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Tyrosine Kinase Inhibitors
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ALX-350-037 Revised 04-Feb-05
Lavendustin B
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-037-M001   1 mg 80.00 USD Add To Cart
Product Specification
FORMULA: C21H19NO5
MW: 365.4
CAS NUMBER: 125697-91-8
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in methanol, DMSO and dilute aqueous base.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Control for lavendustin A (Prod. No. ALX-350-007); 100-fold less potent than lavendustin A.
Product Specific Literature References
Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus: T. Onoda, et al.; J. Nat. Prod. 52, 1252 (1989) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-270-066 Revised 07-Apr-08
Lavendustin C
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SYNONYMS Compound 5
5-(N-2,5-Dihydroxybenzyl)aminosalicylic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-270-066-M001   1 mg 35.00 USD Add To Cart
Product Specification
FORMULA: C14H13NO5
MW: 275.3
SOURCE/HOST: Synthetic.
PURITY: ≥97%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Potent inhibitor of protein tyrosine kinases and Ca2+/calmodulin-dependent kinase II. Acts also as an inhibitor of EGFR tyrosine kinase and pp60c-src kinase.
Product Specific Literature References
Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus: T. Onoda, et al.; J. Nat. Prod. 52, 1252 (1989) Abstract
Long-term potentiation in the hippocampus is blocked by tyrosine kinase inhibitors: T.J. O'Dell, et al.; Nature 353, 558 (1991) Abstract
Hypericin and pseudohypericin specifically inhibit protein kinase C: possible relation to their antiretroviral activity: I. Takahashi, et al.; BBRC 165, 1207 (1989) Abstract
Inhibition of crystal-induced neutrophil activation by a protein tyrosine kinase inhibitor: H.M. Burt, et al.; J. Leukoc. Biol. 55, 112 (1994) Abstract
Endotoxin increases intercellular resistance in microvascular endothelial cells by a tyrosine kinase pathway: D. Lidington, et al.; J. Cell Physiol. 185, 117 (2000) Abstract
 
 
ALX-350-084 Revised 07-Apr-08
Lavendustin C methyl ester
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SYNONYMS Compound 5 methyl ester
5-Amino-N-(2,5-dihydroxybenzyl)methyl salicylate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-084-M001   1 mg 50.00 USD Add To Cart
ALX-350-084-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C15H15NO5
MW: 289.3
SOURCE/HOST: Synthetic.
PURITY: ≥97%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Inhibitor of EGFR tyrosine kinase with improved bioavailability over lavendustin C (Prod. No. ALX-270-066).
Product Specific Literature References
Synthesis and structure-activity studies of a series of [(hydroxybenzyl)amino]salicylates as inhibitors of EGF receptor- associated tyrosine kinase activity: H. Chen, et al.; J. Med. Chem. 36, 4094 (1993) Abstract
Structure-activity relationships in a series of 5-[(2,5- dihydroxybenzyl)amino]salicylate inhibitors of EGF-receptor-associated tyrosine kinase: importance of additional hydrophobic aromatic interactions: H. Chen, et al.; J. Med. Chem. 37, 845 (1994) Abstract
Related Products
Further Categories Containing This Product:
Tyrosine Kinase InhibitorsEGFR Kinase Inhibitors
 
 
ALX-430-095 Revised 23-Jan-08
Leflunomide
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SYNONYMS HWA486
5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide)
N-(4-Trifluoromethylphenyl)-5-methylisoxazol-4-carboxamide
PRODUCT LINE Immunology
PRODUCT CATEGORY Immunomodulators Other Products
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ALX-430-095-M010   10 mg 15.00 USD Add To Cart
ALX-430-095-M050   50 mg 40.00 USD Add To Cart
ALX-430-095-G001   1 g 380.00 USD Add To Cart
Product Specification
FORMULA: C12H9F3N2O2
MW: 270.2
CAS NUMBER: 75706-12-6
MERCK INDEX: 14: 5432
RTECS: NY2354200
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep under inert gas. Protect from light.
HAZARD: HARMFUL.

Product Description
Immunosuppressive drug that inhibits T and B cell responses in vivo. Inhibitor of tyrosine phosphorylation (tyrosine kinase inhibitor), of dihydroorotate dehydrogenase, an enzyme for de novo pyrimidine synthesis, of TNF-dependent NF-κB activation, and of COX-2. The physiological activity of leflunomide is attributed mainly to its metabolite A77 1726 (Prod. No. ALX-430-096).
Product Specific Literature References
Immunopharmacological profile of a novel isoxazol derivative, HWA 486, with potential antirheumatic activity-I. Disease modifying action on adjuvant arthritis of the rat: R.R. Bartlett & R. Schleyerbach; Int. J. Immunopharmacol. 7, 7 (1985) Abstract
Leflunomide (HWA 486), a novel immunomodulating compound for the treatment of autoimmune disorders and reactions leading to transplantation rejection: R.R. Bartlett, et al.; Agents Actions 32, 10 (1991) Abstract
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993) Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995) Abstract; Full Text
Molecular mechanisms of action of new xenobiotic immunosuppressive drugs: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide: T.R. Brazelton & R.E. Morris; Curr. Opin. Immunol. 8, 710 (1996) Abstract
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract
Regulation of B cell function by the immunosuppressive agent leflunomide: K.F. Siemasko, et al.; Transplantation 61, 635 (1996) Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996) Abstract
Potencies of leflunomide and HR325 as inhibitors of prostaglandin endoperoxide H synthase-1 and -2: comparison with nonsteroidal anti- inflammatory drugs: A.P. Curnock, et al.; J. Pharmacol. Exp. Ther. 282, 339 (1997) Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997) Abstract
Leflunomide, a novel immunomodulating agent, prevents the development of allergic sensitization in an animal model of allergic asthma: E. Eber, et al.; Clin. Exp. Allergy 28, 376 (1998) Abstract
Species-related inhibition of human and rat dihydroorotate dehydrogenase by immunosuppressive isoxazol and cinchoninic acid derivatives: W. Knecht & M. Löffler; Biochem. Pharmacol. 56, 1259 (1998) Abstract
Inhibition of JAK3 and STAT6 tyrosine phosphorylation by the immunosuppressive drug leflunomide leads to a block in IgG1 production: K.F. Siemasko, et al.; J. Immunol. 160, 1581 (1998) Abstract
In vivo activity of leflunomide: pharmacokinetic analyses and mechanism of immunosuppression: A.S. Chong, et al.; Transplantation 68, 100 (1999) Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF- dependent nuclear factor-kappa B activation and gene expression: S.K. Manna and B.B. Aggarwal; J. Immunol. 162, 2095 (1999) Abstract
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate- sensitive manner: L.C. Hamilton, et al.; Br. J. Pharmacol. 127, 1589 (1999) Abstract
Leflunomide: mode of action in the treatment of rheumatoid arthritis: F.C. Breedveld & J.M. Dayer; Ann. Rheum. Dis. 59, 841 (2000) Abstract
General Literature References
Leflunomide, a novel immunomodulator for the treatment of active rheumatoid arthritis: M.M. Goldenberg; Clin. Ther. 21, 1837 (1999), (Review) Abstract
Leflunomide, mycophenolic acid and matrix metalloproteinase inhibitors: D.E. Furst; Rheumatology (Oxford) 38 Suppl 2, 14 (1999), (Review) Abstract
Leflunomide and methotrexate: R.F. Laan, et al.; Curr. Opin. Rheumatol. 13, 159 (2001), (Review) Abstract
Experiences with leflunomide in solid organ transplantation: J.W. Williams, et al.; Transplantation 73, 358 (2002), (Review) Abstract
Further Categories Containing This Product:
NF-kB Pathway InhibitorsCOX InhibitorsTyrosine Kinase Inhibitors
 
 
ALX-270-342 Revised 06-Dec-04
MAZ51
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SYNONYMS 3-(4-Dimethylamino-naphthalen-1-yl-methylene)-1,3-dihydro-indol-2-one
PRODUCT LINE Chemokines & Cytokines
PRODUCT CATEGORY VEGFs & VEGF-Rs Other Products
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ALX-270-342-M002   2 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C21H18N2O
MW: 314.4
CAS NUMBER: 163655-37-6
PURITY: ≥98%
APPEARANCE: Orange crystals.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep under inert gas. Protect from light.
HAZARD: TOXIC.

Product Description
Inhibits vascular endothelial cell growth factor-C (VEGF-C)-induced intracellular phosphorylation of VEGFR-3 (Flt-4) (IC50=1µM).
Product Specific Literature References
Characterization of indolinones which preferentially inhibit VEGF-C- and VEGF-D-induced activation of VEGFR-3 rather than VEGFR-2: V. Kirkin, et al.; Eur. J. Biochem. 268, 5530 (2001) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-270-088 Revised 07-Apr-05
ML-7 . hydrochloride
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SYNONYMS 1-(5-Iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-270-088-M005   5 mg 40.00 USD Add To Cart
ALX-270-088-M025   25 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C15H17IN2O2S . HCl
MW: 416.0 . 36.5
CAS NUMBER: 110448-33-4
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (can be further diluted with water), 100% ethanol (warm) or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibits smooth-muscle myosin light chain kinase, protein kinase C (PKC), and cAMP-dependent protein kinase (PKA).
Product Specific Literature References
Selective inhibition of catalytic activity of smooth muscle myosin light chain kinase: M. Saitoh, et al.; J. Biol. Chem. 262, 7796 (1987) Abstract; Full Text
Further Categories Containing This Product:
PKC InhibitorsPKA InhibitorsMyosin Light Chain Kinase Inhibitors
 
 
ALX-270-319 Revised 04-Mar-05
PD 156,273
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SYNONYMS 6-Amino-4-[(3-bromophenyl)amino]-7-(methylamino)quinazoline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-319-M001   1 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C15H14BrN5
MW: 344.2
PURITY: ≥98%
APPEARANCE: Off white to yellow powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Protect from light.

Product Description
Potent inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC50=690pM). Inhibits the growth of primary human tumor cell cultures.
Product Specific Literature References
Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor: A.J. Bridges, et al.; J. Med. Chem. 39, 267 (1996) Abstract; Full Text
Inhibition of growth of primary human tumour cell cultures by a 4-anilinoquinazoline inhibitor of the epidermal growth factor receptor family of tyrosine kinases: B.C. Baguley, et al.; Eur. J. Cancer 34, 1086 (1998) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-270-322 Revised 27-Nov-08
PD 168,393
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SYNONYMS 4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-322-M001   1 mg 156.00 USD Add To Cart
Product Specification
FORMULA: C17H13BrN4O
MW: 369.2
PURITY: ≥95%
APPEARANCE: Yellow to orange solid.
SOLUBILITY: Soluble in DMSO (200 mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Protect from light.

Product Description
Potent, cell permeable, irreversible, and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50=700pM). Antitumor agent in vivo.
Product Specific Literature References
Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor: D.W. Fry, et al.; PNAS 95, 12022 (1998) Abstract; Full Text
Further Categories Containing This Product:
Tyrosine Kinase InhibitorsAntitumor Agents (Enzyme Inhibitors)
 
 
ALX-270-323 Revised 04-Mar-05
PD 174,265
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SYNONYMS 4-[(3-Bromophenyl)amino]-6-propionylamidoquinazoline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY EGFR Kinase Inhibitors
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ALX-270-323-M001   1 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C17H15BrN4O
MW: 371.2
PURITY: ≥98%
APPEARANCE: Off white to yellow powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Protect from light.

Product Description
Potent, cell permeable, reversible, and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50=450pM).
Product Specific Literature References
Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor: D.W. Fry, et al.; PNAS 95, 12022 (1998) Abstract; Full Text
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
 
 
ALX-270-202 Revised 07-Oct-08
Piceatannol
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SYNONYMS 3,4,3',5'-Tetrahydroxy-trans-stilbene
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-270-202-M001   1 mg 22.00 USD Add To Cart
ALX-270-202-M005   5 mg 62.00 USD Add To Cart
ALX-270-202-M010   10 mg 105.00 USD Add To Cart
ALX-270-202-M050   50 mg 375.00 USD Add To Cart
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