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ALX-270-233
Revised 10-Jan-07
PP2
SYNONYMS
4-Amino-5-(4-chlorophenyl)-7-(
t
-butyl)pyrazolo[3,4-d]pyrimidine
AG 1879
PRODUCT LINE
Immunology
PRODUCT CATEGORY
Kinases in T Cell Signal Transduction / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
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ALX-270-233-M001
1 mg
66.00 USD
ALX-270-233-M005
5 mg
265.00 USD
Product Specification
FORMULA:
C
15
H
16
ClN
5
MW:
301.8
PURITY:
≥97% (HPLC)
APPEARANCE:
White to off-white solid
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Potent inhibitor of the oncogenic RET kinase (IC
50
=100nM) and of the Src family of protein tyrosine kinases. Selectively inhibits p56
Ick
, p59
fyn
T
and Hck compared to other tyrosine kinases such as EGF-R, JAK2 or ZAP-70. Potent inhibitor of anti-CD3-stimulated tyrosine phosphorylation of human T cells and subsequent IL-2 gene activation.
Product Specific Literature References
Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation
:
J.H. Janke, et al.; J. Biol. Chem.
271
, 695 (1996)
Abstract
;
Full Text
Efficient inhibition of RET/papillary thyroid carcinoma oncogenic kinases by 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine (PP2)
:
F. Carlomagno, et al.; J. Clin. Endocrinol. Metab.
88
, 1897 (2003)
Abstract
;
Full Text
Further Categories Containing This Product:
Src Family Kinases / Related Products
•
Tyrosine Kinase Inhibitors
ALX-270-244
Revised 03-Apr-08
Caffeic acid phenylethyl ester
SYNONYMS
CAPE
Phenethyl caffeiate
Caffeic acid phenethyl ester
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Natural Products - Anti-inflammatory Agents
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-244-M010
10 mg
20.00 USD
ALX-270-244-M050
50 mg
60.00 USD
Product Specification
FORMULA:
C
17
H
16
O
4
MW:
284.3
CAS NUMBER:
115610-29-2
SOURCE/HOST:
Synthetic.
PURITY:
≥97% (HPLC)
APPEARANCE:
White to off-white crystalline solid.
SOLUBILITY:
Soluble in DMSO, 100% ethanol, methanol, acetone or acetonitrile; insoluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stable for at least one year after receipt when stored at –20°C.
HANDLING:
Protect from light and moisture.
HAZARD:
IRRITANT.
Product Description
Active component of propolis from honeybee hives, known to have anti-mitogenic, anti-carcinogenic, anti-inflammatory, and immunomodulatory properties. Potent and specific inhibitor of NF-κB activation, induced by TNF-α
(Prod. No.
ALX-522-008
(human) or Prod. No.
ALX-522-009
(mouse)), PMA (Prod. No.
ALX-445-004
) and other inflammatory agents. Exhibits inhibitory activity against HIV-1 integrase (IC
50
=7µM). Suppresses lipid peroxidation and inhibits ornithine decarboxylase, protein tyrosine kinase and lipoxygenase activities. Induces apoptosis.
Product Specific Literature References
Hydroxylated aromatic inhibitors of HIV-1 integrase:
T.R. Burke Jr., et al.; J. Med. Chem.
38
, 4171 (1995)
Abstract
Apoptosis and altered redox state induced by caffeic acid phenethyl ester (CAPE) in transformed rat fibroblast cells:
C. Chiao, et al.; Cancer Res.
55
, 3576 (1995)
Abstract
Caffeic acid phenethyl ester is a potent and specific inhibitor of activation of nuclear transcription factor NF-kappa B:
K. Natarajan, et al.; PNAS
93
, 9090 (1996)
Abstract
Inhibitory effects of caffeic acid phenethyl ester on the activity and expression of cyclooxygenase-2 in human oral epithelial cells and in a rat model of inflammation:
P. Michaluart, et al.; Cancer Res.
59
, 2347 (1999)
Abstract
Caffeic acid phenethyl ester induces leukocyte apoptosis, modulates nuclear factor-kappa B and suppresses acute inflammation:
Z. Orban, et al.; Neuroimmunomodulation
7
, 99 (2000)
Abstract
Caffeic acid phenethyl ester inhibits T-cell activation by targeting both nuclear factor of activated T-cells and NF-kappaB transcription factors:
N. Marquez, et al.; J. Pharmacol. Exp. Ther.
308
, 993 (2004)
Abstract
Caffeic acid derivatives: in vitro and in vivo anti-inflammatory properties:
F.M. da Cunha, et al.; Free Radic. Res.
38
, 1241 (2004)
Abstract
Drastic effect of several caffeic acid derivatives on the induction of heme oxygenase-1 expression revealed by quantitative real-time RT-PCR:
K. Suzuki, et al.; Biofactors
28
, 151 (2006)
Abstract
Related Products
ALX-270-231
Caffeic acid
ALX-270-480
Caffeic acid ethyl ester
Further Categories Containing This Product:
Natural Products - Chemopreventive Agents
•
Natural Products - NF-kB Pathway Inhibitors
•
Tyrosine Kinase Inhibitors
•
Natural Products - Protein Kinase Inhibitors
•
Natural Products - Immunomodulators
•
Natural Products - Antiviral / anti-HIV Agents
•
Natural Products - Apoptosis Inducers & Inhibitors
•
Phenolic Acids
•
NF-kB Pathway Inhibitors
•
HIV / AIDS / Related Products
ALX-270-281
Revised 28-Sep-06
Daphnetin
SYNONYMS
7,8-Dihydroxycoumarin
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
EGFR Kinase Inhibitors
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ALX-270-281-M005
5 mg
25.00 USD
ALX-270-281-M025
25 mg
95.00 USD
Product Specification
FORMULA:
C
9
H
6
O
4
MW:
178.1
CAS NUMBER:
486-35-1
RTECS:
GN6382600
PURITY:
≥97%
APPEARANCE:
White to rose powder.
SOLUBILITY:
Soluble in 100% ethanol, methanol or dimethyl formamide.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+20°C
Product Description
Inhibitor of protein kinases. EGF receptor tyrosine kinase (IC
50
=7.87µM), PKA (IC
50
=9.33µM), PKC (IC
50
=25.01µM). Antioxidant. Antimalarial agent.
Product Specific Literature References
Daphnetin: a novel antimalarial agent with in vitro and in vivo activity:
Y.Z. Yang, et al.; Am. J. Trop. Med. Hyg.
46
, 15 (1992)
Abstract
Daphnetin, one of coumarin derivatives, is a protein kinase inhibitor:
E.B. Yang, et al.; BBRC
260
, 682 (1999)
Abstract
Further Categories Containing This Product:
Antioxidants, Flavonoids & Free Radical Scavengers Other Products
•
PKA Inhibitors
•
Malaria / Related Products
•
Tyrosine Kinase Inhibitors
ALX-270-313
Revised 03-Mar-05
BPIQ-I
SYNONYMS
8-[(3-Bromophenyl)amino]-3-methyl-3
H
-imidazo[4,5-γ]-quinazoline
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
EGFR Kinase Inhibitors
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Product Numbers:
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ALX-270-313-M001
1 mg
140.00 USD
Product Specification
FORMULA:
C
16
H
12
BrN
5
MW:
354.2
PURITY:
≥95%
APPEARANCE:
Off white to yellow solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Keep under inert gas.
Product Description
Potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC
50
=25 pM).
Product Specific Literature References
Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor:
G.W. Rewcastle, et al.; J. Med. Chem.
39
, 918 (1996)
Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
ALX-270-316
Revised 12-Jan-07
Compound 56
SYNONYMS
4-[(3-Bromophenyl)amino]-6,7-diethoxyquinazoline
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
EGFR Kinase Inhibitors
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ALX-270-316-C500
500 µg
135.00 USD
Product Specification
FORMULA:
C
18
H
18
BrN
3
O
2
MW:
388.3
PURITY:
≥97% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
HAZARD:
MAY BE MUTAGENIC. HARMFUL.
Product Description
Potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC
50
=6pM).
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
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
ALX-270-319
Revised 04-Mar-05
PD 156,273
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
Product Specification
FORMULA:
C
15
H
14
BrN
5
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) (IC
50
=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 04-Mar-05
PD 168,393
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
Product Specification
FORMULA:
C
17
H
13
BrN
4
O
MW:
369.2
PURITY:
≥95%
APPEARANCE:
Yellow to orange solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Keep under inert gas.
Product Description
Potent, cell permeable, irreversible, and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC
50
=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 Inhibitors
•
Antitumor Agents (Enzyme Inhibitors)
ALX-270-323
Revised 04-Mar-05
PD 174,265
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
Product Specification
FORMULA:
C
17
H
15
BrN
4
O
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 (IC
50
=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-270-330
Revised 14-Jul-05
SU 4984
SYNONYMS
3[4-(1-Formylpiperazin-4-yl)benzylidenyl]-2-indolinone
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Tyrosine Kinase Inhibitors
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ALX-270-330-M001
1 mg
120.00 USD
Product Specification
FORMULA:
C
20
H
19
N
3
O
2
MW:
333.4
PURITY:
≥98%
APPEARANCE:
Orange to red crystalline solid.
SOLUBILITY:
Soluble in DMSO or acetone.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Inhibitor of tyrosine kinase activity of fibroblast growth factor receptor 1 (FGFR1). Inhibits αFGF-induced tyrosine phosphorylation of ERK1 and ERK2 (IC
50
=20-4µM) and the tyrosine phosphorylation of the PDGF receptor and the insulin receptor. Does not inhibit the kinase activity of the EGF receptor.
Product Specific Literature References
Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors
:
M. Mohammadi, et al.; Science
276
, 955 (1997)
Abstract
ALX-270-338
Revised 03-Mar-05
BPIQ-II
SYNONYMS
8-[(3-Bromophenyl)amino]-1
H
-imidazo[4,5-γ]-quinazoline
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
EGFR Kinase Inhibitors
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ALX-270-338-M001
1 mg
140.00 USD
Product Specification
FORMULA:
C
15
H
10
BrN
5
MW:
340.2
PURITY:
≥98%
APPEARANCE:
Pale pink solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Keep under inert gas.
Product Description
Potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC
50
=8pM).
Product Specific Literature References
Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor
:
G.W. Rewcastle, et al.; J. Med. Chem.
39
, 918 (1996)
Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors
ALX-270-342
Revised 06-Dec-04
MAZ51
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
