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Antitumor Agents (Enzyme Inhibitors)
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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
Ordering Information
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:
Tyrosine Kinase Inhibitors • TNF-alpha & TNF Receptors Other Products • Cell Cycle Blockers & Inhibitors / Related Products • EGFR Kinase Inhibitors • Natural Products - Topoisomerase Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Natural Products - Antitumor Reagents • Active Substances from Fruit and Vegetables • Antitumor Agents (Apoptosis Inducers) • Natural Products for Cell Cycle Research • Natural Products for Angiogenesis Research • Natural Products - Apoptosis Inducers & Inhibitors • Isoflavones • Antitumor Agents (Anti-proliferative)
 
 
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 • Antitumor Agents (Enzyme Inhibitors) • Parasitic Diseases Other Products
 
 
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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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:
Protein Kinase Inhibitors Other Products • Akt [PKB] / Related Products • Antitumor Agents (Enzyme 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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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:
Antitumor Agents (Enzyme Inhibitors) • Natural Products - Antitumor Reagents
 
 
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 • erbB-2 / Related Products • Antitumor Agents (Enzyme Inhibitors)
 
 
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) • Antitumor Agents (Apoptosis Inducers) • MDR Other Products • Folic Acid & Folate Receptors / Related Products • DNA Replication Inhibitors
 
 
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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ALX-270-193-G005   5 g 80.00 USD Add To Cart
Product Specification
FORMULA: C13H12N2O5S
MW: 308.3
CAS NUMBER: 51803-78-2
MERCK INDEX: 14: 6548
PURITY: ≥99%
APPEARANCE: Light tan crystals.
SOLUBILITY: Soluble in 100% ethanol, methanol, DMSO or acetonitrile. Ethanol is most commonly used for stock solutions, but solubility is only about 4mg/ml.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Selective inhibitor of cyclooxygenase 2 (COX-2). Platelet aggregation inhibitor.
Product Specific Literature References
Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system: J. Barnett, et al.; Biochim. Biophys. Acta 1209, 130 (1994) Abstract
A structural feature of N-[2-(cyclohexyloxy)-4-nitrophenyl] methanesulfonamide (NS-398) that governs its selectivity and affinity for cyclooxygenase 2 (COX2): R. Huff, et al.; Inflamm. Res. 44, S145 (1995) Abstract
Purification and characterization of prostaglandin H synthase-2 from sheep placental cotyledons: J.L. Johnson, et al.; Arch. Biochem. Biophys. 324, 26 (1995) Abstract
Further Categories Containing This Product:
Antithrombotic Agents / Platelet Aggregation Inhibitors / Related Products • Antitumor Agents (Enzyme Inhibitors) • COX Inhibitors • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-086 Revised 08-Apr-08
Nordihydroguaiaretic acid
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SYNONYMS NDGA
4,4'-(2,3-Dimethyl-1,4-butanediyl)bis[1,2-benzenediol]
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products for Inflammation Research
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-086-G001   1 g 62.00 USD Add To Cart
Product Specification
FORMULA: C18H22O4
MW: 302.4
CAS NUMBER: 500-38-9
MERCK INDEX: 14: 6693
SOURCE/HOST: Synthetic.
PURITY: ≥95%
APPEARANCE: Crystalline powder.
SOLUBILITY: Soluble in 100% ethanol, methanol or acetone; slightly soluble in hot water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C

Product Description
Antioxidant and antineoplastic. Lipoxygenase inhibitor. Stimulates the rapid retrograde movement of both Golgi stacks and the trans-Golgi network to the endoplasmatic reticulum (ER). Displays pleiotropic effects on cells, which include apoptosis, cell proliferation, differentiation and chemotaxis. Anticancer agent.
Product Specific Literature References
Inhibition of tumoral cell respiration and growth by nordihydroguaiaretic acid: M. Pavani, et al.; Biochem. Pharmacol. 48, 1935 (1994) Abstract
Nordihydroguaiaretic acid blocks protein transport in the secretory pathway causing redistribution of Golgi proteins into the endoplasmic reticulum: T. Fujiwara, et al.; J. Biol. Chem. 273, 3068 (1998) Abstract; Full Text
Effect of nordihydroguaiaretic acid on the secretion of lipoprotein lipase: S.M. Kim, et al.; J. Biochem. Mol. Biol. 35, 518 (2002) Abstract; Full Text
Mechanisms underlying the activation of large conductance Ca2+-activated K+ channels by nordihydroguaiaretic acid: H. Yamamura, et al.; Jpn. J. Pharmacol. 89, 53 (2002) Abstract
Direct interaction of the Golgi membrane with the endoplasmic reticulum membrane caused by nordihydroguaiaretic acid: T. Fujiwara, et al.; BBRC 301, 927 (2003) Abstract
Stepwise dissection of the intracellular fate of cationic cell-penetrating peptides: R. Fischer, et al.; J. Biol. Chem. 279, 12625 (2004) Abstract; Full Text
The anti-apoptotic effects of nordihydroguaiaretic acid: inhibition of cPLA(2) activation during TNF-induced apoptosis arises from inhibition of calcium signaling: C.A. Culver, et al.; Life Sci. 77, 2457 (2005) Abstract
Nordihydroguaiaretic acid is a potent in vitro scavenger of peroxynitrite, singlet oxygen, hydroxyl radical, superoxide anion and hypochlorous acid and prevents in vivo ozone-induced tyrosine nitration in lungs: E. Floriano-Sanchez, et al.; Free Radic. Res. 40, 523 (2006) Abstract
Nordihydroguaiaretic acid affects multiple dynein-dynactin functions in interphase and mitotic cells: K. Arasaki, et al.; Mol. Pharmacol. 71, 454 (2007) Abstract
Protective role of nordihydroguaiaretic acid (NDGA) against the genotoxic damage induced by ethynodiol diacetate in human lymphocytes in vitro: Y.H. Siddique, et al.; J. Environ. Biol. 28, 279 (2007) Abstract
Further Categories Containing This Product:
Golgi Apparatus • Lipoxygenases / Related Products • Natural Products - Antioxidants • Natural Products - Antitumor Reagents • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-300-006 Revised 03-Jul-06
1-O-Octadecyl-2-O-methyl-rac-glycero-3-phosphocholine
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SYNONYMS rac-ET-18-OCH3
Edelfosine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phospholipids / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-300-006-M050   50 mg 45.00 USD Add To Cart
ALX-300-006-M250   250 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C27H58NO6P
MW: 523.7
CAS NUMBER: 70641-51-9
RTECS: YK0718000
PURITY: ≥99%
APPEARANCE: White to off-white amorphous solid.
SOLUBILITY: