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Antitumor Agents (Enzyme Inhibitors)
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ALX-380-065 Revised 24-Sep-08
Fostriecin
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SYNONYMS Phosphotrienin
CI-920
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Topoisomerase Inhibitors
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ALX-380-065-C010   10 µg 150.00 USD Add To Cart
Product Specification
FORMULA: C19H26O9PNa
MW: 452.4
CAS NUMBER: 87860-39-7
RTECS: UQ0600000
SOURCE/HOST: Isolated from Streptomyces pulveraceous subsp. fostreus.
PURITY: ≥98% (HPLC)
APPEARANCE: Colorless solid.
SOLUBILITY: Soluble in water (50mg/ml), methanol (10mg/ml) or 100% ethanol (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year when stored at -20°C. Use fresh solution.
HANDLING: Protect from light. Packaged under inert gas. Hygroscopic.

Product Description
Antitumor antibiotic. Catalytic inhibitor of topoisomerase II. Strong protein phosphatase 2A (PP2A) inhibitor (IC50=3.2nM). Weak inhibitor for PP1 (IC50=131µM). No apparent effect on PP2B. The binding site for fostriecin on PP2A is different from that of okadaic acid (see Prod. No. ALX-350-003).
Product Specific Literature References
Novel antitumor agents CI-920, PD 113,270 and PD 113,271. II. Isolation and characterization: S.S. Stampwala, et al.; J. Antibiot. (Tokyo) 36, 1601 (1983) Abstract
Novel antitumor agents CI-920, PD 113,270 and PD 113,271. I. Taxonomy, fermentation and biological properties: J.B. Tunac, et al.; J. Antibiot. (Tokyo) 36, 1595 (1983) Abstract
Studies on the biochemical mechanism of the novel antitumor agent, CI- 920: D.W. Fry, et al.; Cancer Chemother. Pharmacol. 13, 171 (1984) Abstract
Anticancer activity of the structurally novel antibiotic Cl-920 and its analogues: W.R. Leopold, et al.; Cancer Res. 44, 1928 (1984) Abstract
Inhibition of type II topoisomerase by fostriecin: T.J. Boritzki, et al.; Biochem. Pharmacol. 37, 4063 (1988) Abstract
Comparison of effects of fostriecin, novobiocin, and camptothecin, inhibitors of DNA topoisomerases, on DNA replication and repair in human cells: C.M. Gedik & A.R. Collins; Nucl. Acids Res. 18, 1007 (1990) Abstract
The cell cycle related differences in susceptibility of HL-60 cells to apoptosis induced by various antitumor agents: W. Gorczyca, et al.; Cancer Res. 53, 3186 (1993) Abstract
Induction of DNA strand breaks associated with apoptosis during treatment of leukemias: W. Gorczyca, et al.; Leukemia 7, 659 (1993) Abstract
Antitumor drug fostriecin inhibits the mitotic entry checkpoint and protein phosphatases 1 and 2A: M. Roberge, et al.; Cancer Res. 54, 6115 (1994) Abstract
Fostriecin: a review of the preclinical data: R.S. de Jong, et al.; Anticancer Drugs 8, 413 (1997) Abstract
Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A: A.H. Walsh, et al.; FEBS Lett. 416, 230 (1997) Abstract
Fostriecin, an inhibitor of protein phosphatase 2A, limits myocardial infarct size even when administered after onset of ischemia: C. Weinbrenner, et al.; Circulation 98, 899 (1998) Abstract
Phase I and pharmacokinetic study of the topoisomerase II catalytic inhibitor fostriecin: R.S. de Jong, et al.; Br. J. Cancer 79, 882 (1999) Abstract
Fostriecin: chemistry and biology: D.S. Lewy, et al.; Curr. Med. Chem. 9, 2005 (2002) Abstract
Further Categories Containing This Product:
Antibiotics - Other Signal Transduction Pathway Modulators • Antitumor Antibiotics • Antitumor Agents (Enzyme Inhibitors) • PP2A / Related Products
 
 
ALX-350-006 Revised 05-Apr-08
Genistein (synthetic)
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SYNONYMS 4',5,7-Trihydroxyisoflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-006-M010   10 mg 25.00 USD Add To Cart
ALX-350-006-M025   25 mg 50.00 USD Add To Cart
ALX-350-006-M050   50 mg 90.00 USD Add To Cart
ALX-350-006-M100   100 mg 150.00 USD Add To Cart
ALX-350-006-G001   1 g 480.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 446-72-0
MERCK INDEX: 14: 4391
RTECS: NR2392000
SOURCE/HOST: Synthetic.
PURITY: ≥99% (HPLC)
APPEARANCE: White to yellow crystalline powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Tyrosine protein kinase inhibitor. Inhibits phosphorylation of EGFR kinase. Inhibits tumor cell proliferation and induces tumor cell differentiation. Inhibits topoisomerase II activity in vivo. Produces cell cycle arrest and apoptosis. Direct inhibitor of insulin-induced glucose uptake in adipocytes (IC50=20µM).
Product Specific Literature References
Genistein, a specific inhibitor of tyrosine-specific protein kinases: T. Akiyama, et al.; J. Biol. Chem. 262, 5592 (1987) Abstract; Full Text
Erbstatin blocks platelet activating factor-induced protein-tyrosine phosphorylation, polyphosphoinositide hydrolysis, protein kinase C activation, serotonin secretion and aggregation of rabbit platelets: H. Salari, et al.; FEBS Lett. 263, 104 (1990) Abstract
Mechanisms of cancer chemoprevention by soy isoflavone genistein: F.H. Sarkar & Y. Li; Cancer Metastasis Rev. 21, 265 (2002) Abstract
Soy isoflavone phyto-pharmaceuticals in interleukin-6 affections. Multi-purpose nutraceuticals at the crossroad of hormone replacement, anti-cancer and anti-inflammatory therapy: N. Dijsselbloem, et al.; Biochem. Pharmacol. 68, 1171 (2004), Review Abstract
Genistein affects testosterone secretion by Leydig cells in roosters (Gallus gallus domesticus): M. Opalka, et al.; Reprod. Biol. 4, 185 (2004) Abstract
Genistein directly inhibits GLUT4-mediated glucose uptake in 3T3-L1 adipocytes: M. Bazuine, et al.; BBRC 325, 511 (2005) Abstract
Decreased circulating levels of tumor necrosis factor-alpha in postmenopausal women during consumption of soy-containing isoflavones: Y. Huang, et al.; J. Clin. Endocrinol. Metab. 90, 3956 (2005) Abstract
Phytoestrogens and lipoproteins in women: C.N. Bairey Merz, et al.; J. Clin. Endocrinol. Metab. 91, 2209 (2006) Abstract
Clinical review: a critical evaluation of the role of soy protein and isoflavone supplementation in the control of plasma cholesterol concentrations: A. Dewell, et al.; J. Clin. Endocrinol. Metab. 91, 772 (2006), Review Abstract
The role of genistein and synthetic derivatives of isoflavone in cancer prevention and therapy: F.H. Sarkar, et al.; Mini Rev. Med. Chem. 6, 401 (2006), Review Abstract
Further Categories Containing This Product:
Natural Products - Topoisomerase Inhibitors • TNF-alpha & TNF Receptors Other Products • EGFR Kinase Inhibitors • Tyrosine Kinase Inhibitors • Active Substances from Fruit and Vegetables • Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Anti-proliferative) • Natural Products for Angiogenesis Research • Isoflavones • Cell Cycle Blockers & Inhibitors / Related Products • Antitumor Agents (Apoptosis Inducers) • Natural Products for Cell Cycle Research • Natural Products - Antitumor Reagents • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-300-093 Revised 23-Mar-05
Hexadecyl-phosphocholine (C16:0)
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SYNONYMS Miltefosine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phospholipids / Related Products
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ALX-300-093-M250   250 mg 50.00 USD Add To Cart
ALX-300-093-G001   1 g 150.00 USD Add To Cart
Product Specification
FORMULA: C21H46NO4P
MW: 407.6
CAS NUMBER: 58066-85-6
MERCK INDEX: 14: 6198
PURITY: ≥99%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent antitumor agent. Inhibitor of protein kinase C (PKC) and phosphatidylcholine biosynthesis. Costimulates human T cell activation.
Product Specific Literature References
H.R. Berger, et al.; Akt. Onkologie 34, 27 (1987)
The phospholipid analogue, hexadecylphosphocholine, inhibits protein kinase C in vitro and antagonises phorbol ester-stimulated cell proliferation: C.C. Geilen, et al.; Eur. J. Cancer 27, 1650 (1991) Abstract
The phospholipid analogue hexadecylphosphocholine inhibits phosphatidylcholine biosynthesis in Madin-Darby canine kidney cells: R. Haase, et al.; FEBS Lett. 288, 129 (1991) Abstract
Hexadecylphosphocholine-mediated enhancement of T-cell responses to interleukin 2: K. Vehmeyer, et al.; Cellular Immunology 137, 232 (1991) Abstract
Further Categories Containing This Product:
PKC Inhibitors • Parasitic Diseases Other Products • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-270-292 Revised 09-Feb-05
1L-6-Hydroxymethyl-chiro-inositol-2-[(R)-2-O-methyl-3-O-octadecylcarbonate]
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-270-292-M001   1 mg 85.00 USD Add To Cart
ALX-270-292-M005   5 mg 330.00 USD Add To Cart
Product Specification
FORMULA: C30H58O10
MW: 578.8
PURITY: >98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry.

Product Description
Potent inhibitor of Akt (PKB) (IC50=2.0µM). Weak inhibitor of PI(3)K (phosphoinositide 3-kinase) (IC50=83µM). Has been shown to inhibit the growth of the following cancer cell lines: HeLa (IC50=2.5µM), HT-29 (IC50=10µM), MCF-7 (IC50=1.2µM) and PC-3 (IC50=2.0µM).
Product Specific Literature References
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth: Y. Hu, et al.; J. Med. Chem. 43, 3045 (2000) Abstract
Further Categories Containing This Product:
Akt [PKB] / Related Products • Antitumor Agents (Enzyme Inhibitors) • Protein Kinase Inhibitors Other Products
 
 
ALX-270-492 Revised 23-Dec-08 New product
Imatinib . mesylate
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SYNONYMS STI-571
CGP-57148B
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Enzyme Inhibitors)
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-492-M025   25 mg 35.00 USD Add To Cart
ALX-270-492-M100   100 mg 90.00 USD Add To Cart
ALX-270-492-M500   500 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C29H31N7O . CH3SO3H
MW: 493.6 . 96.1
CAS NUMBER: 220127-57-1
MERCK INDEX: 14: 4902
PURITY: ≥98%
APPEARANCE: White to pale yellow crystalline powder.
SOLUBILITY: Freely soluble in water, sparingly soluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL). Also shown to inhibit the transmembrane receptor kit and platelet-derived growth factor (PDGF) receptors.
Product Specific Literature References
Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative: E. Buchdunger, et al.; Cancer Res. 56, 100 (1996) Abstract
Abl protein-tyrosine kinase inhibitor STI571 inhibits in vitro signal transduction mediated by c-kit and platelet-derived growth factor receptors: E. Buchdunger, et al.; J. Pharmacol. Exp. Ther. 295, 139 (2000) Abstract
The kinase inhibitor imatinib--an immunosuppressive drug?: D. Wolf, et al.; Cancer Drug Targets 7, 251 (2007), (Review) Abstract
Imatinib: C.E. de Kogel & J.H. Schellens; Oncologist 12, 1390 (2007), (Review) Abstract
Imatinib mesylate for the treatment of chronic myeloid leukemia: S. Soverini, et al.; Expert Rev. Anticancer Ther. 8, 853 (2008), (Review) Abstract
Imatinib as a novel therapeutic approach for fibrotic disorders: J.H. Distler & O. Distler; Rheumatology (Oxford) epub ahead of print, (2008) Abstract
Is autophagy rather than apoptosis the regression driver in imatinib-treated gastrointestinal stromal tumors?: F. Miselli, et al.; Transl. Oncol. 1, 177 (2008) Abstract
Combination of imatinib and vinorelbine enhances cell growth inhibition in breast cancer cells via PDGFR beta signalling: M.T. Weigel, et al.; Cancer Lett. 273, 70 (2009) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-430-139 Revised 20-Feb-08
Irinotecan . hydrochloride . trihydrate
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SYNONYMS Camptosar
7-ethyl-10-hydroxycamptothecin
CPT-11
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Topoisomerase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-139-M005   5 mg 90.00 USD Add To Cart
ALX-430-139-M025   25 mg 315.00 USD Add To Cart
Product Specification
FORMULA: C33H38N4O6 . HCl . 3H2O
MW: 586.7 . 36.4 . 54.0
CAS NUMBER: 100286-90-6; 136572-09-3
MERCK INDEX: 14: 5091
PURITY: ≥98% (HPLC)
APPEARANCE: Pale yellow powder.
SOLUBILITY: Slightly soluble in methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
A member of the camptothecin drug family, and an inhibitor of the nuclear enzyme topoisomerase I, which is involved in cellular DNA replication and transcription. During replication topoisomerase I mediates the relaxation of super coiled DNA, and its inhibition results in breakage of the DNA chain and likely induce apoptosis. Irinotecan is, therefore, an attractive target for anticancer drug development. Currently it is used for the treatment of small cell lung cancer and advanced colorectal cancer.
Product Specific Literature References
Induction of tumor necrosis factor by a camptothecin derivative, irinotecan, in mice and human mononuclear cells: S. Goto, et al.; Anticancer Res. 16, 2507 (1996) Abstract
The role of irinotecan in colorectal cancer: L.B. Saltz; Curr. Oncol. Rep. 1, 155 (1999) Abstract
Therapeutic advances in small cell lung cancer: F.P. Worden and G.P. Kalemkerian; Expert Opin. Investig. Drugs 9, 565 (2000) Abstract
Human DNA-Topoisomerases - Diagnostic and Therapeutic Implications for Cancer: U. Kellner, et al.; Onkologie 23, 424 (2000) Abstract
Irinotecan activates p53 with its active metabolite, resulting in human hepatocellular carcinoma apoptosis: Y. Takeba, et al.; J. Pharmacol. Sci. 104, 232 (2007) Abstract
Further Categories Containing This Product:
Natural Products - Antitumor Reagents • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-350-292 Revised 26-Mar-05
Kahalalide F - Discontinued Due to Patent Restrictions
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-292-C500   500 µg Inquire
Product Specification
FORMULA: C75H124N14O16
MW: 1477.9
CAS NUMBER: 149204-42-2
SOURCE/HOST: Isolated from marine mollusc Elysia rufescens.
PURITY: ≥95%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Highly selective activity against prostate tumors in vitro. Disrupts lysosomal membranes. Inhibitor of c-erbB-2 (ErbB2).
Product Specific Literature References
The antitumoral compound Kahalalide F acts on cell lysosomes: M. Garcia-Rocha, et al.; Cancer Lett. 99, 43 (1996) Abstract
Synthesis and structure determination of kahalalide F (1,2): Synthesis and structure determination of kahalalide F (1,2); J. Am. Chem. Soc. 123, 11398 (2001) Abstract
Chemical and enzymatic stability of a cyclic depsipeptide, the novel, marine-derived, anti-cancer agent kahalalide F: R.W. Sparidans, et al.; Anticancer Drugs 12, 575 (2001) Abstract
Preclinical toxicity studies of kahalalide F, a new anticancer agent: single and multiple dosing regimens in the rat: A.P. Brown, et al.; Cancer Chemother. Pharmacol. 50, 333 (2002) Abstract
Quantitative analysis of the novel depsipeptide anticancer drug Kahalalide F in human plasma by high-performance liquid chromatography under basic conditions coupled to electrospray ionization tandem mass spectrometry: E. Stokvis, et al.; J. Mass. Spectrom. 37, 992 (2002) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Natural Products - Protein Kinase Inhibitors • Antitumor Agents (Enzyme Inhibitors) • erbB-2 / Related Products
 
 
ALX-440-045 Revised 17-Jul-07
Methotrexate
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SYNONYMS (+)-Amethopterin
4-Amino-10-methylfolic acid
Methylaminopterin
MTX
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (Enzyme Inhibitors)
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-440-045-M050   50 mg 25.00 USD Add To Cart
ALX-440-045-M100   100 mg 45.00 USD Add To Cart
ALX-440-045-M500   500 mg 135.00 USD Add To Cart
ALX-440-045-G001   1 g 240.00 USD Add To Cart
Product Specification
FORMULA: C20H22N8O5
MW: 454.5
CAS NUMBER: 59-05-2
MERCK INDEX: 14: 5985
PURITY: ≥98%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in alkaline solution; insoluble in water, 100% ethanol or ether.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: TOXIC. MAY BE CARCINOGENIC. MAY BE TERATOGENIC.

Product Description
Folic acid antagonist. Potent inhibitor of dihydrofolate reductase. Induces apoptosis. Inhibits DNA synthesis. Anticancer agent.
Product Specific Literature References
Immunosuppressive properties of methotrexate: apoptosis and clonal deletion of activated peripheral T cells: L. Genestier, et al.; J. Clin. Invest. 102, 322 (1998) Abstract
Methotrexate induces apoptotic cell death in human keratinocytes: M. Heenen, et al.; Arch. Dermatol. Res. 290, 240 (1998) Abstract
Activation-dependent lymphocyte apoptosis induced by methotrexate: R. Paillot, et al.; Transplant. Proc. 30, 2348 (1998) Abstract
Methotrexate inhibits the first committed step of purine biosynthesis in mitogen-stimulated human T-lymphocytes: a metabolic basis for efficacy in rheumatoid arthritis?: L.D. Fairbanks, et al.; Biochem. J. 342, 143 (1999) Abstract
Antiproliferative and antiinflammatory effects of methotrexate on cultured differentiating myeloid monocytic cells (THP-1) but not on synovial macrophages from patients with rheumatoid arthritis: M. Cutolo, et al.; J. Rheumatol. 27, 2551 (2000) Abstract
Mechanisms of action of methotrexate: L. Genestier, et al.; Immunopharmacology 47, 247 (2000) Abstract
Further Categories Containing This Product:
Antitumor Agents (DNA Interaction & Gene Regulation) • DNA Replication Inhibitors • Antitumor Agents (Apoptosis Inducers) • Folic Acid & Folate Receptors / Related Products • MDR Other Products
 
 
ALX-270-193 Revised 04-Mar-05
Nimesulide
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SYNONYMS N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide
PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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