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Antitumor Agents (Enzyme Inhibitors)
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ALX-300-006 Revised 03-Jul-06
1-O-Octadecyl-2-O-methyl-rac-glycero-3-phosphocholine
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SYNONYMS rac-ET-18-OCH3
Edelfosine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phospholipids / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-300-006-M050   50 mg 45.00 USD Add To Cart
ALX-300-006-M250   250 mg 180.00 USD Add To Cart
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
 
 
ALX-300-093 Revised 23-Mar-05
Hexadecyl-phosphocholine (C16:0)
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SYNONYMS Miltefosine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phospholipids / Related Products
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ALX-300-093-M250   250 mg 50.00 USD Add To Cart
ALX-300-093-G001   1 g 150.00 USD Add To Cart
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:
PKC InhibitorsParasitic Diseases Other ProductsAntitumor Agents (Enzyme Inhibitors)
 
 
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
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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
 
 
ALX-350-006 Revised 05-Apr-08
Genistein (synthetic)
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SYNONYMS 4',5,7-Trihydroxyisoflavone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-006-M010   10 mg 25.00 USD Add To Cart
ALX-350-006-M025   25 mg 50.00 USD Add To Cart
ALX-350-006-M050   50 mg 90.00 USD Add To Cart
ALX-350-006-M100   100 mg 150.00 USD Add To Cart
ALX-350-006-G001   1 g 480.00 USD Add To Cart
Product Specification
FORMULA: C15H10O5
MW: 270.2
CAS NUMBER: 446-72-0
MERCK INDEX: 14: 4391
RTECS: NR2392000
SOURCE/HOST: Synthetic.
PURITY: ≥99% (HPLC)
APPEARANCE: White to yellow crystalline powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Tyrosine protein kinase inhibitor. Inhibits phosphorylation of EGFR kinase. Inhibits tumor cell proliferation and induces tumor cell differentiation. Inhibits topoisomerase II activity in vivo. Produces cell cycle arrest and apoptosis. Direct inhibitor of insulin-induced glucose uptake in adipocytes (IC50=20µM).
Product Specific Literature References
Genistein, a specific inhibitor of tyrosine-specific protein kinases: T. Akiyama, et al.; J. Biol. Chem. 262, 5592 (1987) Abstract; Full Text
Erbstatin blocks platelet activating factor-induced protein-tyrosine phosphorylation, polyphosphoinositide hydrolysis, protein kinase C activation, serotonin secretion and aggregation of rabbit platelets: H. Salari, et al.; FEBS Lett. 263, 104 (1990) Abstract
Mechanisms of cancer chemoprevention by soy isoflavone genistein: F.H. Sarkar & Y. Li; Cancer Metastasis Rev. 21, 265 (2002) Abstract
Soy isoflavone phyto-pharmaceuticals in interleukin-6 affections. Multi-purpose nutraceuticals at the crossroad of hormone replacement, anti-cancer and anti-inflammatory therapy: N. Dijsselbloem, et al.; Biochem. Pharmacol. 68, 1171 (2004), Review Abstract
Genistein affects testosterone secretion by Leydig cells in roosters (Gallus gallus domesticus): M. Opalka, et al.; Reprod. Biol. 4, 185 (2004) Abstract
Genistein directly inhibits GLUT4-mediated glucose uptake in 3T3-L1 adipocytes: M. Bazuine, et al.; BBRC 325, 511 (2005) Abstract
Decreased circulating levels of tumor necrosis factor-alpha in postmenopausal women during consumption of soy-containing isoflavones: Y. Huang, et al.; J. Clin. Endocrinol. Metab. 90, 3956 (2005) Abstract
Phytoestrogens and lipoproteins in women: C.N. Bairey Merz, et al.; J. Clin. Endocrinol. Metab. 91, 2209 (2006) Abstract
Clinical review: a critical evaluation of the role of soy protein and isoflavone supplementation in the control of plasma cholesterol concentrations: A. Dewell, et al.; J. Clin. Endocrinol. Metab. 91, 772 (2006), Review Abstract
The role of genistein and synthetic derivatives of isoflavone in cancer prevention and therapy: F.H. Sarkar, et al.; Mini Rev. Med. Chem. 6, 401 (2006), Review Abstract
 
 
ALX-350-015 Revised 02-Dec-08
(S)-(+)-Camptothecin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Topoisomerase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-015-M050   50 mg 40.00 USD Add To Cart
ALX-350-015-M250   250 mg 150.00 USD Add To Cart
ALX-350-015-G001   1 g 295.00 USD Add To Cart
Product Specification
FORMULA: C20H16N2O4
MW: 348.4
CAS NUMBER: 7689-03-4
MERCK INDEX: 14: 1735
RTECS: UQ0492000
SOURCE/HOST: Isolated from Mappia foetida Miers (Nothapodytes foetida (Wt.) Sleumer).
PURITY: ≥98% (HPLC)
APPEARANCE: Pale yellow powder.
SOLUBILITY: Soluble in DMSO (10mg/ml), methanol (40mg/ml), 0.1N sodium hydroxide (50mg/ml) or acetic acid; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and moisture. After reconstitution, prepare aliquots and store at -20°C.
HAZARD: TOXIC.

Product Description
Potent antitumor agent. Inhibitor of DNA-topoisomerase I. Activates p53 resulting in upregulated expression of TRAIL-R2 (DR5) and Bak to overcome TRAIL resistance in Bax-deficient human colon carcinoma cells. Suppresses nitric oxide (NO) biosynthesis.
Product Specific Literature References
M.E. Wall, et al.; JACS 88, 3888 (1966)
The current status of camptothecin analogues as antitumor agents: W.J. Slichenmyer, et al.; J. Natl. Cancer Inst. 85, 271 (1993), (Review) Abstract
RNA synthesis inhibitors increase melatonin production in Y79 human retinoblastoma cells: J.L. Janavs, et al.; Mol. Brain Res. 23, 47 (1994) Abstract
Camptothecins: from bench research to hospital wards: M. Potmesil; Cancer Res. 54, 1431 (1994), (Review) Abstract
Forskolin and camptothecin induce a 30 kDa protein associated with melatonin production in Y79 human retinoblastoma cells: J.L. Janavs, et al.; J. Neurosci. 15, 298 (1995) Abstract
Differential stabilization of eukaryotic DNA topoisomerase I cleavable complexes by camptothecin derivatives: A. Tanizawa, et al.; Biochemistry 34, 7200 (1995) Abstract
The anti-cancer drug camptothecin inhibits elongation but stimulates initiation of RNA polymerase II transcription: M. Ljungman & P.C. Hanawalt; Carcinogenesis 17, 31 (1996) Abstract
The cell cycle effects of camptothecin: Z. Darzynkiewicz, et al.; Ann. N. Y. Acad. Sci. 803, 93 (1996) Abstract
Camptothecin-induced apoptosis in p53-null human leukemia HL60 cells and their isolated nuclei: effects of the protease inhibitors Z-VAD-fmk and dichloroisocoumarin suggest an involvement of both caspases and serine proteases: T. Shimizu & Y. Pommier; Leukemia 11, 1238 (1997) Abstract
Camptothecin and taxol: discovery to clinic: M.E. Wall; Med. Res. Rev. 18, 299 (1998), Review Abstract
Camptothecin suppresses nitric oxide biosynthesis in RAW 264.7 macrophages: W.F. Chiou, et al.; Life Sci. 69, 625 (2001) Abstract
Reversal of multidrug resistance-associated protein-mediated daunorubicin resistance by camptothecin: D. Chauvier, et al.; J. Pharm. Sci. 91, 1765 (2002) Abstract
Camptothecin and taxol: historic achievements in natural products research: N.H. Oberlies & D.J. Kroll; J. Nat. Prod. 67, 129 (2004), Review Abstract
Camptothecin and its analogues: a review on their chemotherapeutic potential: D. Sriram, et al.; Nat. Prod. Res. 19, 393 (2005), Review Abstract
The effects of camptothecin on RNA polymerase II transcription: roles of DNA topoisomerase I:: G. Capranico, et al.; Biochimie 89, 482 (2007) Abstract
Related Products
 
 
ALX-350-086 Revised 08-Apr-08
Nordihydroguaiaretic acid
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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
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ALX-350-086-G001   1 g 62.00 USD Add To Cart
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
 
 
ALX-350-118 Revised 22-Sep-08
Deguelin
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SYNONYMS [-]-Deguelin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-118-M005   5 mg 60.00 USD Add To Cart
ALX-350-118-M025   25 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C23H22O6
MW: 394.4
CAS NUMBER: 522-17-8
MERCK INDEX: 14: 2863
RTECS: DX1500000
PURITY: ≥95%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in acetone, acetonitrile or DMSO. Slightly soluble in 100% ethanol. Insoluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Inhibitor of Akt (protein kinase B; PKB) in an in vitro lung carcinogenesis progression model. Inhibits cell proliferation - cells accumulate in the G2-M phase of the cell cycle. Induces apoptosis. Exhibits a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. Inhibits cyclooxygenase-2 (COX-2) expression.
Product Specific Literature References
Deguelin inhibits the growth of colon cancer cells through the induction of apoptosis and cell cycle arrest: G. Murillo, et al.; Eur. J. Cancer 38, 2446 (2002) Abstract
Effects of deguelin on the phosphatidylinositol 3-kinase/Akt pathway and apoptosis in premalignant human bronchial epithelial cells: K.H. Chun, et al.; J. Natl. Cancer Inst. 95, 291 (2003) Abstract; Full Text
Cancer Chemopreventive Activity of Rotenoids from Derris trifoliata: C. Ito, et al.; Planta Med. 70, 8 (2004) Abstract
Apoptosis induction by the natural product cancer chemopreventive agent deguelin is mediated through the inhibition of mitochondrial bioenergetics.: N. Hail, et al.; Apoptosis 9, 437 (2004) Abstract
Deguelin-induced inhibition of cyclooxygenase-2 expression in human bronchial epithelial cells: H.Y. Lee, et al.; Clin. Cancer Res. 10, 1074 (2004) Abstract
 
 
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
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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: