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Antitumor Reagents
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ALX-350-298 Revised 03-Apr-08
Betulinic acid (~95%)
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SYNONYMS 3β-Hydroxy-20(29)-lupaene-28-oic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-298-M100   100 mg 55.00 USD Add To Cart
ALX-350-298-M500   500 mg 180.00 USD Add To Cart
ALX-350-298-G001   1 g 290.00 USD Add To Cart
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Product Specification
FORMULA: C30H48O3
MW: 456.7
CAS NUMBER: 472-15-1
SOURCE/HOST: Isolated from Platanus acerifolia (plane tree) bark.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator.
Product Specific Literature References
Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids: T. Fujioka, et al.; J. Nat. Prod. 57, 243 (1994) Abstract
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis: E. Pisha, et al.; Nat. Med. 1, 1046 (1995) Abstract
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents: Y. Kashiwada, et al.; J. Med. Chem. 39, 1016 (1996) Abstract
Betulinic acid triggers CD95 (APO-1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors: S. Fulda, et al.; Cancer Res. 57, 4956 (1997) Abstract
Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives: F. Hashimoto, et al.; Bioorg. Med. Chem. 5, 2133 (1997) Abstract
Betulinic acid induces apoptosis in human neuroblastoma cell lines: M.L. Schmidt, et al.; Eur. J. Cancer 33, 2007 (1997) Abstract
Induction of p53 without increase in p21WAF1 in betulinic acid-mediated cell death is preferential for human metastatic melanoma: M. Rieber & M. Strasberg Rieber; DNA Cell Biol. 17, 399 (1998) Abstract
Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid: S. Fulda, et al.; J. Biol. Chem. 273, 33942 (1998) Abstract; Full Text
Betulinic acid inhibits aminopeptidase N activity: M.F. Melzig & H. Bormann; Planta Med. 64, 655 (1998) Abstract
Correspondence re: S. Fulda et al., Betulinic acid triggers CD95 (Apo1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors. Cancer Res., 57: 4956, 1997: M. Rieber & M. Strasberg Rieber; Cancer. Res. 58, 5876 (1998) Abstract
Betulinic acid: a new cytotoxic agent against malignant brain-tumor cells: S. Fulda, et al.; Int. J. Cancer 82, 435 (1999) Abstract
Betulinic acid-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing: W. Wick, et al.; J Pharmacol. Exp. Ther. 289, 1306 (1999) Abstract; Full Text
Effects of betulinic acid alone and in combination with irradiation in human melanoma cells: E. Selzer, et al.; J. Invest. Dermatol. 114, 935 (2000) Abstract
Betulinic acid suppresses carcinogen-induced NF-kappa B activation through inhibition of I kappa B alpha kinase and p65 phosphorylation: abrogation of cyclooxygenase-2 and matrix metalloprotease-9: Y. Takada & B.B. Aggarwal; J. Immunol. 171, 3278 (2003) Abstract
Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection: R.H. Cichewicz & S.A. Kouzi; Med. Res. Rev. 24, 90 (2004), Review Abstract
Betulinic acid-induced apoptosis in leukemia cells: H. Ehrhardt, et al.; Leukemia 18, 1406 (2004) Abstract
Betulinic acid and its derivatives: a review on their biological properties: P. Yogeeswari & D. Sriram; Curr. Med. Chem. 12, 657 (2005), Review Abstract
Betulinic acid decreases expression of bcl-2 and cyclin D1, inhibits proliferation, migration and induces apoptosis in cancer cells: W. Rzeski, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 374, 11 (2006) Abstract
Activation and inhibition of the proteasome by betulinic acid and its derivatives: L. Huang, et al.; FEBS Lett. 581, 4955 (2007) Abstract
Further Categories Containing This Product:
CDK & Cyclin Inhibitors • NF-kB Pathway Inhibitors • Other Natural Products - DNA Regulation / Transcription • Natural Products - NF-kB Pathway Inhibitors • MPTP [Mitochondrial Transition Pore] / Related Products • Natural Products - Anti-inflammatory Agents • Natural Products - Antiviral / anti-HIV Agents • Antitumor Agents (Apoptosis Inducers) • Ubiquitin & Proteasome Other Products • Natural Products - Apoptosis Inducers & Inhibitors • HIV / AIDS / Related Products
 
 
ALX-350-313 Revised 11-Dec-07
3-O-Acetyl-betulinic acid
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-313-M005   5 mg 35.00 USD Add To Cart
ALX-350-313-M025   25 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C32H50O4
MW: 498.8
CAS NUMBER: 10376-50-8
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO; sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Shows cytotoxic activity on human cancer cell lines.
Product Specific Literature References
Synthesis and cytotoxic activity of 3-O-acyl/3-hydrazine /2-bromo/20,29-dibromo betulinic acid derivatives: R. Mukherjee, et al.; Bioorg. Med. Chem. Lett. 14, 4087 (2004) Abstract
Synthesis of A-seco derivatives of betulinic acid with cytotoxic activity: M. Urban, et al.; J. Nat. Prod. 67, 1100 (2004) Abstract
 
 
ALX-270-476 Revised 11-Mar-08
Bicalutamide
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SYNONYMS N-(4-Cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methylpropanamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Androgens & Androgen Receptors / Related Products
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ALX-270-476-M100   100 mg 40.00 USD Add To Cart
ALX-270-476-M500   500 mg 140.00 USD Add To Cart
ALX-270-476-G001   1 g 220.00 USD Add To Cart
Product Specification
FORMULA: C18H14F4N2O4S
MW: 430.4
CAS NUMBER: 90357-06-5
SOURCE/HOST: Synthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in acetone and tetrahydrofuran; slightly soluble in 100% ethanol or methanol; practically insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Nonsteroidal antiandrogen. Effective in the treatment of prostate cancer. Induces cell death by a pathway that is independent of changes in mitochondrial membrane potential and Bcl-2 action.
Product Specific Literature References
Antiproliferative activity of casodex (ICI 176.334) in hormone-dependent tumours: A. Maucher & E. von Angerer; J. Cancer Res. Clin. Oncol. 119, 669 (1993) Abstract
Antiandrogen-induced cell death in LNCaP human prostate cancer cells: E.C. Lee, et al.; Cell Death Differ. 10, 761 (2003) Abstract
Proanthocyanidins from grape seeds inhibit expression of matrix metalloproteinases in human prostate carcinoma cells, which is associated with the inhibition of activation of MAPK and NF kappa B: P.K. Vayalil, et al.; Carcinogenesis 25, 987 (2004) Abstract; Full Text
Wnt3a growth factor induces androgen receptor-mediated transcription and enhances cell growth in human prostate cancer cells: M. Verras, et al.; Cancer Res. 64, 8860 (2004) Abstract; Full Text
Glycogen synthase kinase-3beta activity is required for androgen-stimulated gene expression in prostate cancer: X. Liao, et al.; Endocrinology 145, 2941 (2004) Abstract; Full Text
A phase I pharmacokinetic and pharmacodynamic study of OGX-011, a 2’-methoxyethyl antisense oligonucleotide to clusterin, in patients with localized prostate cancer: K.N. Chi, et al.; J. Natl. Cancer Inst. 97, 1287 (2005) Abstract; Full Text
The mechanisms and managements of hormone-therapy resistance in breast and prostate cancers: K.M. Rau, et al.; Endocr. Relat. Cancer 12, 511 (2005), Review Abstract; Full Text
Signal transduction pathways in androgen-dependent and -independent prostate cancer cell proliferation: P.M. Ghosh, et al.; Endocr. Relat. Cancer 12, 119 (2005) Abstract; Full Text
Recent advances on multiple tumorigenic cascades involved in prostatic cancer progression and targeting therapies: M. Mimeault & S.K. Batra; Carcinogenesis 27, 1 (2006), Review Abstract; Full Text
Bcl-xL is overexpressed in hormone-resistant prostate cancer and promotes survival of LNCaP cells via interaction with proapoptotic Bak: C. Castilla, et al.; Endocrinology 147, 4960 (2006) Abstract; Full Text
Androgen receptor corepressors and prostate cancer: C.J. Burd, et al.; Endocr. Relat. Cancer 13, 979 (2006), Review Abstract; Full Text
Par-4-dependent apoptosis by the dietary compound withaferin A in prostate cancer cells: S. Srinivasan, et al.; Cancer Res. 67, 246 (2006) Abstract; Full Text
Androgen receptor structural and functional elements: role and regulation in prostate cancer: S.M. Dehm & D.J. Tindall; Mol. Endocrinol. 21, 2855 (2007), Review Abstract
Phosphoinositide 3-kinase-independent non-genomic signals transit from the androgen receptor to Akt1 in membrane raft microdomains: B. Cinar, et al.; JBC 282, 29584 (2007) Abstract; Full Text
A novel class of pyranocoumarin anti-androgen receptor signaling compounds: J. Guo, et al.; Mol. Cancer Ther. 6, 907 (2007) Abstract; Full Text
Increased resistance to trail-induced apoptosis in prostate cancer cells selected in the presence of bicalutamide: M. Mitterberger, et al.; Prostate 67, 1194 (2007) Abstract
Interplay of nuclear factor-kappaB and B-myb in the negative regulation of androgen receptor expression by tumor necrosis factor alpha: S. Ko, et al.; Mol. Endocrinol. 22, 273 (2008) Abstract
Further Categories Containing This Product:
Antitumor Agents (Hormone-related) • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-630-107 Revised 21-Feb-08
Bleomycin . sulfate
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SYNONYMS Blenoxane
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-630-107-M010   10 mg 155.00 USD Add To Cart
ALX-630-107-M050   50 mg 595.00 USD Add To Cart
Product Specification
FORMULA: C55H82N17O21S3 . H2SO4
MW: 1413.6 . 98.1
CAS NUMBER: 9041-93-4
MERCK INDEX: 14: 1318
RTECS: EC5991990
SOURCE/HOST: A group of related glycopeptide antibiotics isolated from Streptomyces verticillus.
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (20mg/ml) or methanol.
ACTIVITY: 1'500-2'000 IU/mg
(corresponds to 1.5-2.0 bleomycin units (USP)/mg)
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Solutions in normal saline (~2mg/ml) are stable for 3 months when stored at +4°C in a glass container or stable for 1 month when stored at +4°C in a PVC container. Solutions in water are stable for several days only.
HAZARD: MAY BE CARCINOGENIC. TOXIC.

Product Description

Radiomimetic DNA-cleaving agent that produces double and single DNA strand breaks through an oxygen-radical-dependent mechanism. Inhibits intracellular DNA replication. DNA alkylating agent. Antineoplastic.
Product Specific Literature References
Bleomycin and other antitumor antibiotics of high molecular weight: H. Umezawa; Antimicrobial Agents Chemother. (Bethesda) 5, 1079 (1965) Abstract
Specificity of deoxyribonucleic acid cleavage by bleomycin, phleomycin, and tallysomycin: J. Kross, et al.; Biochemistry 21, 4310 (1982) Abstract
Chromatin structure during bleomycin-induced DNA damage and repair
: B.P. Cuiffo, et al.; J. Free Radic. Biol. Med. 1, 139 (1985) Abstract
Cleavage of tRNA by Fe(II)-bleomycin: A. Huttenhofer, et al.; J. Biol. Chem. 267, 24471 (1992) Abstract
Antiangiogenic chemotherapeutic agents: characterization in comparison to their tumor growth inhibition in human renal cell carcinoma models: M. Schirner, et al.; Clin. Cancer Res. 4, 1331 (1998) Abstract
Sequence-specific changes in the metal site of ferric bleomycin induced by the binding of DNA: J.W. Sam, et al.; J. Biol. Chem. 273, 16090 (1998) Abstract
Changes in c-Jun but not Bcl-2 family proteins in p53-dependent apoptosis of mouse cerebellar granule neurons induced by DNA damaging agent bleomycin: T. Araki, et al.; Brain Res. 794, 239 (1998) Abstract
Induction of apoptosis by bleomycin in resting and cycling human lymphocytes: P. Vernole, et al.; Mutagenesis 13, 209 (1998) Abstract
Synergistic Effects of Laserthermia and Bleomycin-sulfate on Micronuclei Formation in Cytokinesis-blocked HeLa Cells: A.Sh. Monfared & H. Mozdarani; Irn. J. Med. Sci. 24, 87 (1999)
Bleomycin: new perspectives on the mechanism of action: S.M. Hecht; J. Nat. Prod. 63, 158 (2000), (Review) Abstract
Bleomycin-induced alterations in DNA replication: relationship to DNA damage: J. Dziegielewski, et al.; Biochemistry 40, 704 (2001) Abstract
Further Categories Containing This Product:
Antitumor Agents (DNA Interaction & Gene Regulation) • DNA Fragmentation & Chromatin Condensation
 
 
ALX-350-019 Revised 16-Oct-08
(+)-Brefeldin A
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SYNONYMS BFA
Ascotoxin
Decumbin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-019-M005   5 mg 80.00 USD Add To Cart
ALX-350-019-M010   10 mg 130.00 USD Add To Cart
ALX-350-019-M025   25 mg 270.00 USD Add To Cart
ALX-350-019-M050   50 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C16H24O4
MW: 280.4
CAS NUMBER: 20350-15-6
MERCK INDEX: 14: 1369
SOURCE/HOST: Isolated from Eupenicillium brefeldianum.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, methanol, acetone or ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Inhibitor of intracellular protein transport and protein secretion, interfering with trafficking in the trans-Golgi network, leading to the accumulation of cycling proteins in ERGIC clusters. Blocks ADP-ribosylation factor (Arf) in an inactive GDP-bound conformation and thereby prevents binding of COPI coats to ERGIC and Golgi membranes. Upon brefeldin A treatment the Golgi rapidly tubulates and fuses with the ER by an energy-, temperature-, and microtubule-dependent process. In contrast, the drug has little effect on the ERGIC, which keeps its identity, although the ERGIC clusters become larger and more uniformly distributed in the cytoplasm of the cells. Inhibits intracellular collagen degradation. Also inhibits apical Na+ channels in epithelia. Induces apoptosis.
Product Specific Literature References
Decumbin, a new compound from a species of Penicillium: V.L. Singleton, et al.; Nature 181, 1072 (1958)
Über die Isolierung neuer Stoffwechselprodukte aus Penicillium brefeldianum Dodge.: E. Harri, et al.; Helv. Chim. Acta 46, 1235 (1963)
Novel blockade by brefeldin A of intracellular transport of secretory proteins in cultured rat hepatocytes: Y. Misumi, et al.; J. Biol. Chem. 261, 11398 (1986) Abstract; Full Text
Brefeldin A causes disassembly of the Golgi complex and accumulation of secretory proteins in the endoplasmic reticulum: T. Fujiwara, et al.; J. Biol. Chem. 263, 18545 (1988) Abstract; Full Text
Brefeldin A, thapsigargin, and AIF4- stimulate the accumulation of GRP78 mRNA in a cycloheximide dependent manner, whilst induction by hypoxia is independent of protein synthesis: B.D. Price, et al.; J. Cell. Physiol. 152, 545 (1992) Abstract
Brefeldin A and the endocytic pathway. Possible implications for membrane traffic and sorting: W. Hunziker, et al.; FEBS Lett. 307, 93 (1992), (Review) Abstract
Brefeldin A inhibits degradation as well as production and secretion of collagen in human lung fibroblasts: C.R. Ripley, et al.; J. Biol. Chem. 268, 3677 (1993) Abstract
Brefeldin A is a potent inducer of apoptosis in human cancer cells independently of p53: R.G. Shao, et al.; Exp. Cell Res. 227, 190 (1996) Abstract
Brefeldin A inhibition of apical Na+ channels in epithelia: R.S. Fisher, et al.; Am. J. Physiol. 270, C138 (1996) Abstract
Brefeldin A: deciphering an enigmatic inhibitor of secretion: A. Nebenfuhr, et al.; Plant Physiol. 130, 1102 (2002), Review Abstract
NKT cells provide help for dendritic cell-dependent priming of MHC class I-restricted CD8+ T cells in vivo: D. Stober, et al.; J. Immunol. 170, 2540 (2003) Abstract; Full Text
Interaction of BIG2, a brefeldin A-inhibited guanine nucleotide-exchange protein, with exocyst protein Exo70: K.F. Xu, et al.; PNAS 102, 2784 (2005) Abstract
Further Categories Containing This Product:
ADP Ribosylation Factor [ARF] / Related Products • Golgi Apparatus • Collagen / Related Products • Na+ Channels • Antitumor Antibiotics • Antitumor Agents (Apoptosis Inducers) • Antibiotics - Antiviral / Anti-HIV • Antibiotics - Antifungal • Autophagy Other Products
 
 
ALX-385-029 Revised 07-Oct-08
4’-Bromoflavone
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SYNONYMS 4’-Bromo-2-phenylbenzopyran
4’-Bromo-2-phenyl-4H-1-benzopyran-4-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
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ALX-385-029-G001   1 g 90.00 USD Add To Cart
Product Specification
FORMULA: C15H9BrO2
MW: 301.1
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: IRRITANT.

Product Description
Chemopreventive compound. Potent inducer of phase II detoxifying enzymes.
Product Specific Literature References
Simple vs. complex inheritance of inducible aryl hydrocarbon hydroxylase in mouse tissues: K. Burki, et al.; Biochem. Genet. 13, 417 (1975) Abstract
Cancer chemopreventive activity mediated by 4’-bromoflavone, a potent inducer of phase II detoxification enzymes: L.L. Song, et al.; Cancer Res. 59, 578 (1999) Abstract
Further Categories Containing This Product:
Natural Products - Chemopreventive Agents • Respiratory Chain Other Products
 
 
ALX-350-005 Revised 02-Oct-07
Bryostatin 1
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-005-C010   10 µg 85.00 USD Add To Cart
Product Specification
FORMULA: C47H68O17
MW: 905.0
CAS NUMBER: 83314-01-6
MERCK INDEX: 14: 1457
PURITY: ≥97%
APPEARANCE: Colorless oil.
SOLUBILITY: 25mg/ml soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Store tightly sealed. Binds to glass and plastic surfaces in aqueous solutions.

Product Description
Binds to and activates protein kinase C (PKC). Antineoplastic.
Product Specific Literature References
Isolation and structure of Bryostatin 1: G.R. Pettit, et al.; J. Am. Chem. Soc. 104, 6846 (1982)
Bryostatin 1: differentiating agent from the depths: R.M. Stone; Leuk. Res. 21, 399 (1997) Abstract
Chemistry and clinical biology of the bryostatins: R. Mutter & M. Wills; Bioorg. Med. Chem. 8, 1841 (2000), (Review) Abstract
The clinical development of the bryostatins: A. Clamp and G.C. Jayson; Anticancer Drugs 13, 673 (2002) Abstract
The chemistry and biology of the bryostatin antitumour macrolides: K.J. Hale, et al.; Nat. Prod. Rep. 19, 413 (2002), Review Abstract
Bryostatin-1: pharmacology and therapeutic potential as a CNS drug: M.K. Sun & D.L. Alkon; CNS Drug Rev. 12, 1 (2006), Review Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Activators & Inducers) • PKC Activators • Natural Products - Immunomodulators • Natural Products - Antitumor Reagents • Marine Natural Products
 
 
ALX-400-048 Revised 06-Dec-07
Busulfan
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SYNONYMS 1,4-Butanediol dimethanesulfonate
PRODUCT LINE Cancer
PRODUCT CATEGORY Antitumor Agents (DNA Interaction & Gene Regulation)
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ALX-400-048-G010   10 g 20.00 USD Add To Cart
Product Specification
FORMULA: C6H14O6S2
MW: 246.3
CAS NUMBER: 55-98-1
MERCK INDEX: 14: 1505
RTECS: EK1750000
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White to off-white crystalline powder.
SOLUBILITY: Soluble in acetone, 100% ethanol or DMSO; insoluble in water.
SHIPPING: AMBIENT