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Antitumor Agents (Anti-proliferative)
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ALX-350-262 Revised 07-Oct-08
Kuanoniamine C
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-262-M001   1 mg 98.00 USD Add To Cart
Product Specification
FORMULA: C21H18N4OS
MW: 374.5
CAS NUMBER: 133401-11-3
SOURCE/HOST: Isolated from the sponge Oceanapia spec.
PURITY: ≥97%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Cytotoxic. Inhibits proliferation of several cell lines. Binds to adenosine receptor subtypes A1 and A2A.
Product Specific Literature References
Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp: C. Eder, et al.; J. Nat. Prod. 61, 301 (1998) Abstract
Pyrroloquinoline and pyridoacridine alkaloids from marine sources: Q. Ding, et al.; Curr. Med. Chem. 6, 1 (1999) Abstract
Further Categories Containing This Product:
Alkaloids • Adenosine Receptors / Related Products • Natural Products for Neurological Research • Antitumor Agents (Anti-proliferative) • Marine Natural Products
 
 
ALX-385-016 Revised 02-Jun-08
Morin
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SYNONYMS 2’,3,4’,5,7-Pentahydroxyflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonols
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ALX-385-016-G001   1 g 16.00 USD Add To Cart
Product Specification
FORMULA: C15H10O7
MW: 302.2
CAS NUMBER: 480-16-0
MERCK INDEX: 14: 6269
RTECS: LK8749000
PURITY: ≥85%
APPEARANCE: White to brown powder.
SOLUBILITY: Soluble in methanol or 100% ethanol; slightly soluble in ether or acetic acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: IRRITANT.

Product Description
Antioxidant flavonoid. Shows anti-proliferative and antitumor properties. Induces apoptosis. Induces cell cycle arrest at the G2/M phase. Anti-inflammatory compound. Suppresses NF-κB activation. Induces lipid peroxidation and DNA strand breaks.
Product Specific Literature References
Structure-antioxidant activity relationships of flavonoids and phenolic acids: C.A. Rice-Evans, et al.; Free Radical Biol. & Med. 20, 933 (1996), (Review) Abstract
Lipid peroxidation and DNA damage induced by morin and naringenin in isolated rat liver nuclei: S. C. Sahu & G. C. Gray; Food Chem. Toxicol. 35, 443 (1997) Abstract
Morin inhibits the growth of human leukemia HL-60 cells via cell cycle arrest and induction of apoptosis through mitochondria dependent pathway: H.M. Kuo, et al.; Anticancer Res. 27, 395 (2007) Abstract
Morin (3,5,7,2’,4’-Pentahydroxyflavone) abolishes nuclear factor-kappaB activation induced by various carcinogens and inflammatory stimuli, leading to suppression of nuclear factor-kappaB-regulated gene expression and up-regulation of apoptosi: S.K. Manna, et al.; Clin. Cancer Res. 13, 2290 (2007) Abstract
Further Categories Containing This Product:
NF-kB Pathway Inhibitors • Natural Products - Anti-inflammatory Agents • Antitumor Agents (Anti-proliferative) • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Antitumor Reagents • Natural Products - Antioxidants • Cell Cycle Blockers & Inhibitors / Related Products • Natural Products for Cell Cycle Research • Lipid Peroxidation
 
 
ALX-380-281 Revised 20-Jun-08
PKC412
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SYNONYMS 4’-N-Benzoyl-staurosporine
Midostaurin
CGP 41251
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-380-281-M001   1 mg 60.00 USD Add To Cart
ALX-380-281-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C35H30N4O4
MW: 570.6
CAS NUMBER: 120685-11-2
MERCK INDEX: 14: 6185
SOURCE/HOST: Semisynthetic product prepared from staurosporine (a fermentation product of Streptomyces staurosporeus) (Prod. No. ALX-380-014).
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (10mg/ml), MDC (10mg/ml) or methanol (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Inhibitor of a variety of serine/threonine and tyrosine kinases, like protein kinase C (PKC), cyclic AMP-dependent protein kinase (PKA), S6 kinase, Akt (protein kinase B; PKB) and epidermal growth factor receptor (EGFR) tyrosine kinase activity. Potently inhibits FLT-3 kinase in vitro and in vivo. Apoptosis inducer. Showed broad antiproliferative activity against various tumor cell lines. Selectively inhibits T lymphocyte production of TNF-α. Upregulates endothelial nitric oxide synthase (eNOS; NOS III).
Product Specific Literature References
Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251: E. Andrejauskas-Buchdunger & U. Regenass; Cancer Res. 52, 5353 (1992) Abstract; Full Text
Analogs of staurosporine: potential anticancer drugs?: A. Gescher; Gen. Pharmacol. 31, 721 (1998), (Review) Abstract
Differential effects of UCN-01, staurosporine and CGP 41 251 on cell cycle progression and CDC2/cyclin B1 regulation in A431 cells synchronized at M phase by nocodazole: T. Akiyama, et al.; Anticancer Drugs 10, 67 (1999) Abstract
Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent: D. Fabbro, et al.; Pharmacol. Ther. 82, 293 (1999) Abstract
The phosphatidylinositide 3’-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C: A. Tenzer, et al.; Cancer Res. 61, 8203 (2001) Abstract; Full Text
Phase I and pharmacokinetic study of PKC412, an inhibitor of protein kinase C: D.J. Propper, et al.; J. Clin. Oncol. 19, 1485 (2001) Abstract; Full Text
A protein kinase C inhibitor induces phenotypic reversion of ras-transformed pancreatic cancer cells and cooperatively blocks tumor cell proliferation with an anti- ras peptide.: D. Way, et al.; Cancer Chemother. Pharmacol. 49, 429 (2002) Abstract
Protein kinase C inhibitors: H.C. Swannie & S.B. Kaye; Curr. Oncol. Rep. 4, 37 (2002), (Review) Abstract
PKC412 inhibits the zinc finger 198-fibroblast growth factor receptor 1 fusion tyrosine kinase and is active in treatment of stem cell myeloproliferative disorder: J. Chen, et al.; PNAS 101, 14479 (2004) Abstract; Full Text
Cotreatment with 17-allylamino-demethoxygeldanamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3: P. George, et al.; Cancer Res. 64, 3645 (2004) Abstract; Full Text
Effects of the kinase inhibitor CGP41251 (PKC 412) on lymphocyte activation and TNF-alpha production: M.S. Si, et al.; Int. Immunopharmacol. 5, 1141 (2005) Abstract
N-Benzoylstaurosporine (PKC412) inhibits Akt kinase inducing apoptosis in multiple myeloma cells.: N.J. Bahlis, et al.; Leuk. Lymphoma 46, 899 (2005) Abstract
Midostaurin upregulates eNOS gene expression and preserves eNOS function in the microcirculation of the mouse: H. Li, et al.; Nitric Oxide 12, 231 (2005) Abstract
Inhibitors of the PI3-kinase/Akt pathway induce mitotic catastrophe in non-small cell lung cancer cells: T.H. Hemström, et al.; Int. J. Cancer 119, 1028 (2006) Abstract
Antitumor and normal cell protective effect of PKC412 in the athymic mouse model of ovarian cancer: M. Kim, et al.; Ann. Clin. Lab. Sci. 36, 455 (2006) Abstract
PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects.: K.V. Gleixner, et al.; Blood 107, 752 (2006) Abstract; Full Text
Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT: K.V. Gleixner, et al.; Haematologica 92, 1451 (2007) Abstract; Full Text
PKC 412 small-molecule tyrosine kinase inhibitor: single-compound therapy for pancreatic cancer: J. El Fitori, et al.; Cancer 110, 1457 (2007) Abstract
PKC412 (CGP41251) modulates the proliferation and lipopolysaccharide-induced inflammatory responses of RAW 264.7 macrophages: K. Miyatake, et al.; BBRC 360, 115 (2007) Abstract
Divergent cytotoxic effects of PKC412 in combination with conventional antileukemic agents in FLT3 mutation-positive versus -negative leukemia cell lines.: Y. Furukawa, et al.; Leukemia 21, 1005 (2007) Abstract
PKC412 demonstrates JNK-dependent activity against human multiple myeloma cells: J. Sharkey, et al.; Blood 109, 1712 (2007) Abstract
The FLT3 inhibitor PKC412 exerts differential cell cycle effects on leukemic cells depending on the presence of FLT3 mutations: T. Odgerel, et al.; Oncogene 27, 3102 (2008) Abstract
The FLT3 inhibitor PKC412 in combination with cytostatic drugs in vitro in acute myeloid leukemia: L. Möllgard, et al.; Cancer Chemother. Pharmacol. 62, 439 (2008) Abstract
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Further Categories Containing This Product:
PKA Inhibitors • PKC Inhibitors • Staurosporine / Related Products • Akt [PKB] / Related Products • EGFR Kinase Inhibitors • Antitumor Agents (Anti-proliferative) • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Nitric Oxide Pathway Modulators • NOS Cofactors & Activators • Ribosomal Protein S6 Kinase / Related Products
 
 
ALX-630-086 Revised 10-Oct-08
Podophyllotoxin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Toxins
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ALX-630-086-M100   100 mg 45.00 USD Add To Cart
Product Specification
FORMULA: C22H22O8
MW: 414.4
CAS NUMBER: 518-28-5
MERCK INDEX: 14: 7546
RTECS: LV2500000
SOURCE/HOST: Isolated from Podophyllum peltatum.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble 100% ethanol or acetone, acetic acid or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from moisture. Very hygroscopic.
HAZARD: TOXIC.

Product Description
Potent inhibitor of microtubule assembly. Antineoplastic glucoside. Antitumor agent. DNA topoisomerase II inhibitor.
Product Specific Literature References
Podophyllotoxin-resistant mutants of Chinese hamster ovary cells: cross- resistance studies with various microtubule inhibitors and podophyllotoxin analogues: R.S. Gupta; Cancer Res. 43, 505 (1983) Abstract
Antitumor agents. I. DNA topoisomerase II inhibitory activity and the structural relationship of podophyllotoxin derivatives as antitumor agents: T. Terada, et al.; Chem. Pharmacol. Bull. (Tokyo) 40, 2720 (1992) Abstract
Podophyllotoxin, steganacin and combretastatin: natural products that bind at the colchicine site of tubulin: D.L. Sackett; Pharmacol. Therap. 59, 163 (1993) Abstract
Antineoplastic and antiviral activities of podophyllotoxin related lignans: M. Gordaliza, et al.; Arch. Pharmacol. 327, 175 (1994) Abstract
Er:YAG laser followed by topical podophyllotoxin for hard-to-treat palmoplantar warts.: U. Wollina; Cosmet. Laser Ther. 5, 35 (2003) Abstract
An evidence-based review of medical and surgical treatments of genital warts.: N. Scheinfeld & DS. Lehman; Dermatol. Online J. 12, 5 (2006) Abstract
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Further Categories Containing This Product:
Antitumor Agents (Anti-proliferative) • Natural Products for Cytoskeletal Research • Microtubule Modulators • Natural Products - Topoisomerase Inhibitors • Natural Products - Antitumor Reagents
 
 
ALX-270-459 Revised 22-May-07
PQ401
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SYNONYMS IGF-IR Inhibitor
N-(5-Chloro-2-methoxyphenyl)-N’-(2-methyl-4-quinolinyl)urea
PRODUCT LINE Chemokines & Cytokines
PRODUCT CATEGORY Insulin-like Growth Factors [IGFs] & Receptors / Related Products
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ALX-270-459-M001   1 mg 40.00 USD Add To Cart
ALX-270-459-M005   5 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C18H16ClN3O2
MW: 341.8
CAS NUMBER: 196868-63-0
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO (10mg/ml) or methanol (7mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
MELTINGPOINT: 208-210°C

Product Description
Potent inhibitor of insulin-like growth factor I receptor (IGF-IR) signalling and breast cancer cell growth in culture and in vivo.
Product Specific Literature References
Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth: K.L. Gable, et al.; Mol. Cancer Ther. 5, 1079 (2006) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Antitumor Agents (Anti-proliferative)
 
 
ALX-350-323 Revised 20-Jun-08
Psoralidin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-323-M001   1 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C20H16O5
MW: 336.3
CAS NUMBER: 18642-23-4
SOURCE/HOST: Isolated from Psoralea corylifolia.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Antineoplastic compound. Cytotoxic against stomach cancer cell lines. Shows antibacterial activity against Shigella sonnei and S. flexneri. Shows strong antioxidant activity and inhibits tyrosine phosphatase 1B (PTP1B) activity. Was shown to possess potent antidepressant properties.
Product Specific Literature References
Influence of nitrogen on accumulation of isosojagol (a newly detected coumestan in soybean) and associated isoflavonoids in roots and nodules of mycorrhizal and non-mycorrhizal soybean: D. Morandi and J.L. Le Quere; New Phytol. 117, 75 (1991) Full Text
The cytotoxicity of psoralidin from Psoralea corylifolia: Y.M. Yang, et al.; Planta Med. 62, 353 (1996) Abstract
Coumarins: A. Estevez-Braun and A.G. Gonzalez; Nat. Prod. Rep. 14, 465 (1997) Abstract
Cytotoxic constituents of Psoralea corylifolia: W. Mar, et al.; Arch. Pharm. Res. 24, 211 (2001) Abstract
Antibacterial compounds from the seeds of Psoralea corylifolia: N.A. Khatune, et al.; Fitoterapia 75, 228 (2004) Abstract
Inducible flavone in oats (Avena sativa) is a novel defense against plant-parasitic nematodes: I. R. Soriano, et al.; Nematology 94, 1207 (2004) Full Text
Antioxidants from a Chinese medicinal herb - Psoralea corylifolia L.: G. Jiangning, et al.; Food Chem. 91, 287 (2005)
In vitro protein tyrosine phosphatase 1B inhibitory phenols from the seeds of Psoralea corylifolia: Y.C. Kim, et al.; Planta Med. 71, 87 (2005) Abstract
Antidepressant-like effects of psoralidin isolated from the seeds of Psoralea Corylifolia in the forced swimming test in mice: L.T. Yi, et al.; Prog. Neuropsychopharmacol. Biol. Psychiatry 32, 510 (2008) Abstract
Further Categories Containing This Product:
Monoamine Neurotransmitters & Receptors Other Products • Antitumor Agents (Anti-proliferative) • Natural Products with Antibiotic Activity • Natural Products - Antioxidants • Natural Products - Other Signal Transduction Pathway Modulators • Protein Tyrosine Phosphatases Other Products
 
 
ALX-480-083 Revised 05-Jun-07
Puromycin aminonucleoside
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SYNONYMS 3'-Amino-3'-deoxy-N,N-dimethyl-adenosine
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-480-083-M010   10 mg 50.00 USD Add To Cart
ALX-480-083-M050   50 mg 160.00 USD Add To Cart
ALX-480-083-M250   250 mg 590.00 USD Add To Cart
Product Specification
FORMULA: C12H18N6O3
MW: 294.3
CAS NUMBER: 58-60-6
RTECS: AU7337000
PURITY: ≥95%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: MAY BE TERATOGENIC. MAY BE MUTAGENIC.

Product Description
Antibiotic with antineoplastic properties. Does not inhibit protein synthesis or induce apoptosis. May cause nephrosis.
Product Specific Literature References
Puromycin aminonucleoside suppresses integrin expression in cultured glomerular epithelial cells: U. Krishnamurti, et al.; J. Am. Soc. Nephrol. 12, 758 (2001) Abstract
Further Categories Containing This Product:
Antitumor Agents (Anti-proliferative)
 
 
ALX-270-346 Revised 28-May-08
Ratjadone A (synthetic)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-270-346-C002   2 µg 150.00 USD Add To Cart
Product Specification
FORMULA: C28H40O5
MW: 456.6
CAS NUMBER: 163564-92-9
SOURCE/HOST: Synthetic.
PURITY: ≥95%
FORMULATION: Liquid. Solution in methanol.
SOLUBILITY: Soluble in methanol (20mg/ml) or aqueous buffers (<100µM).
SHIPPING: SHIPPED ON DRY ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Sensitive to acids and bases. Unstable in acidic buffer systems (pH<6). Stable in substance as oil and in solution in methanol at -20°C.
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Represents a new class of natural compounds, which inhibit proliferation in eukaryotes by blocking nuclear export. As potent as leptomycin B (Prod. No. ALX-380-100) and specific for G1/S checkpoint. Cytotoxic secondary metabolite (IC50=50pg/ml in mouse cell line L929) that arrests tumor cells in the G1 phase at remarkably low concentrations (50pg/ml in HeLa cell line KB3.1). Inhibits the binding between the nuclear export signal (NES) of proteins and the chromosome maintenance region protein (CRM1). Anticancer compound. Belongs to the family of orphan ligands which include polyketides like leptomycin B, callystatin A and other related compounds.
Product Specific Literature References
Antibiotics from gliding bacteria, LXIII. Ratjadone: a new antifungal metabolite from Sorangium cellulosum: D. Schummer, et al.; Liebigs Ann. 685 (1995)
Ratjadon: a new antifungal compound from Sorangium cellulosum (myxobacteria) production, physio-chemical and biological properties: J. Gerth, et al.; J. Antibiot. 48, 973 (1995) Abstract
The chemistry and biology of ratjadone: M. Kalesse, et al.; ChemBioChem. 9, 709 (2001) Abstract
The chemistry and biology of the leptomycin family: M. Kalesse & M. Christmann; Synthesis 8, 981 (2002) Abstract
Ratjadone and leptomycin B block CRM1-dependent nuclear export by identical mechanisms: T. Meissner, et al.; FEBS Lett. 576, 27 (2004)
Nuclear targeting of adenovirus type 2 requires CRM1-mediated nuclear export: S. Strunze, et al.; Mol. Biol. Cell 16, 2999 (2005) Abstract
Further Categories Containing This Product:
Antitumor Antibiotics • Antibiotics - Antifungal • Cell Cycle Blockers & Inhibitors / Related Products • Nuclear Envelope & Nuclear Transport • Antitumor Agents (Anti-proliferative)
 
 
ALX-270-369 Revised 28-May-08
Ratjadone C (native)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-270-369-C005   5 µg 180.00 USD Add To Cart
Product Specification
FORMULA: C28H40O5
MW: