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Antitumor Agents (Enzyme Inhibitors)
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ALX-306-022 Revised 07-Feb-05
D-erythro-Sphingosine chloride, N,N,N-Trimethyl-
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SYNONYMS N,N,N-Trimethyl-D-erythro-sphingosine chloride
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Ceramides / Cerebrosides / Sphingolipids / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-306-022-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C21H44ClNO2
MW: 378.0
SOURCE/HOST: Synthetic.
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in water, methanol or DMSO; slightly soluble in chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Hygroscopic.

Product Description
Stable N-methylated derivative of sphingosine that exhibits antitumor and anti-inflammatory properties and inhibits platelet activating factor (PAF) activation and protein kinase C (PKC) activity. Inhibits IL-1β-induced NF-κB activation and cell surface expression of crucial selectins which promote adhesion of Lex- or sialosyl-Lex-expressing cells with platelets and endothelial cells.
Product Specific Literature References
Downregulation of GMP-140 (CD62 or PADGEM) expression on platelets by N,N-dimethyl and N,N,N-trimethyl derivatives of sphingosine: K. Handa, et al.; Biochemistry 30, 11682 (1991) Abstract
Cell membrane signaling as target in cancer therapy. II: Inhibitory effect of N,N,N-trimethylsphingosine on metastatic potential of murine B16 melanoma cell line: H. Okoshi, et al.; Cancer Res. 51, 6019 (1991) Abstract
Effect of sphingosine and its N-methyl derivatives on oxidative burst, phagokinetic activity, and trans-endothelial migration of human neutrophils: S. Kimura, et al.; Biochem. Pharmacol. 44, 1585 (1992) Abstract
Liposomal N,N,N-trimethylsphingosine (TMS) as an inhibitor of B16 melanoma cell growth and metastasis with reduced toxicity and enhanced drug efficacy compared to free TMS: cell membrane signaling as a target in cancer therapy III: Y.S. Park, et al.; Cancer Res. 54, 2213 (1994) Abstract
N,N,N-trimethylsphingosine inhibits interleukin-1 beta-induced NF-kappa B activation and consequent E-selectin expression in human umbilical vein endothelial cells: A. Masamune, et al.; FEBS Lett. 367, 205 (1995) Abstract
Lysophosphatidylcholine promotes P-selectin expression in platelets and endothelial cells. Possible involvement of protein kinase C activation and its inhibition by nitric oxide donors: T. Murohara, et al.; Circ. Res. 78, 780 (1996) Abstract; Full Text
Further Categories Containing This Product:
PKC Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Anti-inflammatory Agents Other Products • NF-kB Pathway Inhibitors
 
 
ALX-270-400 Revised 31-Mar-05
SU 9516
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SYNONYMS 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-400-M005   5 mg 80.00 USD Add To Cart
ALX-270-400-M025   25 mg 320.00 USD Add To Cart
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Product Specification
FORMULA: C13H11N3O2
MW: 241.3
PURITY: ≥95%
APPEARANCE: Yellow to orange solid.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. Packaged under inert gas.

Product Description
Cell permeable, potent, selective and ATP-competitive inhibitor of CDK2/cyclin A (IC50=22nM), CDK1/cyclin B (IC50=40nM) and CDK4/cyclin D1 (IC50=200nM). Has no effect on the activity of PKC, p38, PDGFRβ and EGFR (IC50>10µM). Displays anti-proliferative and pro-apoptotic properties in tumor cells. Inhibits proliferation of growth factor-stimulated colon carcinoma cells by binding to CDK2 and thus preventing the phosphorylation of pRb and its dissociation from E2F.
Product Specific Literature References
A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells: M.E. Lane, et al.; Cancer Res. 61, 6170 (2001) Abstract
SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells: B. Yu, et al.; Biochem Pharmacol. 64, 1091 (2002) Abstract
SU9516: biochemical analysis of cdk inhibition and crystal structure in complex with cdk2: D.J. Moshinsky, et al.; BBRC 310, 1026 (2003) Abstract
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors: X. Li, et al.; Bioorg. Med. Chem. Lett. 13, 1939 (2003) Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Anti-proliferative) • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-430-022 Revised 11-Jun-08
Suramin . hexasodium salt
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SYNONYMS Suramin . 6Na
PRODUCT LINE Neurobiology
PRODUCT CATEGORY P2X Purinergic Receptors / Related Products
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ALX-430-022-M050   50 mg 33.00 USD Add To Cart
ALX-430-022-M250   250 mg 132.00 USD Add To Cart
ALX-430-022-G001   1 g 310.00 USD Add To Cart
Product Specification
FORMULA: C51H34N6O23S6 . 6Na
MW: 1291.2 . 137.9
CAS NUMBER: 129-46-4
MERCK INDEX: 14: 9006
RTECS: QM7000000
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water or physiological saline; sparingly soluble in 95% ethanol; insoluble in benzene, ether or chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
P2x and P2y purinergic receptor antagonist. Antitumor and antiparasitic compound.
Product Specific Literature References
PPADS and suramin as antagonists at cloned P2Y- and P2U-purinoceptors: S.J. Charlton, et al.; Br. J. Pharmacol. 118, 704 (1996) Abstract
Further Categories Containing This Product:
P2Y Purinergic Receptors / Related Products • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-400-053 Revised 21-Apr-08
Teniposide
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SYNONYMS (5R,5aR,8aR,9S)-5,8,8a,9-Tetrahydro-5-(4-hydroxy-3,5-dimethoxyphenyl)-9-[[4,6-O-[(R)-2-thienylmethylene]-β-D-glucopyranosyl]oxy]furo[3’,4’:6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one
4’-Demethylepipodophyllotoxin-β-D-thenylidine glucoside
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (DNA Interaction & Gene Regulation)
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ALX-400-053-M025   25 mg 55.00 USD Add To Cart
ALX-400-053-M100   100 mg 165.00 USD Add To Cart
Product Specification
FORMULA: C32H32O13S
MW: 656.7
CAS NUMBER: 29767-20-2
MERCK INDEX: 14: 9145
SOURCE/HOST: Semisynthetic derivative of podophyllotoxin.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in acetone or dimethyl formamide; slightly soluble in methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Glycoside-derivative of podophyllotoxin. Has cytostatic effect. Inhibits topoisomerase II. Induces apoptosis.
Product Specific Literature References
Role of topoisomerase II in mediating epipodophyllotoxin-induced DNA cleavage: W. Ross, et al.; Cancer Res. 44, 5857 (1984) Abstract; Full Text
Human cytochrome P450 metabolism of teniposide and etoposide: M.V. Relling, et al.; J. Pharmacol. Exp. Ther. 261, 491 (1992) Abstract
Topoisomerase II as a target of VM-26 and 4’-(9-acridinylamino)methanesulfon-m-aniside in atypical multidrug resistant human small cell lung carcinoma cells: S de Jong, et al.; Cancer Res. 53, 1064 (1993) Abstract; Full Text
Topoisomerase II trapping agent teniposide induces apoptosis and G2/M or S phase arrest of oral squamous cell carcinoma: J. Li, et al.; World J. Surg. Oncol. 4, 41 (2006) Abstract; Full Text
Related Products
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers) • Antitumor Agents (Enzyme Inhibitors) • Natural Products - Antitumor Reagents • Topoisomerase Inhibitors Other Products
 
 
ALX-350-133 Revised 28-May-08
Topotecan . hydrochloride
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SYNONYMS 9-[(Dimethylamino)methyl]-10-hydroxy-(20S)-camptothecin . HCl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Topoisomerase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-133-M001   1 mg 30.00 USD Add To Cart
ALX-350-133-M005   5 mg 90.00 USD Add To Cart
ALX-350-133-M025   25 mg 315.00 USD Add To Cart
Product Specification
FORMULA: C23H23N3O5 . HCl
MW: 421.5 . 36.5
CAS NUMBER: 119413-54-6
MERCK INDEX: 14: 9548
SOURCE/HOST: Semisynthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: Light yellow to greenish powder.
SOLUBILITY: Soluble in water (1mg/ml) or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Potent antitumor agent. Inhibitor of DNA-topoisomerase. Analog of (S)-(+)-camptothecin (Prod. No. ALX-350-015). Used in chemotherapy of several different cancers.
Product Specific Literature References
Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity: W.D. Kingsbury, et al.; J. Med. Chem. 34, 98 (1991) Abstract
In vitro and in vivo activity of topotecan against human B-lineage acute lymphoblastic leukemia cells: F.M. Uckun, et al.; Blood 85, 2817 (1995) Abstract
Clinical status and optimal use of topotecan: C.H. Takimoto & S.G. Arbuck; Oncology (Williston Park) 11, 1635 (1997), Review Abstract
Topoisomerase I inhibition with topotecan: pharmacologic and clinical issues: B. Arun & E.P. Frenkel; Expert Opin. Pharmacother. 2, 491 (2001), Review Abstract
Topotecan for the treatment of small-cell lung cancer: S.J. Nicum & M.E. O´Brien; Expert Rev. Anticancer Ther. 7, 795 (2007) Abstract
Related Products
Further Categories Containing This Product:
Natural Products - Antitumor Reagents • Antitumor Agents (Enzyme Inhibitors)
 
 
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