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Antitumor Agents (DNA Interaction & Gene Regulation)
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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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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
Related Products
 
 
ALX-630-107 Revised 21-Feb-08
Bleomycin . sulfate
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SYNONYMS Blenoxane
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-630-107-M010   10 mg 155.00 USD Add To Cart
ALX-630-107-M050   50 mg 595.00 USD Add To Cart
Product Specification
FORMULA: C55H82N17O21S3 . H2SO4
MW: 1413.6 . 98.1
CAS NUMBER: 9041-93-4
MERCK INDEX: 14: 1318
RTECS: EC5991990
SOURCE/HOST: A group of related glycopeptide antibiotics isolated from Streptomyces verticillus.
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (20mg/ml) or methanol.
ACTIVITY: 1'500-2'000 IU/mg
(corresponds to 1.5-2.0 bleomycin units (USP)/mg)
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Solutions in normal saline (~2mg/ml) are stable for 3 months when stored at +4°C in a glass container or stable for 1 month when stored at +4°C in a PVC container. Solutions in water are stable for several days only.
HAZARD: MAY BE CARCINOGENIC. TOXIC.

Product Description

Radiomimetic DNA-cleaving agent that produces double and single DNA strand breaks through an oxygen-radical-dependent mechanism. Inhibits intracellular DNA replication. DNA alkylating agent. Antineoplastic.

Product Specific Literature References
Bleomycin and other antitumor antibiotics of high molecular weight: H. Umezawa; Antimicrobial Agents Chemother. (Bethesda) 5, 1079 (1965) Abstract
Specificity of deoxyribonucleic acid cleavage by bleomycin, phleomycin, and tallysomycin: J. Kross, et al.; Biochemistry 21, 4310 (1982) Abstract
Chromatin structure during bleomycin-induced DNA damage and repair
:
B.P. Cuiffo, et al.; J. Free Radic. Biol. Med. 1, 139 (1985) Abstract
Cleavage of tRNA by Fe(II)-bleomycin: A. Huttenhofer, et al.; J. Biol. Chem. 267, 24471 (1992) Abstract
Antiangiogenic chemotherapeutic agents: characterization in comparison to their tumor growth inhibition in human renal cell carcinoma models: M. Schirner, et al.; Clin. Cancer Res. 4, 1331 (1998) Abstract
Sequence-specific changes in the metal site of ferric bleomycin induced by the binding of DNA: J.W. Sam, et al.; J. Biol. Chem. 273, 16090 (1998) Abstract
Changes in c-Jun but not Bcl-2 family proteins in p53-dependent apoptosis of mouse cerebellar granule neurons induced by DNA damaging agent bleomycin: T. Araki, et al.; Brain Res. 794, 239 (1998) Abstract
Induction of apoptosis by bleomycin in resting and cycling human lymphocytes: P. Vernole, et al.; Mutagenesis 13, 209 (1998) Abstract
Synergistic Effects of Laserthermia and Bleomycin-sulfate on Micronuclei Formation in Cytokinesis-blocked HeLa Cells: A.Sh. Monfared & H. Mozdarani; Irn. J. Med. Sci. 24, 87 (1999)
Bleomycin: new perspectives on the mechanism of action: S.M. Hecht; J. Nat. Prod. 63, 158 (2000), (Review) Abstract
Bleomycin-induced alterations in DNA replication: relationship to DNA damage: J. Dziegielewski, et al.; Biochemistry 40, 704 (2001) Abstract
 
 
ALX-400-048 Revised 06-Dec-07
Busulfan
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SYNONYMS 1,4-Butanediol dimethanesulfonate
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (DNA Interaction & Gene Regulation)
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ALX-400-048-G010   10 g 20.00 USD Add To Cart
Product Specification
FORMULA: C6H14O6S2
MW: 246.3
CAS NUMBER: 55-98-1
MERCK INDEX: 14: 1505
RTECS: EK1750000
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White to off-white crystalline powder.
SOLUBILITY: Soluble in acetone, 100% ethanol or DMSO; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: MAY BE CARCINOGENIC. VERY TOXIC. MAY BE TERATOGENIC.

Product Description
Antineoplastic bifunctional, DNA alkylating agent that causes DNA damage by cross-linking DNA and proteins. Causes double-base lesions mainly at 5’-GA-3’ and, to a lesser extent, at 5’-GG-3’ sequences. Forms an intrastrand cross-link at the 5’-GA-3’ sequence, in addition to monoalkylation. Selectively induces normal human fibroblast senescence through Erk and p38 pathways.
Product Specific Literature References
DNA intrastrand cross-link at the 5’-GA-3’ sequence formed by busulfan and its role in the cytotoxic effect: T. Iwamoto, et al.; Cancer Sci. 95, 454 (2004) Abstract
Kinetic of genotoxic expression in the pharmacodynamics of busulfan: P. Morales-Ramirez, et al.; Arch. Med. Res. 37, 316 (2006) Abstract
Busulfan-induced senescence is dependent on ROS production upstream of the MAPK pathway: V. Probin, et al.; Free Radic. Biol. Med. 42, 1858 (2007) Abstract
 
 
ALX-270-286 Revised 18-Sep-07
C75
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SYNONYMS trans-4-Carboxy-5-octyl-3-methylene-butyrolactone
PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Fatty Acid Synthase [FAS] / Related Products
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ALX-270-286-M001   1 mg 65.00 USD Add To Cart
ALX-270-286-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C14H22O4
MW: 254.3
CAS NUMBER: 191282-48-1
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in dichloromethane, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
Inhibitor of fatty acid synthase (FAS) reducing food intake and body weight in mice. Exhibits irreversible slow-binding biphasic inactivation of fatty acid synthase. Downregulates neuropeptide Y and Agouti-related protein expression. Has been proposed to activate CPT-1 activity in liver and adipose tissue, leading to increased fatty acid oxidation and energy production. Shows significant in vivo antitumor activity in human breast cancer cells. Suppresses DNA replication and induces apoptosis. FAS inhibition by C75 leads to a dramatic accumulation of the CDK inhibitor p27KIP1 from cytosol to cell nuclei.
Product Specific Literature References
Pharmacological inhibitors of mammalian fatty acid synthase suppress DNA replication and induce apoptosis in tumor cell lines: E.S. Pizer, et al.; Cancer Res. 58, 4611 (1998) Abstract
Synthesis and antitumor activity of an inhibitor of fatty acid synthase: F.P. Kuhajda, et al.; PNAS 97, 3450 (2000) Abstract
Reduced food intake and body weight in mice treated with fatty acid synthase inhibitors: T.M. Loftus, et al.; Science 288, 2379 (2000) Abstract
Malonyl-coenzyme-A is a potential mediator of cytotoxicity induced by fatty-acid synthase inhibition in human breast cancer cells and xenografts: E.S. Pizer, et al.; Cancer Res. 60, 213 (2000) Abstract
Increased fatty acid synthase is a therapeutic target in mesothelioma: E.W. Gabrielson, et al.; Clin. Cancer Res. 7, 153 (2001) Abstract
Pharmacological inhibition of fatty acid synthase activity produces both cytostatic and cytotoxic effects modulated by p53: J.N. Li, et al.; Cancer Res. 61, 1493 (2001) Abstract
Green tea epigallocatechin gallate: a natural inhibitor of fatty-acid synthase: X. Wang & W. Tian; BBRC 288, 1200 (2001) Abstract
Comparison of central and peripheral administration of c75 on food intake, body weight, and conditioned taste aversion: D.J. Clegg, et al.; Diabetes 51, 3196 (2002) Abstract
Expression of FAS within hypothalamic neurons: a model for decreased food intake after C75 treatment: E.K. Kim, et al.; Am. J. Physiol. Endocrinol. Metab. 283, E867 (2002) Abstract
Differential effects of a centrally acting fatty acid synthase inhibitor in lean and obese mice: M.V. Kumar, et al.; PNAS 99, 1921 (2002) Abstract; Full Text
Effect of a fatty acid synthase inhibitor on food intake and expression of hypothalamic neuropeptides: T. Shimokawa, et al.; PNAS 99, 66 (2002) Abstract
C75 increases peripheral energy utilization and fatty acid oxidation in diet-induced obesity: J.N. Thupari, et al.; PNAS 99, 9498 (2002) Abstract
Effect of the anorectic fatty acid synthase inhibitor C75 on neuronal activity in the hypothalamus and brainstem: S. Gao and M.D. Lane; PNAS 100, 10 (2003) Abstract
Hypothalamic malonyl-CoA as a mediator of feeding behavior: Z. Hu, et al.; PNAS 100, 12624 (2003) Abstract
C75 inhibits food intake by increasing CNS glucose metabolism: M.D. Wortman, et al.; Nat. Med. 9, 483 (2003) Abstract
Fatty Acid Synthase Inhibition Triggers Apoptosis during S Phase in Human Cancer Cells: W. Zhou, et al.; Cancer Res. 63, 7330 (2003) Abstract
Long-term effects of a fatty acid synthase inhibitor on obese mice: food intake, hypothalamic neuropeptides, and UCP3: S.H. Cha, et al.; BBRC 317, 301 (2004) Abstract
C75, a fatty acid synthase inhibitor, modulates AMP-activated protein kinase to alter neuronal energy metabolism: L.E. Landree, et al.; J. Biol. Chem. 279, 3817 (2004) Abstract
Inhibition of tumor-associated fatty acid synthase activity antagonizes estradiol- and tamoxifen-induced agonist transactivation of estrogen receptor (ER) in human endometrial adenocarcinoma cells: J.A. Menendez, et al.; Oncogene 23, 4945 (2004) Abstract
C75 activates malonyl-CoA sensitive and insensitive components of the CPT system: C. Nicot, et al.; BBRC 325, 660 (2004) Abstract
The anorexigenic fatty acid synthase inhibitor, C75, is a non-specific neuronal activator: K.A. Takahashi, et al.; Endocrinology 145, 184 (2004) Abstract
 
 
ALX-400-037 Revised 10-Apr-08
Carmustine
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SYNONYMS 1,3-bis[2-Chloroethyl]-1-nitrosourea
BCNU
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (DNA Interaction & Gene Regulation)
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ALX-400-037-M025   25 mg 52.00 USD Add To Cart
Product Specification
FORMULA: C5H9CI2N3O2
MW: 214.1
CAS NUMBER: 154-93-8
MERCK INDEX: 14: 1845
PURITY: ≥96% (Assay)
APPEARANCE: Off-white to yellow crystalline solid.
SOLUBILITY: Soluble in water (4mg/ml) or 50% ethanol (150mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HAZARD: IRRITANT. MAY BE CARCINOGENIC.

Product Description
DNA alkylating agent causing DNA interstrand cross-linking. Inhibitor of glutathione reductase, lipoamide dehydrogenase and trypanothione reductase.
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Further Categories Containing This Product:
DNA Repair Other Products
 
 
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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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
 
 
ALX-400-049 Revised 14-Nov-07
Chlorambucil
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SYNONYMS 4-[Bis(2-chloroethyl)amino]benzenebutanoic acid
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (DNA Interaction & Gene Regulation)
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ALX-400-049-M250   250 mg 25.00 USD Add To Cart
ALX-400-049-G001   1 g 45.00 USD Add To Cart
ALX-400-049-G005   5 g 180.00 USD Add To Cart
Product Specification
FORMULA: C14H19Cl2NO2
MW: 304.2
CAS NUMBER: 305-03-3
MERCK INDEX: 14: 2073
RTECS: ES7525000
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in ether or ethanol:chloroform:acetone (3:5:4) (warm); practically insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
A nitrogen mustard bifunctional alkylating agent. Shows antineoplastic and immunosuppressant effect. Induces apoptosis in chronic lymphocytic leukemia cells.
Product Specific Literature References
DNA damage and mutagenesis induced by nitrogen mustards: L.F. Povirk & D.E. Shuker; Mutat. Res. 318, 205 (1994) Abstract
Reduced DNA double strand breaks in chlorambucil resistant cells are related to high DNA-PKcs activity and low oxidative stress: I. Boldogh, et al.; Toxicology 193, 137 (2003) Abstract
Chlorambucil cytotoxicity in malignant B lymphocytes is synergistically increased by 2-(morpholin-4-yl)-benzo[h]chomen-4-one (NU7026)-mediated inhibition of DNA double-strand break repair via inhibition of DNA-dependent protein kinase: L. Amrein, et al.; J. Pharmacol. Exp. Ther. 321, 848 (2007) Abstract
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
 
 
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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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
Related Products
Further Categories Containing This Product:
Antitumor AntibioticsAntitumor 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/H