloxacin and norfloxacin in rats: S. Sen, et al.; Singapore Med. J. 48, 1028 (2007) Abstract; Full Text
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Further Categories Containing This Product:
Antibiotics - DNA Replication Inhibitors • Antibiotics - Topoisomerase Inhibitors
 
 
ALX-380-288 Revised 08-Aug-08
Ciprofloxacin . hydrochloride
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SYNONYMS 1-Cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid . hydrochloride
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ALX-380-288-G005   5 g 20.00 USD Add To Cart
ALX-380-288-G025   25 g 55.00 USD Add To Cart
Product Specification
FORMULA: C17H18FN3O3 . HCl . H2O
MW: 331.3 . 36.5 . 18.0
CAS NUMBER: 86393-32-0
MERCK INDEX: 14: 2314
PURITY: ≥88.5% (Assay)
APPEARANCE: White to light yellow powder.
SOLUBILITY: Soluble in water (35mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Fluoroquinolone antibacterial agent. Inhibits bacterial DNA gyrase (topoisomerase). Inhibits cell division and causes double-strand breaks in the bacterial chromosome. Broad-spectrum antibiotic effective against Gram-positive, Gram-negative and anaerobic bacteria. Effective against Mycobacterium tuberculosis. Potentially anxiogenic.
Product Specific Literature References
Is ciprofloxacin active against clinically important anaerobes?: B. Watt & F.V. Brown; J. Antimicrob. Chemother. 17, 605 (1986) Abstract
Ciprofloxacin and norfloxacin, two fluoroquinolone antimicrobials: D.E. Nix & J.M. DeVito; Clin. Pharm. 6, 105 (1987) Abstract
Mechanisms of action of and resistance to ciprofloxacin: D.C. Hooper, et al.; Am. J. Med. 82, 12 (1987) Abstract
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy: R.K. Shandil, et al.; Antimicrob. Agents Chemother. 51, 576 (2007) Abstract; Full Text
Anxiogenic potential of ciprofloxacin and norfloxacin in rats: S. Sen, et al.; Singapore Med. J. 48, 1028 (2007) Abstract; Full Text
Related Products
Further Categories Containing This Product:
Antibiotics - DNA Replication Inhibitors • Antibiotics - Topoisomerase Inhibitors
 
 
ALX-380-289 Revised 05-Aug-08
Clinafloxacin
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SYNONYMS 7-(3-Amino-1-pyrrolidinyl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
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ALX-380-289-M250   250 mg 55.00 USD Add To Cart
ALX-380-289-G001   1 g 160.00 USD Add To Cart
Product Specification
FORMULA: C17H17ClFN3O3
MW: 365.8
CAS NUMBER: 105956-97-6
MERCK INDEX: 14: 2355
PURITY: ≥95% (Assay)
APPEARANCE: White to light yellow crystalline powder.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by NMR.

Product Description
Fluoroquinolone with broad-spectrum activity against Gram-negative and Gram-positive bacteria, aerobes and anaerobes. Inhibits bacterial DNA topoisomerase IV and DNA gyrase.
Product Specific Literature References
DNA gyrase and topoisomerase IV are dual targets of clinafloxacin action in Streptococcus pneumoniae: X.S. Pan & L.M. Fisher; Antimicrob. Agents Chemother. 42, 2810 (1998) Abstract; Full Text
Streptococcus pneumoniae DNA gyrase and topoisomerase IV: overexpression, purification, and differential inhibition by fluoroquinolones: X.S. Pan and L.M. Fisher; Antimicrob. Agents Chemother. 43, 1129 (1999) Abstract; Full Text
Fluoroquinolones inhibit preferentially Streptococcus pneumoniae DNA topoisomerase IV than DNA gyrase native proteins: E. Fernandez-Moreira, et al.; Microb. Drug Resist. 6, 259 (2000) Abstract
Activities of clinafloxacin, gatifloxacin, gemifloxacin, and trovafloxacin against recent clinical isolates of levofloxacin-resistant Streptococcus pneumoniae: J.H. Jorgensen, et al.; Antimicrob. Agents Chemother. 44, 2962 (2000) Abstract; Full Text
Further Categories Containing This Product:
Antibiotics - DNA Replication Inhibitors • Antibiotics - Topoisomerase Inhibitors
 
 
ALX-380-043 Revised 03-Apr-08
Daunorubicin . hydrochloride
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SYNONYMS Daunomycin . HCl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-043-M010   10 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C27H29NO10 . HCl
MW: 527.5 . 36.5
CAS NUMBER: 23541-50-6
MERCK INDEX: 14: 2832
SOURCE/HOST: Isolated from Streptomyces spec.
PURITY: ≥98% (HPLC)
APPEARANCE: Orange to red solid.
SOLUBILITY: Soluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description

Anthracycline anticancer antibiotic. Induces DNA damage by intercalating into DNA and inhibiting topoisomerase I and II. Inhibits RNA and DNA synthesis. Induces DNA single strand breaks and apoptosis in tumor cells.
Product Specific Literature References
Ceramide synthase mediates daunorubicin-induced apoptosis: an alternative mechanism for generating death signals: R. Bose, et al.; Cell 82, 405 (1995) Abstract
Daunorubicin activates NFkappaB and induces kappaB-dependent gene expression in HL-60 promyelocytic and Jurkat T lymphoma cells: M.P. Boland, et al.; J. Biol. Chem. 272, 12952 (1997) Abstract; Full Text
Alteration of the daunorubicin-triggered sphingomyelin-ceramide pathway and apoptosis in MDR cells: influence of drug transport abnormalities: M.G. Come, et al.; Int. J. Cancer 81, 580 (1999) Abstract
A critical evaluation of the mechanisms of action proposed for the antitumor effects of the anthracycline antibiotics adriamycin and daunorubicin: D.A. Gewirtz; Biochem. Pharmacol. 57, 727 (1999) Abstract
Altered multidrug resistance phenotype caused by anthracycline analogues and cytosine arabinoside in myeloid leukemia: X.F. Hu, et al.; Blood 93, 4086 (1999) Abstract
Implication of radical oxygen species in ceramide generation, c-Jun N- terminal kinase activation and apoptosis induced by daunorubicin: V. Mansat-de Mas, et al.; Mol. Pharmacol. 56, 867 (1999) Abstract
The phosphoinositide 3-kinase/Akt pathway is activated by daunorubicin in human acute myeloid leukemia cell lines: I. Plo, et al.; FEBS Lett 452, 150 (1999) Abstract
Caspase-3-like activity is necessary but not sufficient for daunorubicin-induced apoptosis in Jurkat human lymphoblastic leukemia cells: K.J. Turnbull, et al.; Leukemia 13, 1056 (1999) Abstract
Regulation of phospholipase D activity and ceramide production in daunorubicin-induced apoptosis in A-431 cells: J. Chen, et al.; Biochim. Biophys. Acta. 1488, 219 (2000) Abstract
Signaling pathways activated by daunorubicin:: G. Laurent & J. P. Jaffrezou; Blood 98, 913 (2001), Review Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors) • Antibiotics - Immunomodulators • Antitumor Agents (Apoptosis Inducers) • Antibiotics - Topoisomerase Inhibitors • Antibiotics - Apoptosis Inducers & Inhibitors • DNA Intercalators & Crosslinkers • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-380-042 Revised 05-May-08
Doxorubicin . hydrochloride
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SYNONYMS DXR . HCl
14-Hydroxydaunomycin . HCl
Adriamycin . HCl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-042-M005   5 mg 60.00 USD Add To Cart
ALX-380-042-M010   10 mg 110.00 USD Add To Cart
ALX-380-042-M025   25 mg 250.00 USD Add To Cart
Product Specification
FORMULA: C27H29NO11 . HCl
MW: 543.5 . 36.5
CAS NUMBER: 25316-40-9
MERCK INDEX: 14: 3439
RTECS: QI9295900
SOURCE/HOST: Isolated from Streptomyces peucetius var. caesius.
PURITY: ≥98%
APPEARANCE: Red solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: MAY BE CARCINOGENIC. MAY BE TERATOGENIC. TOXIC. MAY BE MUTAGENIC.

Product Description
Antitumor antibiotic. Induces DNA damage by intercalating into DNA and inhibiting topoisomerase II. Binds covalently to DNA. Inhbibits reverse transcriptase, RNA polymerase and the catalytic activity of Dnmt1. Immunosuppressive. Antineoplastic. Induces apoptosis.
Product Specific Literature References
Adriamycin and daunomycin induce programmed cell death (apoptosis) in tumour cells: A. Skladanowski & J. Konopa; Biochem. Pharmacol. 46, 375 (1993) Abstract
A critical evaluation of the mechanisms of action proposed for the antitumor effects of the anthracycline antibiotics adriamycin and daunorubicin: D.A. Gewirtz; Biochem. Pharmacol. 57, 727 (1999) Abstract
Doxorubicin treatment activates a Z-VAD-sensitive caspase, which causes deltapsim loss, caspase-9 activity, and apoptosis in Jurkat cells: S. Gamen, et al.; Exp. Cell Res. 258, 223 (2000) Abstract
Involvement of cyclin-dependent kinases in doxorubicin-induced apoptosis in human tumor cells: Y. Lu, et al.; Mol. Carcinog. 29, 1 (2000) Abstract
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