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Antitumor Reagents
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ALX-380-110 Revised 03-Apr-08
17-DMAG
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SYNONYMS 17-[2-(Dimethylamino)ethyl]amino-17-desmethoxygeldanamycin
NSC 707545
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Angiogenesis Research
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-110-C100   100 µg 50.00 USD Add To Cart
ALX-380-110-M001   1 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C32H48N4O8
MW: 616.8
CAS NUMBER: 150270-08-9
SOURCE/HOST: Semisynthetic from geldanamycin (Prod. No. ALX-380-054).
PURITY: ≥99%
APPEARANCE: Purple to black powder.
SOLUBILITY: Soluble in water, 100% ethanol (10mg/ml) or DMSO (>25mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description

Less toxic, more potent synthetic derivative of geldanamycin. Inhibitor of angiogenesis. Inhibitor of heat shock protein 90 (HSP90). Inducer of apoptosis with higher antitumor activity than 17-AAG (Prod. No. ALX-380-091).
Product Specific Literature References
Pharmacokinetics, tissue distribution, and metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (NSC 707545) in CD2F1 mice and Fischer 344 rats: M.J. Egorin, et al.; Cancer Chemother. Pharmacol. 49, 7 (2002) Abstract
Biliary excretion of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) and metabolites by Fischer 344 rats: S.M. Musser, et al.; Cancer Chemother. Pharmacol. 52, 139 (2003) Abstract
Crystal structure and molecular modeling of 17-DMAG in complex with human Hsp90: J.M. Jez, et al.; Chem. Biol. 10, 361 (2003) Abstract
Synthesis and biological activities of novel 17-aminogeldanamycin derivatives: Z.Q. Tian, et al.; Bioorg. Med. Chem. 12, 5317 (2004) Abstract
Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator: G. Kaur, et al.; Clin. Cancer Res. 10, 4813 (2004) Abstract
Enhanced tumor cell radiosensitivity and abrogation of G2 and S phase arrest by the Hsp90 inhibitor 17-(Dimethylaminoethylamino)-17-demethoxygeldanamycin: E.E. Bull, et al.; Clin. Cancer Res. 10, 8077 (2004) Abstract
ErbB3 expression predicts tumor cell radiosensitization induced by Hsp90 inhibition: H. Dote, et al.; Cancer Res. 65, 6967 (2005) Abstract
In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative: M. Hollingshead, et al.; Cancer Chemother. Pharmacol. 56, 115 (2005) Abstract
Comparison of 17-dimethylaminoethylamino-17-demethoxy-geldanamycin (17DMAG) and 17-allylamino-17-demethoxygeldanamycin (17AAG) in vitro: effects on Hsp90 and client proteins in melanoma models: V. Smith, et al.; Cancer Chemother. Pharmacol. 56, 126 (2005) Abstract
Preclinical toxicity of a geldanamycin analog, 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG), in rats and dogs: potential clinical relevance: E.R. Glaze, et al.; Cancer Chemother. Pharmacol. 56, 637 (2005) Abstract
17-Allyamino-17-demethoxygeldanamycin and 17-NN-dimethyl ethylene diamine-geldanamycin have cytotoxic activity against multiple gynecologic cancer cell types: D.R. Gossett, et al.; Gynecol. Oncol. 96, 381 (2005) Abstract
Structure-based design of 7-carbamate analogs of geldanamycin: G. Rastelli, et al.; Biooorg. Med. Chem. Lett. 15, 5016 (2005) Abstract
Generation of a novel anti-geldanamycin antibody: E. Barzilay, et al.; BBRC 330, 561 (2005) Abstract
Determination of the heat shock protein 90 inhibitor 17-dimethylaminoethylamino-17-demethoxygeldanamycin in plasma by liquid chromatography-electrospray mass spectrometry: K. Hwang, et al.; J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. 830, 35 (2006) Abstract
Related Products
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Tyrosine Kinase Inhibitors • Antitumor Antibiotics • HSP90 / HtpG / Related Products
 
 
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
Characterization of Adriamycin-Induced G2 Arrest and Its Abrogation by Caffeine in FL-Amnion Cells with or without p53: Y. Minemoto, et al.; Exp. Cell Res. 262, 37 (2001) Abstract
Enhancement of Fas-mediated apoptosis in renal cell carcinoma cells by adriamycin: X.X. Wu, et al.; Cancer Res. 60, 2912 (2000) Abstract
Doxorubicin-induced apoptosis in endothelial cells and cardiomyocytes is ameliorated by nitrone spin traps and ebselen. Role of reactive oxygen and nitrogen species: S. Kotamraju, et al.; J. Biol. Chem. 275, 33585 (2000) Abstract; Full Text
The power and potential of doxorubicin-DNA adducts: S.M. Cutts, et al.; IUBMB Life 57, 73 (2005), Review Abstract
Adriamycin-induced interference with cardiac mitochondrial calcium homeostasis: K.B. Wallace; Cardiovasc. Toxicol. 7, 101 (2007), Review Abstract
Doxorubicin-induced cardiomyopathy from the cardiotoxic mechanisms to managemen: G. Takemura & H. Fujiwara; Prog. Cardiovasc. Dis. 49, 330 (2007), Review Abstract
Further Categories Containing This Product:
Other Toxins • Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Apoptosis Inducers) • Antibiotics - Immunomodulators • Antibiotics - Topoisomerase Inhibitors • DNA Intercalators & Crosslinkers • Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-380-273 Revised 03-Apr-08
Doxycycline . hyclate
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SYNONYMS Doxycycline . hydrochloride . hemiethanolate . hemihydrate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Angiogenesis Research
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ALX-380-273-G001   1 g 20.00 USD Add To Cart
ALX-380-273-G005   5 g 60.00 USD Add To Cart
Product Specification
FORMULA: C22H24N2O8 . HCl . 0.5C2H6O . 0.5H2O
MW: 444.4 . 36.5 . 23.0 . 9.0
CAS NUMBER: 24390-14-5
MERCK INDEX: 14: 3440
RTECS: QI8925000
SOURCE/HOST: Semisynthetic from oxytetracycline.
PURITY: ≥98% (Assay on dry basis)
APPEARANCE: Yellow crystalline solid.
SOLUBILITY: Soluble in water (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
HAZARD: HARMFUL. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description
Broad spectrum antibiotic and bacteriostatic. Shows antiprotozoal properties. Potent inhibitor of MMPs (matrix metalloproteinases) in vivo. Inhibits collagen synthesis.
Product Specific Literature References
Alpha-6-deoxyoxytetracycline. I. Some biological properties: A.R. English; Proc. Soc. Exp. Biol. Med. 122, 1107 (1966) Abstract
A compilation of LD50 values in newborn and adult animals: E.I. Goldenthal; Toxicol. Appl. Pharmacol. 18, 185 (1971) Abstract
An efficacy trial of doxycycline chemoprophylaxis against leptospirosis: E.T. Takafuji, et al.; N. Engl. J. Med. 310, 497 (1984) Abstract
Specificity of the anticollagenase action of tetracyclines: relevance to their anti-inflammatory potential: K. Suomalainen, et al.; Antimicrob. Agents Chemother. 36, 227 (1992) Abstract
Matrix metalloproteinase-8 is expressed in rheumatoid synovial fibroblasts and endothelial cells. Regulation by tumor necrosis factor-alpha and doxycycline: R. Hanemaaijer, et al.; J. Biol. Chem. 272, 31504 (1997) Abstract; Full Text
Doxycycline and tissue repair in rats: S. Lamparter, et al.; J. Lab. Clin. Med. 139, 295 (2002) Abstract
Molecular interactions between matrilysin and the matrix metalloproteinase inhibitor doxycycline investigated by deuterium exchange mass spectrometry: R.A. Garcia, et al.; Mol. Pharmacol. 67, 1128 (2005) Abstract; Full Text
Doxycycline alters vascular smooth muscle cell adhesion, migration, and reorganization of fibrillar collagen matrices: C. Franco, et al.; Am. J. Pathol. 168, 1697 (2006) Abstract; Full Text
Doxycycline inhibits MMPs via modulation of plasminogen activators in focal cerebral ischemia: D. Burggraf, et al.; Neurobiol. Dis. 25, 506 (2007) Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors) • MMP Inhibitors • Antitumor Agents (Anti-proliferative) • Antitumor Antibiotics
 
 
ALX-380-201 Revised 27-Jun-08
Echinomycin
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SYNONYMS Quinomycin A
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - DNA Replication Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-201-M001   1 mg 80.00 USD Add To Cart
ALX-380-201-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C51H64N12O12S2
MW: 1101.3
CAS NUMBER: 512-64-1
MERCK INDEX: 14: 3497
RTECS: JW5250000
SOURCE/HOST: Isolated from Streptomyces echinatus (DSM 40013).
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, dimethyl formamide or DMSO; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
HAZARD: TOXIC. MAY BE MUTAGENIC.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Antitumor antibiotic. Powerful, selective inhibitor of nucleic acid synthesis in vitro. Potent inhibitor of hypoxia-inducible factor 1 (HIF-1) DNA binding activity. Induces apoptosis. Displays antibacterial, antifungal and antiviral activities.
Product Specific Literature References
A “quinoxaline antibiotic” similar to the triostins, q.v.: I. Kuroya, et al.; J. Antibiot. 14A, 324 (1961)
Identity of levomycin and quinomycin A (echimomycin): K. Katagiri, et al.; J. Antibiot. 15, 273 (1962) Abstract
The mode of action of quinoxaline antibiotics. Interaction of quinomycin A with deoxyribonucleic acid: K. Sato, et al.; J. Antibiot. 20, 270 (1967) Abstract
The binding of echinomycin to deoxyribonucleic acid: S.P. Wakelin & M.J. Waring; Biochem. J. 157, 721 (1976) Abstract; Full Text
Bifunctional intercalation and sequence specificity in the binding of quinomycin and triostin antibiotics to deoxyribonucleic acid: J.S. Lee & M.J. Waring; Biochem. J. 173, 115 (1978) Abstract; Full Text
Kinetics of the interaction between echinomycin and deoxyribonucleic acid: K.R. Fox, et al.; Biochemistry 20, 5768 (1981) Abstract
Sequence-specific binding of echinomycin to DNA: evidence for conformational changes affecting flanking sequences: C.M. Low, et al.; Nucl. Acids Res. 12, 4865 (1984) Abstract; Full Text
Echinomycin binding sites on DNA: M.M. Van Dyke & P.B. Dervan; Science 225, 1122 (1984) Abstract
Kinetic evidence that echinomycin migrates between potential DNA binding sites: K.R. Fox & M.J. Waring; Nucl. Acids Res. 13, 595 (1985) Abstract; Full Text
Effect of echinomycin on DNA methylation: R.L. Adams & A. Rinaldi; FEBS Lett. 215, 266 (1987) Abstract
Interaction of echinomycin with An.Tn. and (AT)n regions flanking its CG binding site: K. Waterloh & K.R. Fox; Nucl. Acids Res. 19, 6719 (1991) Abstract; Full Text
Localized chemical reactivity in DNA associated with the sequence-specific bisintercalation of echinomycin: C. Bailly, et al.; Biochem. J. 300, 165 (1994) Abstract; Full Text
Energetics of echinomycin binding to DNA: F. Leng, et al.; Nucl. Acids Res. 31, 6191 (2003) Abstract; Full Text
Echinomycin inhibits chromosomal DNA replication and embryonic development in vertebrates: L.G. May, et al.; Nucl. Acids Res. 32, 65 (2004) Abstract; Full Text
Echinomycin and a novel analogue induce apoptosis of HT-29 cells via the activation of MAP kinases pathway: J.Y. Park, et al.; Pharmacol. Res. 50, 201 (2004) Abstract
Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity: D. Kong, et al.; Cancer Res. 65, 9047 (2005) Abstract; Full Text
Molecular signaling cascade in DNA bisintercalator, echinomycin-induced apoptosis of HT-29 cells: evidence of the apoptotic process via activation of the cytochrome c-ERK-caspase-3 pathway: J.Y. Park, et al.; Int. J. Biochem. Cell Biol. 38, 244 (2006) Abstract
Synergistic effects of CoCl(2) and ROCK inhibition on mesenchymal stem cell differentiation into neuron-like cells: E. Pacary, et al.; J. Cell Sci. 119, 2667 (2006) Abstract; Full Text
Metabolic targeting of hypoxia and HIF1 in solid tumors can enhance cytotoxic chemotherapy: R.A. Cairns, et al.; PNAS 104, 9445 (2007) Abstract
Further Categories Containing This Product:
Antibiotics - Antiviral / Anti-HIV • Antitumor Agents (Apoptosis Inducers) • Hypoxia-inducible Factor [HIF] / Related Products • Antibiotics - Antifungal • Antitumor Antibiotics
 
 
ALX-380-115 Revised 03-Apr-08
Echinosporin
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SYNONYMS NSC357683
XK 213
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-115-M001   1 mg 90.00 USD Add To Cart
ALX-380-115-M005   5 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C10H9NO5
MW: 223.2
CAS NUMBER: 79127-35-8
RTECS: JW5313000
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in dimethyl formamide, methanol or water.
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.
HAZARD: HARMFUL.

Product Description
Antitumor antibiotic. Inhibits cell cycle at the G(2)/M phase and induces apoptosis.
Product Specific Literature References
A new antibiotic echinosporin (XK-213) - producing organism, isolation and characterization: T. Sato, et al.; J. Antibiot. 35, 266 (1982) Abstract
Antitumor activity of echinosporin: M. Morimoto and R. Imai; J. Antibiot. 38, 490 (1985) Abstract
Approaches to the total synthesis of the antitumor antibiotic echinosporin: M. A. Kinsella; J. Org. Chem. 55, 105 (1990)
Applications of an asymmetric [2 + 2]-photocycloaddition. Total synthesis of (-)-echinosporin. Construction of an advanced 11-deoxyprostaglandin intermediate: A. B. Smith; JACS 114, 2567 (1992)
Biosynthesis of the antibiotic echinosporin by a novel branch of the shikimate pathway: A. Dubeler; Eur. J. Org. Chem. 2002, 983 (2002)
Echinosporins as new cell cycle inhibitors and apoptosis inducers from marine-derived Streptomyces albogriseolus: C.B. Cui, et al.; Fitoterapia 78, 238 (2007) Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Antibiotics for Cell Cycle Research
 
 
ALX-300-152 Revised 09-Feb-05
1-Elaidylphosphocholine (C18:1, trans)
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phospholipids / Related Products
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ALX-300-152-M250   250 mg 80.00 USD Add To Cart
ALX-300-152-G001   1 g 240.00 USD Add To Cart
Product Specification
FORMULA: C23H48NO4P
MW: 433.6
PURITY: ≥98%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
Product Description
Cytotoxic alkylphosphocholine for a variey of tumor cells and protozoal diseases (leishmaniasis).
General Literature References
Hexadecylphosphocholine: a new and selective antitumor drug: H. Eibl & C. Unger; Cancer Treat. Rev. 17, 233 (1990), (Review) Abstract
Induction of tumor cell differentiation by alkylphosphocholines: a new approach for in vitro screening: H.R. Maurer & P. Hilgard; Prog. Exp. Tumor Res. 34, 90 (1992), (Review) Abstract
Alkylphosphocholines: a new class of membrane-active anticancer agents: P. Hilgard, et al.; Cancer Chemother. Pharmacol. 32, 90 (1993), (Review) Abstract
Current concepts of treatment in medical oncology: new anticancer drugs: C. Unger; J. Cancer Res. Clin. Oncol. 122, 189 (1996), (Review) Abstract
Further Categories Containing This Product:
Antitumor Reagents Other Products
 
 
ALX-380-212 Revised 10-Dec-07
Elaiophylin
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SYNONYMS Antibiotic 255-E
Antibiotic 5001B
Antibiotic 56-62
Antibiotic 846 I
SNA 4606-3
Azalomycin B
Gopalamicin
Salbomycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-212-M001   1 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C54H88O18
MW: 1025.3
CAS NUMBER: 37318-06-2
RTECS: CL8380000
SOURCE/HOST: Isolated from Streptomyces hygroscopicus MST-AS5386.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Macrolide antibiotic inhibiting testosterone 5-reductase and plasma-proton ATPase (P-ATPase). Shows antifungal, antiprotozoal, antitumor, antihelmintic and immunosuppressive activity.
Product Specific Literature References
Melanosporin and elaiophylin, new antibiotics from Streptomyces malanosporus (sive melanosporofaciens) n. sp.: F.M. Arcamone, et al.; G. Microbiol. 7, 207 (1959)
Metabolic products of microorganisms. 200 Isolation and characterization of niphithricins A, B, and elaiophylin, antibiotics produced by Streptomyces violaceoniger: H.P. Fiedler, et al.; J. Antibiot. (Tokyo) 34, 1107 (1981) Abstract
Elaiophylin as a rumen fermentation efficiency enhancer: C.M. Liu, et al.; J. Antibiot. (Tokyo) 46, 350 (1993) Abstract
SNA-4606-1, a new member of elaiophylins with enzyme inhibition activity against testosterone 5 alpha-reductase: M. Nakakoshi, et al.; J. Antibiot. (Tokyo) 52, 175 (1999) Abstract
Enhancement of the antifungal activity of rapamycin by the coproduced elaiophylin and nigericin: A. Fang, et al.; J. Antibiot. (Tokyo) 53, 158 (2000) Abstract
Cation selective ion channels formed by macrodiolide antibiotic elaiophylin in lipid bilayer membranes: P.A. Grigoriev, et al.; Bioelectrochemistry 54, 11 (2001) Abstract
Further Categories Containing This Product:
Antibiotics - Immunomodulators • Helminth Infections / Related Products • Antitumor Antibiotics • Antibiotics - ATPase Inhibitors
 
 
ALX-270-262 Revised 13-Feb-08
Ellagic acid . dihydrate
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SYNONYMS 4,4',5,5',6,6'-Hexahydroxydiphenic acid 2,6,2',6'-dilactone . 2H2O
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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ALX-270-262-M100   100 mg 12.00 USD Add To Cart
Product Specification
FORMULA: C14H6O8 . 2H2O
MW: 302.2 . 36.0
CAS NUMBER: 476-66-4
MERCK INDEX: 14: 3547
RTECS: DJ2620000
SOURCE/HOST: Isolated from chestnut bark.
PURITY: ≥97%
APPEARANCE: Grey to green solid.
SOLUBILITY: Soluble in 1M sodium hydroxide (10mg/ml) or pyridine.
SHIPPING: AMBIENT