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ALX-300-093

Revised 23-Mar-05

Hexadecyl-phosphocholine (C16:0)
SYNONYMS	Miltefosine
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Phospholipids / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-300-093-M250		250 mg	50.00 USD
ALX-300-093-G001		1 g	150.00 USD

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:

Antitumor Agents (Enzyme Inhibitors) • PKC 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]
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Phosphoinositide 3-kinase [PI(3)K] / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-292-M001		1 mg	85.00 USD
ALX-270-292-M005		5 mg	330.00 USD

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:

ALX-430-139

Revised 20-Feb-08

Irinotecan . hydrochloride . trihydrate
SYNONYMS	Camptosar 7-ethyl-10-hydroxycamptothecin CPT-11
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Topoisomerase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-430-139-M005		5 mg	90.00 USD
ALX-430-139-M025		25 mg	315.00 USD

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
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Antitumor Reagents

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-292-C500		500 µg

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 • Antitumor Agents (Enzyme Inhibitors) • Natural Products - Protein Kinase Inhibitors • erbB-2 / Related Products

ALX-440-045

Revised 17-Jul-07

Methotrexate
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
ALX-440-045-M100		100 mg	45.00 USD
ALX-440-045-M500		500 mg	135.00 USD
ALX-440-045-G001		1 g	240.00 USD

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) • Folic Acid & Folate Receptors / Related Products • DNA Replication Inhibitors • MDR Other Products

ALX-270-193

Revised 04-Mar-05

Nimesulide
SYNONYMS	N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide
PRODUCT LINE	Inflammation
PRODUCT CATEGORY	Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-193-G005		5 g	80.00 USD

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:

Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Apoptosis Inducers) • COX Inhibitors

ALX-350-086

Revised 08-Apr-08

Nordihydroguaiaretic acid
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

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 • Antitumor Agents (Enzyme Inhibitors) • Lipoxygenases / Related Products • Natural Products - Antioxidants • Natural Products - Antitumor Reagents

ALX-300-006

Revised 03-Jul-06

1-O-Octadecyl-2-O-methyl-rac-glycero-3-phosphocholine
SYNONYMS	rac-ET-18-OCH₃ Edelfosine
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Phospholipids / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-300-006-M050		50 mg	45.00 USD
ALX-300-006-M250		250 mg	180.00 USD

Product Specification

FORMULA:	C₂₇H₅₈NO₆P
MW:	523.7
CAS NUMBER:	70641-51-9
RTECS:	YK0718000
PURITY:	≥99%
APPEARANCE:	White to off-white amorphous solid.
SOLUBILITY:	Soluble in chloroform (50mg/ml), 100% ethanol (5mg/ml) or water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Hygroscopic.
HAZARD:	MAY BE MUTAGENIC. HARMFUL.

Product Description

Produces strong antitumor and antimetastatic activities. Inhibits phosphatidylinositol specific phospholipase C and protein kinase C (PKC). Induces apoptosis.

Product Specific Literature References

Antiinvasive effect of racemic 1-O-octadecyl-2-O-methylglycero-3- phosphocholine on MO4 mouse fibrosarcoma cells in vitro: G.A. Storme, et al.; Cancer Res. 45, 351 (1985) Abstract
Cytotoxic ether phospholipids. Different affinities to lysophosphocholine acyltransferases in sensitive and resistant cells: D.B.J. Herrmann & H.A. Neumann; J. Biol. Chem. 261, 7742 (1986) Abstract; Full Text
Inhibition of Na,K-ATPase and sodium pump by anticancer ether lipids and protein kinase C inhibitors ET-18-OCH3 and BM 41.440: K. Oishi, et al.; BBRC 157, 1000 (1988) Abstract
Solubilization of the NADPH-oxidase from bone marrow derived macrophages by dialkylphospholipid and purification by HPLC-anion exchange chromatography: J. Storch & E. Ferber; Biol. Chem. Hoppe-Seyler 369, 403 (1988) Abstract
Molecular dynamics of antitumor ether-linked phospholipids in model membranes: a spin-label study: C.-S. Lai, et al.; BBRC 160, 1189 (1989) Abstract
The ether lipid 1-octadecyl-2-methyl-rac-glycero-3-phosphocholine induces expression of fos and jun proto-oncogenes and activates AP-1 transcription factor in human leukaemic cells: F. Mollinedo, et al.; Biochem. J. 302, 325 (1994) Abstract
Ether lipids enhance the cytotoxic effect of teniposide and paclitaxel in liposomes against leukaemic cells in culture: B.B. Lundberg; Anticancer Drug Des. 12, 503 (1997) Abstract
Selective induction of apoptosis in cancer cells by the ether lipid ET- 18-OCH3 (Edelfosine): molecular structure requirements, cellular uptake, and protection by Bcl-2 and Bcl-X(L): F. Mollinedo, et al.; Cancer Res. 57, 1320 (1997) Abstract
The inhibition of cell signaling pathways by antitumor ether lipids: G. Arthur & R. Bittman; Biochim. Biophys. Acta. 1390, 85 (1998) Abstract
Cytotoxic etherphospholipid analogues: D. Berkovic; Gen Pharmacol. 31, 511 (1998) Abstract
Involvement of c-Jun NH2-terminal kinase activation and c-Jun in the induction of apoptosis by the ether phospholipid 1-O-octadecyl-2-O- methyl-rac-glycero-3-phosphocholine: C. Gajate, et al.; Mol. Pharmacol. 53, 602 (1998) Abstract
The anticancer drug edelfosine is a potent inhibitor of neovascularization in vivo: W.R. Vogler, et al.; Cancer Invest. 16, 549 (1998) Abstract
Liposomal ET-18-OCH(3) induces cytochrome c-mediated apoptosis independently of CD95 (APO-1/Fas) signaling: O. Cuvillier, et al.; Blood 94, 3583 (1999) Abstract
Induction of apoptosis in human mitogen-activated peripheral blood T- lymphocytes by the ether phospholipid ET-18-OCH3: involvement of the Fas receptor/ligand system: C. Cabaner, et al.; Br. J. Pharmacol. 127, 813 (1999) Abstract
Alkyl-lysophospholipids activate the SAPK/JNK pathway and enhance radiation-induced apoptosis: G.A. Ruiter, et al.; Cancer Res. 59, 2457 (1999) Abstract
Intracellular triggering of Fas, independently of FasL, as a new mechanism of antitumor ether lipid-induced apoptosis: C. Gajate, et al.; Int. J. Cancer 85, 674 (2000) Abstract
Involvement of mitochondria and caspase-3 in ET-18-OCH(3)-induced apoptosis of human leukemic cells: C. Gajate, et al.; Int. J. Cancer 86, 208 (2000) Abstract

Further Categories Containing This Product:

Phospholipase C / Related Products • Antitumor Agents (Enzyme Inhibitors) • PKC Inhibitors • Antitumor Agents (Apoptosis Inducers)

ALX-300-004

Revised 13-Mar-08

1-O-Octadecyl-2-O-methyl-sn-glycero-3-phosphocholine
SYNONYMS	2-O-Methyl-PAF-C-18 sn-ET-18-OCH₃ Edelfosine
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Phospholipids / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-300-004-M050		50 mg	40.00 USD
ALX-300-004-M250		250 mg	160.00 USD
ALX-300-004-G001		1 g	480.00 USD

Product Specification

FORMULA:	C₂₇H₅₈NO₆P
MW:	523.7
CAS NUMBER:	77286-66-9
PURITY:	≥98%
APPEARANCE:	White amorphous powder.
SOLUBILITY:	Soluble in 100% ethanol, DMSO or dimethyl formamide.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Hygroscopic.

Product Description

Produces strong antitumor and antimetastatic activities. Inhibits phosphatidylinositol specific phospholipase C and protein kinase C from various leukemic cells. Antineoplastic activity.

Product Specific Literature References