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DNA Replication
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ALX-480-099 Revised 25-Mar-08
5-Fluorouracil
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SYNONYMS 5-FU
2,4-Dioxo-5-fluoropyrimidine
5-Fluoro-2,4(1H,3H)-pyrimidinedione
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Apoptosis Inducers)
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ALX-480-099-G001   1 g 15.00 USD Add To Cart
ALX-480-099-G005   5 g 60.00 USD Add To Cart
Product Specification
FORMULA: C4H3FN2O2
MW: 130.1
CAS NUMBER: 51-21-8
MERCK INDEX: 14: 4181
RTECS: YR0350000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white crystalline powder.
SOLUBILITY: Soluble in DMSO (5mg/ml), dimethyl formamide (5mg/ml), methanol (1mg/ml) or hot water (1mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.
IDENTITY: Determined by IR and UV.

Product Description

Potent antitumor agent. Inhibits thymidylate synthetase. Induces p53-dependent apoptosis.

Product Specific Literature References
Apoptosis of human primary and metastatic colon adenocarcinoma cell lines in vitro induced by 5-fluorouracil, verapamil, and hyperthermia: I.B. Shchepotin, et al.; Anticancer Res. 14, 1027 (1994) Abstract
Modulation of the equilibrative nucleoside transporter by inhibitors of DNA synthesis: J. Pressacco, et al.; Br. J. Cancer 72, 939 (1995) Abstract
Nucleoside-mediated mitigation of 5-fluorouracil-induced toxicity in synchronized murine erythroleukemic cells: K.H. Elstein, et al.; Toxicol. Appl. Pharmacol. 146, 29 (1997) Abstract
Effects of perturbations of pools of deoxyribonucleoside triphosphates on expression of ribonucleotide reductase, a G1/S transition state enzyme, in p53-mutated cells: S. Wadler, et al.; Biochem. Pharmacol. 55, 1353 (1998) Abstract
Chemically-induced apoptosis: p21 and p53 as determinants of enterotoxin activity: D.M. Pritchard, et al.; Toxicol. Lett. 102, 19 (1998) Abstract
Effect of 5-fluorouracil on cell cycle regulatory proteins in human colon cancer cell line: H. Takeda, et al.; Jpn. J. Cancer Res. 90, 677 (1999) Abstract
5-fluorouracil sensitivity and dihydropyrimidine dehydrogenase activity in advanced gastric cancer: T. Inada, et al.; Anticancer Res. 20, 2457 (2000) Abstract
Further Categories Containing This Product:
DNA Replication Other Products
 
 
ALX-480-100 Revised 27-Mar-08
Fludarabine
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SYNONYMS 2-Fluoroadenine-9-β-D-arabinofuranoside
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Apoptosis Inducers)
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ALX-480-100-M005   5 mg 45.00 USD Add To Cart
ALX-480-100-M025   25 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C10H12FN5O4
MW: 285.2
CAS NUMBER: 21679-14-1
MERCK INDEX: 14: 4126
RTECS: AU6207000
PURITY: ≥98% (HPLC)
APPEARANCE: White to pale yellow crystalline powder.
SOLUBILITY: Sparingly soluble in water or organic solvents.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
IDENTITY: Determined by IR.

Product Description

Prodrug converted to the free nucleoside 9-β-D-arabinosyl-2-fluoroadenine (F-ara-A). F-ara-A enters cells and accumulates as the 5’-triphosphate. Interferes with DNA synthesis and repair. Induces apoptosis of cancer cells. Inhibits RNA transcription.

Product Specific Literature References
Fludarabine: a new agent with major activity against chronic lymphocytic leukemia: M.J. Keating, et al.; Blood 74, 19 (1989) Abstract; Full Text
Termination of DNA synthesis by 9-beta-D-arabinofuranosyl-2-fluoroadenine. A mechanism for cytotoxicity: P. Huang, et al.; J. Biol. Chem. 265, 16617 (1990) Abstract; Full Text
Action of 9-beta-D-arabinofuranosyl-2-fluoroadenine on RNA metabolism: P. Huang & W. Plunkett; Mol. Pharmacol. 39, 449 (1991) Abstract
Inhibition of RNA transcription: a biochemical mechanism of action against chronic lymphocytic leukemia cells by fludarabine: P. Huang, et al.; Leukemia 14, 1405 (2000) Abstract
Role of fludarabine in hematological malignancies: M. Montillo, et al.; Expert Rev. Anticancer Ther. 6, 1141 (2006) Abstract
Fludarabine-mediated suppression of the excision repair enzyme ERCC1 contributes to the cytotoxic synergy with the DNA minor groove crosslinking agent SJG-136 (NSC 694501) in chronic lymphocytic leukaemia cells: C. Pepper, et al.; Br. J. Cancer 97, 253 (2007) Abstract
Fludarabine induces apoptosis of human T-cell leukemia virus type 1-infected T cells via inhibition of the nuclear factor-kappaB signal pathway: C. Nishioka, et al.; Leukemia 21, 1044 (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-350-016 Revised 31-Jul-08
(+)-Aphidicolin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-016-M001   1 mg 65.00 USD Add To Cart
ALX-350-016-M005   5 mg 260.00 USD Add To Cart
ALX-350-016-M025   25 mg 890.00 USD Add To Cart
Product Specification
FORMULA: C20H34O4
MW: 338.5
CAS NUMBER: 38966-21-1
MERCK INDEX: 14: 727
RTECS: PB9185000
SOURCE/HOST: Isolated from Nigrospora oryzae.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (50mg/ml), methanol (10mg/ml) or 100% ethanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Reversible inhibitor of eukaryotic nuclear DNA replication. Useful for cell synchronization. Blocks the cell cycle at early S phase. Prolongs the half life of DNA methyltransferase. Specific inhibitor of DNA polymerase α and δ in eukaryotic cells and in some viruses of animal origin. Acts synergistically with vincristine and doxorubicin. Apoptosis inhibitor/inducer.
Product Specific Literature References
X-Ray crystallographic determination of the structure of the antibiotic aphidicolin: a tetracyclic diterpenoid containing a new ring system: K.M. Brundret, et al.; J. C. S. Chem. Commun. 1027 (1972)
The production of aphidicolin by Nigrospora sphaerica: A.N. Starratt and S.R Loschiavo; Can. J. Microbiol. 20, 416 (1974)
Aphidicolin prevents mitotic cell division by interfering with the activity of DNA polymerase-alpha: S. Ikegami, et al.; Nature 275, 458 (1978) Abstract
Inhibition by aphidicolin of cell cycle progression and DNA replication in sea urchin embryos: S. Ikegami, et al.; J. Cell. Physiol. 100, 439 (1979) Abstract
New views of the biochemistry of eucaryotic DNA replication revealed by aphidicolin, an unusual inhibitor of DNA polymerase alpha: J.A. Huberman; Cell 23, 647 (1981) Abstract
Aphidicolin: a specific inhibitor of nuclear DNA replication in eukaryotes: S. Spadari, et al.; TIBS 7, 29 (1982)
Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in human myeloid leukemia cell lines: K. Kuwakado, et al.; Biochem. Pharmacol. 46, 1909 (1993) Abstract
Life, death and genomic change in perturbed cell cycles: R.T. Schimke, et al.; Philos. Trans. R. Soc. London B Biol. Sci. 345, 311 (1994) Abstract
Dissociation of nuclear and cytoplasmic cell cycle progression by drugs employed in cell synchronization: L. Urbani, et al.; Exp. Cell. Res. 219, 159 (1995) Abstract
Drug-induced apoptosis is not necessarily dependent on macromolecular synthesis or proliferation in the p53-negative human prostate cancer cell line PC-3: M.M. Borner, et al.; Cancer Res. 55, 2122 (1995) Abstract
TrkA neurogenic receptor regulates differentiation of neuroblastoma cells: W. Poluha, et al.; Oncogene 10, 185 (1995) Abstract
Coordinate regulation of G- and C strand length during new telomere synthesis: X. Fan and C.M. Price; Mol. Biol. Cell 8, 2145 (1997) Abstract; Full Text
Effect of aphidicolin on DNA methyltransferase in the nucleus: I. Suetake, et al.; Cell Struct. Funct. 23, 137 (1998) Abstract
Cytotoxicity of aphidicolin and its derivatives against neuroblastoma cells in vitro: synergism with doxorubicin and vincristine: M. Michaelis, et al.; Anticancer Drugs 11, 479 (2000) Abstract
Aphidicolin and bleomycin induced chromosome damage as biomarker of mutagen sensitivity: a twin study: B. Tedeschi, et al.; Mutat. Res. 546, 55 (2004) Abstract
 
 
ALX-350-092 Revised 03-Apr-08
Emetine . dihydrochloride
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SYNONYMS 6’,7’,10,11-Tetramethoxyemetan . 2HCl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - DNA Replication Inhibitors
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ALX-350-092-M050   50 mg 10.00 USD Add To Cart
Product Specification
FORMULA: C29H40N2O4 . 2HCl
MW: 480.7 . 73.0
CAS NUMBER: 316-42-7
MERCK INDEX: 14: 3559
SOURCE/HOST: Isolated from ground roots of Uragoga ipecacuanha.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. Hygroscopic.
HAZARD: TOXIC.

Product Description
Irreversibly blocks protein synthesis by inhibiting the movement of ribosome along the mRNA. Induces hypotension by blocking adrenoreceptors. Inhibits DNA replication in the early S phase. Inhibits HIF-1 activation by hypoxia. Induces apoptosis in leukemia cells. Antiamebic.
Product Specific Literature References
Inhibitors of protein biosynthesis. V. Effects of emetine on protein and nucleic acid biosynthesis in HeLa cells: A.P. Grollman; J. Biol. Chem. 243, 4089 (1968) Abstract
Cytometric analysis of DNA replication inhibited by emetine and cyclosporin A:: A: T. Schweighoffer, et al.; Histochemistry 96, 93 (1991) Abstract
Emetine allows identification of origins of mammalian DNA replication by imbalanced DNA synthesis, not through conservative nucleosome segregation: W.C. Burhans, et al.; EMBO J. 10, 4351 (1991) Abstract
Role of newly synthesized MHC class II molecules in antigen-specific antigen presentation by B cells: T. Kokuho, et al.; Immunobiology 193, 42 (1995) Abstract
Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells: Y.D. Zhou, et al.; J. Nat. Prod. 68, 947 (2005) Abstract
The alkaloid emetine as a promising agent for the induction and enhancement of drug-induced apoptosis in leukemia cells: M. Moller, et al.; Oncol. Rep. 18, 737 (2007) Abstract
Characteristics of apoptosis induction by the alkaloid emetine in human tumour cell lines: M. Moller & M. Wink; Planta Med. 73, 1389 (2007) Abstract
 
 
ALX-350-146 Revised 03-Oct-07
Neobavaisoflavone
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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ALX-350-146-M001   1 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C20H18O4
MW: 322.4
CAS NUMBER: 41060-15-5
SOURCE/HOST: Isolated from plant Psoralea corylifolia.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR and MS.

Product Description
Inhibits platelet aggregation. DNA polymerase inhibitor. Shows antifungal activity.
Product Specific Literature References
Prenylated isoflavanone from the roots of Erythrina sigmoidea: A.E. Nkengfack, et al.; Phytochemistry 36, 1047 (1994) Abstract
Antiplatelet flavonoids from seeds of Psoralea corylifolia: W.J. Tsai, et al.; J. Nat. Prod. 59, 671 (1996) Abstract
DNA polymerase and topoisomerase II inhibitors from Psoralea corylifolia: N.J. Sun, et al.; J. Nat. Prod. 61, 362 (1998) Abstract
Studies on the chemical constituents of Psoralea corylifolia L.: B. Ruan, et al.; J. Asian Nat. Prod. Res. 9, 41 (2007) Abstract
 
 
ALX-380-023 Revised 19-Oct-07
Mitomycin C
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - DNA Replication Inhibitors
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ALX-380-023-M005   5 mg 98.00 USD Add To Cart
ALX-380-023-M010   10 mg 185.00 USD Add To Cart
Product Specification
FORMULA: C15H18N4O5
MW: 334.3
CAS NUMBER: 50-07-7
MERCK INDEX: 14: 6215
RTECS: CN0700000
SOURCE/HOST: Isolated from Streptomyces caespitosus.
PURITY: ≥98%
APPEARANCE: Blue-violet crystals.
SOLUBILITY: Soluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Antitumor antibiotic. Inhibitor of DNA synthesis, nuclear division and cancer cells. DNA intercalating agent. Apoptosis inducer.
Product Specific Literature References
Mitomycin, a new antibiotic from Streptomyces. I: T. Hata, et al.; J. Antibiot. (Tokyo) 9, 141 (1956) Abstract
S.K. Carter & S.T. Crooke ; 'Mitomycin C. Current Status and New Developments', Academic Press, New York (1979)
Revised absolute configuration of mitomycin C. X-ray analysis of 1-N-(p-bromobenzoyl)mitomycin C: K. Shirahata & N. Hirayama; JACS 105, 7199 (1983)
Sequence-specific DNA damage induced by reduced mitomycin C and 7-N-(p- hydroxyphenyl)mitomycin C: K. Ueda and T. Komano; Nucl. Acids Res. 12, 6673 (1984) Abstract
Isolation and structure of a covalent cross-link adduct between mitomycin C and DNA: M. Tomasz, et al.; Science 235, 1204 (1987) Abstract
The chemistry of DNA modification by antitumor antibiotics: J.F. Fisher & P.A. Aristoff; Prog. Drug Res. 32, 411 (1988) Abstract
DNA sequence specificity of mitomycin cross-linking: S.P. Teng, et al.; Biochemistry 28, 3901 (1989) Abstract
Polyoxyethylene-modified superoxide dismutase reduces side effects of adriamycin and mitomycin C: S. Kawasaki, et al.; J. Cancer Res. 83, 899 (1992) Abstract
Genetic evidence for an activator required for induction of pectin lyase in Erwinia carotovora subsp. carotovora by DNA-damaging agents: J.L. McEvoy, et al.; J. Bacteriol. 174, 5471 (1992) Abstract
Elevated DT-diaphorase activity and messenger RNA content in human non- small cell lung carcinoma: relationship to the response of lung tumor xenografts to mitomycin Cl: A.M. Malkinson, et al.; Cancer Res. 52, 4752 (1992) Abstract
Mitomycins: J. Verweij, et al.; Cancer Chemother. Biol. Response Modif. 18, 46 (1999) Abstract
Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95- independent manner in human gastric adenocarcinoma cells: I.C. Park, et al.; Cancer Lett. 158, 125 (2000) Abstract
Selective inhibition of cyclooxygenase-2 enhances mitomycin-C-induced apoptosis: C.T. Hsueh, et al.; Cancer Chemother. Pharmacol. 45, 389 (2000) Abstract
DNA-damaging agents cause inactivation of translational regulators linked to mTOR signalling: A.R. Tee & C.G. Proud; Oncogene 19, 3021 (2000) Abstract
Re-evaluation of tumor-specific cytotoxicity of mitomycin C, bleomycin and peplomycin: M. Sasaki, et al.; Anticancer Res. 26, 3373 (2006) Abstract
Activation of the S phase DNA damage checkpoint by mitomycin C: E. Mladenov, et al.; J. Cell. Physiol. 211, 468 (2007) Abstract
 
 
ALX-380-089 Revised 29-Jul-08
Blasticidin S . hydrochloride
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - DNA Replication Inhibitors
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ALX-380-089-M100   100 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C17H26N8O5 . HCl
MW: 422.4 . 36.5
CAS NUMBER: 3513-03-9
MERCK INDEX: 14: 1316
SOURCE/HOST: Isolated from Streptomyces griseochromogenes.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water; insoluble in organic solvents.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C