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Antitumor Antibiotics
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ALX-380-084 Revised 30-Oct-07
Actinomycin X0δ
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-084-C200   200 µg 70.00 USD Add To Cart
Product Specification
FORMULA: C62H86N12O17
MW: 1271.5
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (contains traces of ethyl acetate or cyclohexane)
APPEARANCE: Red crystals.
SOLUBILITY: Soluble in methanol, acetone or chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep cool and dry.
HAZARD: TOXIC.
IDENTITY: Determined by 1H-NMR: Identical to standard reference.

Product Description
Antitumor antibiotic.
Product Specific Literature References
Identification of actinomycins by high performance liquid chromatography and fast atom bombardment mass spectrometry: S. Cho, et al.; Arch. Pharm. Res. 17, 424 (1994) Abstract
Further Categories Containing This Product:
Transcription Inhibitors / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors
 
 
ALX-380-085 Revised 30-Oct-07
Actinomycin Z1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-085-C200   200 µg 70.00 USD Add To Cart
Product Specification
FORMULA: C62H84N12O19
MW: 1301.5
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥95% (contains traces of ethyl acetate or cyclohexane)
SOLUBILITY: Soluble in methanol, acetone or chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep cool and dry.
HAZARD: TOXIC.
IDENTITY: Determined by 1H-NMR: Identical to standard reference.

Product Description
Antitumor antibiotic.
Product Specific Literature References
Identification of actinomycins by high performance liquid chromatography and fast atom bombardment mass spectrometry: S. Cho, et al.; Arch. Pharm. Res. 17, 424 (1994) Abstract
Further Categories Containing This Product:
Transcription Inhibitors / Related Products
 
 
ALX-380-088 Revised 30-Jul-08
Netropsin . dihydrochloride
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SYNONYMS 4-([((Aminoiminomethyl)amino)acetyl)amino)-N-(5-(((3-amino-3-iminopropyl)amino)carbonyl]-1-methyl-1H-pyrrol-3-yl)-1-methyl-1H-pyrrole-3-carboxamide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-088-M005   5 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C18H26N10O3 . 2HCl
MW: 430.5 . 73.0
CAS NUMBER: 63770-20-7 (hydrochloride)
RTECS: DW2973000
SOURCE/HOST: Isolated from Streptomyces netropsis.
PURITY: ≥93% (HPLC)
APPEARANCE: Faint yellow powder.
SOLUBILITY: Soluble in alcohols or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
Nucleic acid binding ligand. Binds to A-T-rich regions of the minor groove of DNA.
Product Specific Literature References
Netropsin, a New Antibiotic Produced by a Streptomyces: A.C. Finlay et al.; J. Am. Chem. Soc. 73, 341 (1951)
Efficient Total Syntheses of the Oligopeptide Antibiotics Netropsin and Distamycin: J.W. Lown et al.; J. Org. Chem. 50, 3774 (1985)
Sequence and structural selectivity of nucleic acid binding ligands: J. Ren & J.B. Chaires; Biochemistry 38, 16067 (1999) Abstract
Molecular modelling of the interaction of carbocyclic analogues of netropsin and distamycin with d(CGCGAATTCGCG)2: K. Bielawski, et al.; Acta Biochim. Pol. 47, 855 (2000) Abstract
Recent developments in sequence selective minor groove DNA effectors: B.S. Reddy, et al.; Curr. Med. Chem. 8, 475 (2001), (Review) Abstract
Further Categories Containing This Product:
Other Antibiotics - DNA Regulation / Transcription • Antibiotics - Antiviral / Anti-HIV
 
 
ALX-380-091 Revised 21-Aug-08
17-AAG
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SYNONYMS 17-(Allylamino)-17-desmethoxygeldanamycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-091-C100   100 µg 65.00 USD Add To Cart
ALX-380-091-M001   1 mg 162.00 USD Add To Cart
Product Specification
FORMULA: C31H43N3O8
MW: 585.7
CAS NUMBER: 75747-14-7
SOURCE/HOST: Semisynthetic derivative from geldanamycin.
PURITY: ≥97%
APPEARANCE: Red to dark red powder.
SOLUBILITY: Soluble in DMSO (10mg/ml) or methanol (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Potent, less toxic derivative of geldanamycin (Prod. No. ALX-380-054). Inhibits the essential ATPase activity of HSP90. Inhibitor of telomerase activity. Inducer of apoptosis with antitumor activity.
Product Specific Literature References
Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives: R.C. Schnur, et al.; J. Med. Chem. 38, 3806 (1995) Abstract
The benzoquinone ansamycin 17-allylamino-17-demethoxygeldanamycin binds to HSP90 and shares important biologic activities with geldanamycin: T.W. Schulte & L.M. Neckers; Cancer Chemother. Pharmacol. 42, 273 (1998) Abstract
Gene expression profiling of human colon cancer cells following inhibition of signal transduction by 17-allylamino-17-demethoxygeldanamycin, an inhibitor of the hsp90 molecular chaperone: P.A. Clarke, et al.; Oncogene 19, 4125 (2000) Abstract
Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts: R. Nimmanapalli, et al.; Cancer Res. 61, 1799 (2001) Abstract; Full Text
Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells: P.N. Munster, et al.; Cancer Res. 61, 2945 (2001) Abstract; Full Text
Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin: J. Yang, et al.; Cancer Res. 61, 4010 (2001) Abstract; Full Text
Enhancement of paclitaxel-mediated cytotoxicity in lung cancer cells by 17-allylamino geldanamycin: in vitro and in vivo analysis: D.M. Nguyen, et al.; Ann. Thorac. Surg. 72, 371 (2001) Abstract
ErbB2 degradation mediated by the co-chaperone protein CHIP: P. Zhou, et al.; J. Biol. Chem. 278, 13829 (2003) Abstract
Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells: R. Villa, et al.; Carcinogenesis 24, 851 (2003) Abstract
Geldanamycin and its 17-allylamino-17-demethoxy analogue antagonize the action of Cisplatin in human colon adenocarcinoma cells: differential caspase activation as a basis for interaction: I.A. Vasilevskaya, et al.; Cancer Res. 63, 3241 (2003) Abstract
A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors: A. Kamal, et al.; Nature 425, 407 (2003) Abstract
Chaperoning oncogenes: HSP90 as a target of geldanamycin: L. Neckers; Handb. Exp. Pharmacol. 259 (2006) Abstract
Drugging the cancer chaperone HSP90: Combinatorial therapeutic exploitation of oncogene addiction and tumor stress: P. Workman, et al.; Ann. N.Y. Acad. Sci. 1113, 202 (2007) Abstract
Synergism between etoposide and 17-AAG in leukemia cells: critical roles for Hsp90, FLT3, topoisomerase II, Chk1, and Rad51: Q. Yao, et al.; Clin. Cancer Res. 13, 1591 (2007) Abstract; Full Text
Phase I and pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with refractory advanced cancers: R.K. Ramanathan, et al.; Clin. Cancer Res. 13, 1769 (2007) Abstract
HSP90 inhibitor 17AAG causes apoptosis in ATRA-resistant acute promyelocytic leukemia cells: P.N. Meyer, et al.; Leuk. Res. 32, 143 (2008) Abstract
Intratumor injection of the Hsp90 inhibitor 17AAG decreases tumor growth and induces apoptosis in a prostate cancer xenograft model: C.R. Williams, et al.; J. Urol. 178, 1528 (2007) Abstract
Rituximab and 17-allylamino-17-demethoxygeldanamycin induce synergistic apoptosis in B-cell chronic lymphocytic leukaemia: A.J. Johnson, et al.; Br. J. Haematol. 139, 837 (2007) Abstract
An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models: U. Banerji, et al.; Cancer Chemother. Pharmacol. 62, 769 (2008) Abstract
Further Categories Containing This Product:
HSP90 / HtpG / Related Products • Tyrosine Kinase Inhibitors • Antibiotics - Other Signal Transduction Pathway Modulators • Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-380-099 Revised 03-Apr-08
Concanamycin C
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - ATPase Inhibitors
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ALX-380-099-C100   100 µg 30.00 USD Add To Cart
ALX-380-099-C500   500 µg 90.00 USD Add To Cart
Product Specification
FORMULA: C45H74O13
MW: 823.1
CAS NUMBER: 81552-34-3
RTECS: GK6887000
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥96%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in chloroform, methanol, acetonitrile or DMSO. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: VERY TOXIC.

Product Description
Antibiotic. Inhibits vacuolar-type H+-ATPase. Potential antiosteoporotic agent. Shows antiviral and immunosuppressive activity. Active against fungi and yeasts.
Product Specific Literature References
Structures of concanamycins B and C: H. Kinashi, et al.; J. Antibiot. (Tokyo) 35, 1618 (1982) Abstract
Isolation and characterization of concanamycins A, B and C: H. Kinashi, et al.; J. Antibiot. (Tokyo) 37, 1333 (1984) Abstract
Inhibitory effect of modified bafilomycins and concanamycins on P- and V-type adenosinetriphosphatases: S. Drose, et al.; Biochemistry 32, 3902 (1993) Abstract
Disruption of vma-1, the gene encoding the catalytic subunit of the vacuolar H(+)-ATPase, causes severe morphological changes in Neurospora crassa: E.J. Bowman, et al.; J. Biol. Chem. 275, 167 (2000) Abstract
Semisynthetic derivatives of concanamycin A and C, as inhibitors of V- and P-type ATPases: structure-activity investigations and developments of photoaffinity probes: S. Drose, et al.; Biochemistry 40, 2816 (2001) Abstract
Further Categories Containing This Product:
H+-ATPase / Related Products • Natural Products - Antiviral / anti-HIV Agents • Natural Products - Immunomodulators • Antitumor Antibiotics • Antibiotics - Antifungal
 
 
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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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
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Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • HSP90 / HtpG / Related Products • Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Antibiotics • Antitumor Agents (Enzyme 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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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 Antibiotics • Antitumor Agents (DNA Interaction & Gene Regulation)
 
 
ALX-380-113 Revised 16-Jun-08
Gilvocarcin V
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SYNONYMS Anandimycin A
Toromycin
B 21085
Antibiotic 1072B
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics - DNA Regulation / Transcription
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ALX-380-113-C250   250 µg 180.00 USD Add To Cart
ALX-380-113-M001   1 mg 540.00 USD Add To Cart
Product Specification
FORMULA: C27H26O9
MW: 494.5
CAS NUMBER: 77879-90-4; 84236-01-1
RTECS: DI2240000
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO.
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.
HAZARD: HARMFUL.

Product Description

Antibiotic. Cytotoxic against Gram-positive bacteria. Mediates a unique cross-linking reaction between DNA and histidine H3. Weakly active against Gram-negative bacteria, fungi and tumors. Antineoplastic and photosensitizing compound.
Product Specific Literature References
Gilvocarcins, new antitumor antibiotics. 1. Taxonomy, fermentation, isolation and biological activities: H. Nakano, et al.; J. Antibiot. (Tokyo) 34, 266 (1981) Abstract
Activation of antitumor agent gilvocarcins by visible light: R.K. Elespuru and S.K. Gonda; Science 223, 69 (1984) Abstract
Photosensitized DNA breaks and DNA-to-protein crosslinks induced in human cells by antitumor agent gilvocarcin V: M.J. Peak, et al.; Chem. Biol. Interact. 67, 267 (1988) 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 29A, 1985 (1993) Abstract
Photophysical properties of gilvocarcins V and M and their binding constant to calf thymus DNA: R. Oyola, et al.; Photochem. Photobiol. 65, 802 (1997) Abstract
Histone H3 and heat shock protein GRP78 are selectively cross-linked to DNA by photoactivated gilvocarcin V in human fibroblasts: A. Matsumoto and P.C. Hanawalt; Cancer Res. 60, 3921 (2000) Abstract; Full Text
Further Categories Containing This Product:
Antibiotics - Antifungal • 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