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ALX-430-128 Revised 21-Feb-08
Nutlin-3
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SYNONYMS (±)-4-[4,5-bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl]-piperazin-2-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY p53 Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-128-M001   1 mg 35.00 USD Add To Cart
ALX-430-128-M005   5 mg 160.00 USD Add To Cart
ALX-430-128-M025   25 mg 560.00 USD Add To Cart
Product Specification
FORMULA: C30H30Cl2N4O4
MW: 581.5
CAS NUMBER: 548472-68-0
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in methanol, 100% ethanol, DMSO, dimethyl formamide or acetonitrile; sparingly soluble in a 1:10 solution of ethanol:PBS, pH 7.2.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least one year after receipt when stored at -20°C.

We do not recommend storing the aqueous solution for more than one day.

HAZARD: IRRITANT.

Product Description
Inhibitor of p53/MDM2 interaction (IC50=0.09µM).
Product Specific Literature References
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2: L.T. Vassilev, et al.; Science 303, 844 (2004) Abstract
Reactivation of the p53 pathway as a treatment modality for KSHV-induced lymphomas: G. Sarek, et al.; J. Clin. Invest. 117, 1019 (2007) Abstract; Full Text
General Literature References
Drug discovery and p53: D.P. Lane, et al.; Drug Discov. Today 8, 347 (2003) Abstract
Further Categories Containing This Product:
Ubiquitin Ligases [E3]
 
 
ALX-430-151 Revised 22-Jul-08
RITA
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SYNONYMS Reactivation of p53 and Induction of Tumor Cell Apoptosis
2,5-bis(5-Hydroxymethyl-2-thienyl)furan
NSC652287
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY p53 Other Products
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ALX-430-151-M001   1 mg 75.00 USD Add To Cart
ALX-430-151-M005   5 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C14H12O3S2
MW: 292.4
CAS NUMBER: 213261-59-7
PURITY: ≥98%
APPEARANCE: White to yellow crystalline solid.
SOLUBILITY: Soluble in 100% ethanol (1mg/ml), DMSO (20mg/ml), dimethyl formamide (30mg/ml); 0.5mg/ml soluble in a 1:1 solution of dimethyl formamide: PBS (pH 7.2) (dilute the dimethyl formamide solution with PBS).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least two years after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.

Product Description
Inhibitor of p53/HDM2 interaction. Activator of p53 function in tumors. Potently inhibits the growth of a variety of  cancer cell lines in the submicromolar range. It has been suggested that RITA selectively targets cells expressing p53 by other mechanisms than direct binding to the N-terminal domain of p53 [4].
Product Specific Literature References
[1] DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells: W. Nieves-Neira, et al.; Mol. Pharmacol. 56, 478 (1999) Abstract; Full Text
[2] Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism: M.I. Rivera, et al.; Biochem. Pharmacol. 57, 1283 (1999) Abstract
[3] Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors: N. Issaeva, et al.; Nat. Med. 10, 1321 (2004) Abstract
[4] NMR indicates that the small molecule RITA does not block p53-MDM2 binding in vitro: M. Krajewski, et al.; Nat. Med. 11, 1135 (2005) Abstract
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers)
 
 
ALX-270-263 Revised 03-Apr-08
(-)-Epigallocatechin gallate
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SYNONYMS EGCG
(2R,3R)-2-(3,4,5-Trihydroxyphenyl)-3,4-dihydro-1[2H]-benzopyran-3,5,7-triol 3-(3,4,5-trihydroxybenzoate)
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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ALX-270-263-M010   10 mg 20.00 USD Add To Cart
ALX-270-263-M050   50 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C22H18O11
MW: 458.4
CAS NUMBER: 989-51-5
MERCK INDEX: 14: 3526
SOURCE/HOST: Isolated from green tea.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to yellow powder.
SOLUBILITY: Soluble in 100% ethanol, dimethyl formamide or DMSO; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions in DMSO are stable for up to 3 months when stored at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Keep under inert gas. Protect from light.

Product Description
Antitumor reagent. Antioxidant. Protects cells from lipid peroxidation and DNA damage induced by reactive free radicals. Inhibits inducible nitric oxide synthase (iNOS; NOS II). Chemopreventive anticancer agent. Induces apoptosis in human cancer cell lines. Inhibits MAP kinase mediated signalling pathways. Inhibits angiogenesis. Inhibits telomerase and DNA methyltransferase. Anti-inflammatory agent.
Product Specific Literature References
Inhibitory effect of topical application of a green tea polyphenol fraction on tumor initiation and promotion in mouse skin: M.T. Huang, et al.; Carcinogenesis 13, 947 (1992) Abstract
Inhibition of 12-O-tetradecanoylphorbol-13-acetate and other skin tumor-promoter-caused induction of epidermal interleukin-1 alpha mRNA and protein expression in SENCAR mice by green tea polyphenols: S.K. Katiyar, et al.; J. Invest. Dermatol. 105, 394 (1995) Abstract
Growth inhibition and regression of human prostate and breast tumors in athymic mice by tea epigallocatechin gallate: S. Liao, et al.; Cancer Lett. 96, 239 (1995) Abstract
Inhibition of N-methyl-N'-nitro-N-nitrosoguanidine-induced carcinogenesis by (-)-epigallocatechin gallate in the rat glandular stomach: T. Yamane, et al.; Cancer Res. 55, 2081 (1995) Abstract
(-)-Epigallocatechin gallate, a polyphenolic tea antioxidant, inhibits peroxynitrite-mediated formation of 8-oxodeoxyguanosine and 3-nitrotyrosine: E.S. Fiala, et al.; Experientia 52, 922 (1996) Abstract
Green tea constituent epigallocatechin-3-gallate and induction of apoptosis and cell cycle arrest in human carcinoma cells: N. Ahmad, et al.; J. Natl. Cancer Inst. 89, 1881 (1997) Abstract
Inhibition of inducible nitric oxide synthase gene expression and enzyme activity by epigallocatechin gallate, a natural product from green tea: M.M. Chan, et al.; Biochem. Pharmacol. 54, 1281 (1997) Abstract
(-)-Epigallocatechin-3-gallate blocks the induction of nitric oxide synthase by down-regulating lipopolysaccharide-induced activity of transcription factor nuclear factor-kappaB: Y.L. Lin & J.K. Lin; Mol. Pharmacol. 52, 465 (1997) Abstract
Telomerase inhibition, telomere shortening, and senescence of cancer cells by tea catechins: I. Naasani, et al.; BBRC 249, 391 (1998) Abstract
Epigallocatechin suppression of proliferation of vascular smooth muscle cells: correlation with c-jun and JNK: L.H. Lu, et al.; Br. J. Pharmacol. 124, 1227 (1998) Abstract
ESR study on the structure-antioxidant activity relationship of tea catechins and their epimers: Q. Guo, et al.; Biochim. Biophys. Acta 1427, 13 (1999) Abstract
Pharmacokinetics of the green tea derivative, EGCG, by the topical route of administration in mouse and human skin: K. Dvorakova, et al.; Cancer Chemother. Pharmacol. 43, 331 (1999) Abstract
Polyphenolic antioxidant (-)-epigallocatechin-3-gallate from green tea reduces UVB-induced inflammatory responses and infiltration of leukocytes in human skin: S.K. Katiyar, et al.; Photochem. Photobiol. 69, 148 (1999) Abstract
Antioxidant chemistry of green tea catechins. Identification of products of the reaction of (-)-epigallocatechin gallate with peroxyl radicals: S. Valcic, et al.; Chem. Res. Toxicol. 12, 382 (1999) Abstract
Antimutagenic and anticarcinogenic activity of tea polyphenols: Y. Kuroda & Y. Hara; Mutat. Res. 436, 69 (1999) Abstract
Inhibitory effect of green and black tea on tumor growth: A.H. Conney, et al.; Proc. Soc. Exp. Biol. Med. 220, 229 (1999) Abstract
Green tea epigallocatechin gallate: a natural inhibitor of fatty-acid synthase: X. Wang & W. Tian; BBRC 288, 1200 (2001) Abstract
Epigallocatechin gallate, a constituent of green tea, represses hepatic glucose production: M.E. Waltner-Law, et al.; J. Biol. Chem. 277, 34933 (2002) Abstract; Full Text
The specificities of protein kinase inhibitors: an update:: J. Bain, et al.; Biochem. J. 371, 199 (2003) Abstract; Full Text
Selective inhibition of ADAMTS-1, -4 and -5 by catechin gallate esters: M.N. Vankemmelbeke, et al.; Eur. J. Biochem. 270, 2394 (2003) Abstract
Epigallocatechin-3-gallate, constituent of green tea, suppresses the LPS-induced phenotypic and functional maturation of murine dendritic cells through inhibition of mitogen-activated protein kinases and NF-kappaB: S.C. Ahn, et al.; BBRC 313, 148 (2004) Abstract
Epigallocatechin-3-gallate inhibits epidermal growth factor receptor signaling pathway. Evidence for direct inhibition of ERK1/2 and AKT kinases: J.F. Sah, et al.; J. Biol. Chem. 279, 12755 (2004) Abstract
Inhibition of c-Jun NH2-terminal kinase activity improves ischemia/reperfusion injury in rat lungs: M. Ishii, et al.; J. Immunol. 172, 2569 (2004) Abstract
A constituent of green tea, epigallocatechin-3-gallate, activates endothelial nitric oxide synthase by a phosphatidylinositol-3-OH-kinase-, cAMP-dependent protein kinase-, and Akt-dependent pathway and leads to endothelial-dependent vasorelaxation: M. Lorenz, et al.; J. Biol. Chem. 279, 6190 (2004) Abstract; Full Text
Green tea polyphenols prevent toxin-induced hepatotoxicity in mice by down-regulating inducible nitric oxide-derived prooxidants: J.H. Chen, et al.; Am. J. Clin. Nutr. 80, 742 (2004) Abstract; Full Text
Neuroprotective effects of (-)-epigallocatechin gallate following hypoxia-ischemia-induced brain damage: novel mechanisms of action: B.A. Sutherland, et al.; FASEB J. 19, 258 (2005) Abstract; Full Text
Tea flavanols inhibit angiotensin-converting enzyme activity and increase nitric oxide production in human endothelial cells: I.A. Persson, et al.; J. Pharm. Pharmacol. 58, 1139 (2006) Abstract
General Literature References
Anticarcinogenic effects of (-)-epigallocatechin gallate: H. Fujiki, et al.; Prev. Med. 21, 503 (1992), (Review) Abstract
Absorption, metabolism and antioxidative effects of tea catechin in humans: T. Miyazawa; Biofactors 13, 55 (2000), (Review) Abstract
Inhibition of tumour invasion and angiogenesis by epigallocatechin gallate (EGCG), a major component of green tea: Y.D. Jung and L.M. Ellis; Int. J. Exp. Pathol. 82, 309 (2001), (Review) Abstract
Anti-invasive effects of green tea polyphenol epigallocatechin-3-gallate (EGCG), a natural inhibitor of metallo and serine proteases: R. Benelli, et al.; Biol. Chem. 383, 101 (2002), (Review) Abstract
 
 
ALX-350-236 Revised 04-Sep-08
Homoharringtonine
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Immunomodulators
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ALX-350-236-M001   1 mg 45.00 USD Add To Cart
ALX-350-236-M005   5 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C29H39NO9
MW: 545.6
CAS NUMBER: 26833-87-4
RTECS: FK0260000
SOURCE/HOST: Isolated from Cephalotaxus hainanensis.
PURITY: ≥96%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: VERY TOXIC.

Product Description
Cephalotaxine alkaloid. Inhibits the formation of diphenylalanine and acetylphenylalanyl-puromycin in liver ribosomes. Has promising activity in hematologic malignancies. Lowers the levels of telomerase. Induces apoptosis.
Product Specific Literature References
Different effects of L-histidinol and homoharringtonine on 5- fluorouracil and bis-chloroethylnitrosourea activity in a murine model: R.C. Warrington & W.D. Fang; Anticancer Res. 11, 1879 (1991) Abstract
Selective inhibition of the polypeptide chain elongation in eukaryotic cells: R.M. Tujebajeva, et al.; Biochim. Biophys. Acta 1129, 177 (1992) Abstract
Homoharringtonine is safe and effective for patients with acute myelogenous leukemia: E. Feldman, et al.; Leukemia 6, 1185 (1992) Abstract
Homoharringtonine: history, current research, and future direction: H.M. Kantarjian, et al.; Cancer 92, 1591 (2001), Review Abstract
Homoharringtonine: a new treatment option for myeloid leukemia: C.Y. Luo, et al.; Hematology 9, 259 (2004), Review Abstract
Homoharringtonine-induced apoptosis of human leukemia HL-60 cells is associated with down-regulation of telomerase: W.Z. Xie, et al.; Am. J. Chin. Med. 34, 233 (2006) Abstract
 
 
ALX-350-340 Revised 14-Nov-07
Thielavin B
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products for Inflammation Research
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ALX-350-340-MC05   0.5 mg 390.00 USD Add To Cart
Product Specification
FORMULA: C31H34O10
MW: 566.6
CAS NUMBER: 71950-67-9
SOURCE/HOST: Isolated from an unidentified fungus MST-FP1888.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Fungal metabolite. Glucose-6-phosphatase inhibitor. Potent inhibitor of phospholipase C. Inhibits telomerase, viral reverse transcriptase, peptidoglycan formation and prostaglandin biosynthesis.
Product Specific Literature References
Thielavin A and B, new inhibitors of prostaglandin biosynthesis produced by Thielavia terricola: N. Kitahara, et al.; J. Antibiot. (Tokyo) 34, 1562 (1981) Abstract
The structures of thielavins A, B and C. Prostaglandin synthetase inhibitors from fungi: N. Kitahara, et al.; J. Antibiot. (Tokyo) 36, 599 (1983) Abstract
Screening systems for detecting inhibitors of cell wall transglycosylation in Enterococcus. Cell wall transglycosylation inhibitors in Enterococcus: N. Mani, et al.; J. Antibiot. (Tokyo) 51, 471 (1998) Abstract
Inhibition of telomerase activity by fungus metabolites, CRM646-A and thielavin B: K. Togashi, et al.; Biosci. Biotechnol. Biochem. 65, 651 (2001) Abstract; Full Text
Thielavins as glucose-6-phosphatase (G6Pase) inhibitors: producing strain, fermentation, isolation, structural elucidation and biological activitie: S. Sakemi, et al.; J. Antibiot. (Tokyo) 55, 941 (2002) Abstract
 
 
ALX-380-067 Revised 08-Apr-08
β-Rubromycin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antiviral / Anti-HIV
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ALX-380-067-M001   1 mg 40.00 USD Add To Cart
ALX-380-067-M005   5 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C27H20O12
MW: 536.5
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥99%
SOLUBILITY: Soluble in chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Antibiotic. Inhibitor of HIV-1 reverse transcriptase (RT). Inhibits human telomerase. Cytostatically active against different tumor cell lines.
Product Specific Literature References
The structure of rubromycin: H. Brockmann, et al.; THL 30, 3525 (1966), (Article in German) Abstract
Rubromycin II: H. Brockmann, et al.; Chem. Ber. 102, 126 (1969) Abstract
Rubromycins. 3. The constitution of alpha-rubromycin, beta-rubromycin, gamma-rubromycin, and gamma-iso-rubromycin: H. Brockmann & A. Zeeck; Chem. Ber. 103, 1709 (1970) Abstract
Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: competitive interaction at the template.primer site: M.E. Goldman, et al.; Mol. Pharmacol. 38, 20 (1990) Abstract
Inhibition of human telomerase by rubromycins: implication of spiroketal system of the compounds as an active moiety: T. Ueno, et al.; Biochemistry 39, 5995 (2000) Abstract
Structural and Biosynthetic Investigations of the Rubromycins: C. Puder, et al.; Eur. J. Org. Chem. 2000, 729 (2000)
 
 
ALX-370-002 Revised 19-Sep-06
Dexamethasone
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SYNONYMS 9α-Fluoro-16α-methylprednisolone
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Glucocorticoids & Glucocorticoid Receptors / Related Products
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ALX-370-002-M250   250 mg 22.00 USD Add To Cart
ALX-370-002-G001   1 g 45.00 USD Add To Cart
Product Specification
FORMULA: C22H29FO5
MW: 392.5
CAS NUMBER: 50-02-2
MERCK INDEX: 14: 2943
RTECS: TU3980000
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol. Slightly soluble in acetone or chloroform. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: HARMFUL. MAY BE TERATOGENIC.

Product Description
Inhibits constitutive OPG mRNA steady-state levels in a dose- and time-dependent fashion, promoting osteoclast formation. Glucocorticoid with anti-inflammatory activity. Inhibits the induction of nitric oxide synthases (NOS).
Product Specific Literature References
Inhibition of the induction of nitric oxide synthase by glucocorticoids: yet another explanation for their anti-inflammatory effects?: S. Moncada & R.M.J. Palmer; TIPS 12, 130 (1991), (Review) Abstract
Glucocorticoids inhibit the induction of nitric oxide synthase and the related cell damage in adenocarcinoma cells: K.J. O'Connor & S. Moncada; Biochim. Biophys. Acta 1097, 227 (1991) Abstract
Nitric oxide mediates tumor necrosis factor-alpha cytotoxicity in endothelial cells: C. Estrada, et al.; BBRC 186, 475 (1992) Abstract
Dexamethasone inhibits the expression of an inducible nitric oxide synthase in infarcted rabbit myocardium: R.R. Dudek, et al.; BBRC 202, 1120 (1994) Abstract
Induction of the alkyltransferase (MGMT) gene by DNA damaging agents and the glucocorticoid dexamethasone and comparison with the response of base excision repair genes: T. Grombacher, et al.; Carcinogenesis 17, 2329 (1996) Abstract
Activation of human O6-methylguanine-DNA methyltransferase gene by glucocorticoid hormone: T. Biswas, et al.; Oncogene 18, 525 (1999) Abstract
Dexamethasone-induced thymocyte apoptosis: apoptotic signal involves the sequential activation of phosphoinositide-specific phospholipase C, acidic sphingomyelinase, and caspases: M.G. Cifone, et al.; Blood 93, 2282 (1999) Abstract; Full Text
Dexamethasone induces apoptosis in human T cell clones expressing low levels of Bcl-2: M.S. Montani, et al.; Cell Death Differ 6, 79 (1999) Abstract
Dexamethasone inhibits the phosphorylation of retinoblastoma protein in the suppression of human vascular smooth muscle cell proliferation: T.D. Reil, et al.; J. Surg. Res. 92, 108 (2000) Abstract
Dexamethasone suppresses iNOS gene expression by inhibiting NF-kappaB in vascular smooth muscle cells: M. Matsumura, et al.; Life Sci. 69, 1067 (2001) Abstract
Dexamethasone inhibits inducible nitric-oxide synthase expression and nitric oxide production by destabilizing mRNA in lipopolysaccharide-treated macrophages: R. Korhonen, et al.; Mol. Pharmacol. 62, 698 (2002) Abstract; Full Text
Molecular mechanisms underlying dexamethasone inhibition of iNOS expression and activity in C6 glioma cells: J. Shinoda, et al.; Glia 42, 68 (2003) Abstract
Dexamethasone prevents granulocyte-macrophage colony-stimulating factor-induced nuclear factor-kappaB activation, inducible nitric oxide synthase expression and nitric oxide production in a skin dendritic cell line: A.L. Vital, et al.; Mediators Inflamm. 12, 71 (2003) Abstract
Dexamethasone suppresses eNOS and CAT-1 and induces oxidative stress in mouse resistance arterioles: S.C. Schafer, et al.; Am. J. Physiol. Heart Circ. Physiol. 288, H436 (2005) Abstract; Full Text
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ALX-105-011 Revised 18-Sep-06
S-Trityl-L-cysteine
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SYNONYMS NSC 83265
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY Cell Cycle Blockers & Inhibitors / Related Products
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ALX-105-011-M100   100 mg 20.00 USD Add To Cart
ALX-105-011-M500   500 mg 60.00 USD