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ALX-380-091
Revised 21-Aug-08
17-AAG
SYNONYMS
17-(Allylamino)-17-desmethoxygeldanamycin
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antitumor Antibiotics
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ALX-380-091-C100
100 µg
65.00 USD
ALX-380-091-M001
1 mg
162.00 USD
Product Specification
FORMULA:
C
31
H
43
N
3
O
8
MW:
585.7
CAS NUMBER:
75747-14-7
SOURCE/HOST:
Semisynthetic derivative from geldanamycin.
PURITY:
≥97%
APPEARANCE:
Red to dark red powder.
SOLUBILITY:
Soluble in DMSO (10mg/ml) or methanol (10mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Description
Potent, less toxic derivative of geldanamycin (Prod. No.
ALX-380-054
). Inhibits the essential ATPase activity of HSP90. Inhibitor of telomerase activity. Inducer of apoptosis with antitumor activity.
Product Specific Literature References
Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives:
R.C. Schnur, et al.; J. Med. Chem.
38
, 3806 (1995)
Abstract
The benzoquinone ansamycin 17-allylamino-17-demethoxygeldanamycin binds to HSP90 and shares important biologic activities with geldanamycin:
T.W. Schulte & L.M. Neckers; Cancer Chemother. Pharmacol.
42
, 273 (1998)
Abstract
Gene expression profiling of human colon cancer cells following inhibition of signal transduction by 17-allylamino-17-demethoxygeldanamycin, an inhibitor of the hsp90 molecular chaperone:
P.A. Clarke, et al.; Oncogene
19
, 4125 (2000)
Abstract
Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts:
R. Nimmanapalli, et al.; Cancer Res.
61
, 1799 (2001)
Abstract
;
Full Text
Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells:
P.N. Munster, et al.; Cancer Res.
61
, 2945 (2001)
Abstract
;
Full Text
Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin:
J. Yang, et al.; Cancer Res.
61
, 4010 (2001)
Abstract
;
Full Text
Enhancement of paclitaxel-mediated cytotoxicity in lung cancer cells by 17-allylamino geldanamycin: in vitro and in vivo analysis:
D.M. Nguyen, et al.; Ann. Thorac. Surg.
72
, 371 (2001)
Abstract
ErbB2 degradation mediated by the co-chaperone protein CHIP:
P. Zhou, et al.; J. Biol. Chem.
278
, 13829 (2003)
Abstract
Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells:
R. Villa, et al.; Carcinogenesis
24
, 851 (2003)
Abstract
Geldanamycin and its 17-allylamino-17-demethoxy analogue antagonize the action of Cisplatin in human colon adenocarcinoma cells: differential caspase activation as a basis for interaction:
I.A. Vasilevskaya, et al.; Cancer Res.
63
, 3241 (2003)
Abstract
A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors:
A. Kamal, et al.; Nature
425
, 407 (2003)
Abstract
Chaperoning oncogenes: HSP90 as a target of geldanamycin:
L. Neckers; Handb. Exp. Pharmacol. 259 (2006)
Abstract
Drugging the cancer chaperone HSP90: Combinatorial therapeutic exploitation of oncogene addiction and tumor stress:
P. Workman, et al.; Ann. N.Y. Acad. Sci.
1113
, 202 (2007)
Abstract
Synergism between etoposide and 17-AAG in leukemia cells: critical roles for Hsp90, FLT3, topoisomerase II, Chk1, and Rad51:
Q. Yao, et al.; Clin. Cancer Res.
13
, 1591 (2007)
Abstract
;
Full Text
Phase I and pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with refractory advanced cancers:
R.K. Ramanathan, et al.; Clin. Cancer Res.
13
, 1769 (2007)
Abstract
HSP90 inhibitor 17AAG causes apoptosis in ATRA-resistant acute promyelocytic leukemia cells:
P.N. Meyer, et al.; Leuk. Res.
32
, 143 (2008)
Abstract
Intratumor injection of the Hsp90 inhibitor 17AAG decreases tumor growth and induces apoptosis in a prostate cancer xenograft model:
C.R. Williams, et al.; J. Urol.
178
, 1528 (2007)
Abstract
Rituximab and 17-allylamino-17-demethoxygeldanamycin induce synergistic apoptosis in B-cell chronic lymphocytic leukaemia:
A.J. Johnson, et al.; Br. J. Haematol.
139
, 837 (2007)
Abstract
An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models:
U. Banerji, et al.; Cancer Chemother. Pharmacol.
62
, 769 (2008)
Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors
•
Tyrosine Kinase Inhibitors
•
Antibiotics - Other Signal Transduction Pathway Modulators
•
Antitumor Agents (Enzyme Inhibitors)
•
HSP90 / HtpG / Related Products
ALX-350-104
Revised 10-May-07
Aaptamine
SYNONYMS
8,9-Dimethoxy-1
H
-benzo[
de
][1,6]naphtyridine
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Other Toxins
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ALX-350-104-M001
1 mg
90.00 USD
Product Specification
FORMULA:
C
13
H
12
N
2
O
2
MW:
228.3
CAS NUMBER:
85547-22-4
SOURCE/HOST:
Isolated from the sponge
Aaptos aaptos
.
PURITY:
≥97%
APPEARANCE:
Oil.
SOLUBILITY:
Soluble in DMSO or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
HAZARD:
TOXIC.
Product Description
Competitive antagonist of α-adrenoceptors in vascular smooth muscle cells. Inhibits cancer cell growth.
Product Specific Literature References
Alpha-adrenoceptor blocking action of aaptamine, a novel marine natural product, in vascular smooth muscle
:
Y. Ohizumi, et al.; J. Pharm. Pharmacol.
36
, 785 (1984)
Abstract
Antineoplastic agents 491. Synthetic conversion of aaptamine to isoaaptamine, 9-demethylaaptamine, and 4-methylaaptamine:
G.R. Pettit, et al.; J. Org. Chem.
69
, 2251 (2004)
Abstract
Aaptamine, a spongean alkaloid, activates p21 promoter in a p53-independent manner:
S. Aoki, et al.; BBRC
342
, 101 (2006)
Abstract
Further Categories Containing This Product:
Adrenergics & Adrenergic Receptors / Related Products
•
Natural Products - Antitumor Reagents
•
Antitumor Agents (Anti-proliferative)
•
Alkaloids
•
Marine Natural Products
ALX-350-310
Revised 03-Apr-08
3-O-Acetyl-11-keto-β-boswellic acid
SYNONYMS
AKβBA
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Natural Products - Antitumor Reagents
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ALX-350-310-M005
5 mg
130.00 USD
Product Specification
FORMULA:
C
32
H
48
O
5
MW:
512.7
CAS NUMBER:
67416-61-9
SOURCE/HOST:
Isolated from
Boswellia serrata.
PURITY:
≥99% (HPLC, NMR)
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in acetone, dichloromethane, diethyl ether or DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:
Protect from light.
HAZARD:
MAY BE CARCINOGENIC. HARMFUL.
Product Description
Shows antitumor and anti-inflammatory activities. Potent non-redox, noncompetitive 5-lipoxygenase and topoisomerase I and IIa inhibitor leading to apoptosis. 10-times more potent than 3-O-acetyl-β-boswellic acid (Prod. No.
ALX-350-308
). Exhibits
in vivo
efficacy in tumor growth and inhibition.
Product Specific Literature References
Acetyl-11-keto-beta-boswellic acid induces apoptosis in HL-60 and CCRF-CEM cells and inhibits topoisomerase I:
R.F. Hoernlein, et al.; J. Pharmacol. Exp. Ther.
288
, 613 (1999)
Abstract
;
Full Text
Boswellic acids activate p42(MAPK) and p38 MAPK and stimulate Ca(2+) mobilization:
A. Altmann, et al.; BBRC
290
, 185 (2002)
Abstract
Coupling of boswellic acid-induced Ca2+ mobilisation and MAPK activation to lipid metabolism and peroxide formation in human leucocytes:
A. Altmann, et al.; Br. J. Pharmacol.
141
, 223 (2004)
Abstract
;
Full Text
Inhibition of IkappaB kinase activity by acetyl-boswellic acids promotes apoptosis in androgen-independent PC-3 prostate cancer cells in vitro and in vivo:
T. Syrovets, et al.; J. Biol. Chem.
280
, 6170 (2005)
Abstract
;
Full Text
Boswellic acids: biological actions and molecular targets:
D. Poeckel & O. Werz; Curr. Med. Chem.
13
, 3359 (2006), Review
Abstract
Mechanisms underlying the anti-inflammatory actions of boswellic acid derivatives in experimental colitis:
C. Anthoni, et al.; Am. J. Physiol. Gastrointest. Liver Physiol.
290
, G1131 (2006)
Abstract
Potentiation of antinociceptive effect of NSAIDs by a specific lipooxygenase inhibitor, acetyl 11-keto-beta boswellic acid:
M. Bishnoi, et al.; Indian J. Exp. Biol.
44
, 128 (2006)
Abstract
Related Products
ALX-350-308
3-O-Acetyl-β-boswellic acid
Further Categories Containing This Product:
Natural Products - Protein Kinase Inhibitors
•
Natural Products - Topoisomerase Inhibitors
•
Lipoxygenases / Related Products
•
NF-kB Pathway Inhibitors
•
Natural Products - Anti-inflammatory Agents
•
Antitumor Agents (Apoptosis Inducers)
•
Natural Products - NF-kB Pathway Inhibitors
•
Natural Products - Apoptosis Inducers & Inhibitors
ALX-380-024
Revised 30-Oct-07
Actinomycin C
SYNONYMS
Cactinomycin
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antitumor Antibiotics
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ALX-380-024-M005
5 mg
40.00 USD
ALX-380-024-M025
25 mg
140.00 USD
Product Specification
CAS NUMBER:
8052-16-2
MERCK INDEX:
14:
1606
SOURCE/HOST:
Isolated from
Streptomyces chrysomallus.
PURITY:
≥98%
APPEARANCE:
Orange solid.
FORMULATION:
Mixture of actinomycin C1(= actinomycin D) (R = R’ = D-Val) ~3%, C2(R = D-Val, R’ = D-allo-Ile) ~45%, C3(R = R’ = D-allo-Ile) ~53%.
SOLUBILITY:
Soluble in methanol. Sparingly soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Protect from light.
HAZARD:
TOXIC.
Product Description
Antibiotic complex with antitumor activity.
Product Specific Literature References
Nomenclature of the Actinomycins:
S.A. Waksman, et al.; PNAS
44
, 602 (1958)
Abstract
General Information
For nomenclature see S.A. Waksman, E. Katz and L.C. Vining; PNAS
44
, 602 (1958).
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers)
•
Antibiotics - Apoptosis Inducers & Inhibitors
•
Transcription Inhibitors / Related Products
ALX-380-082
Revised 30-Oct-07
Actinomycin C2
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antitumor Antibiotics
Ordering Information
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ALX-380-082-C500
500 µg
80.00 USD
Product Specification
FORMULA:
C
63
H
88
N
12
O
16
MW:
1269.5
MERCK INDEX:
14:
1606
SOURCE/HOST:
Isolated from
Streptomyces sp.
PURITY:
≥98% (contains traces of ethylacetate or cyclohexane)
APPEARANCE:
Orange crystals.
SOLUBILITY:
Soluble in methanol, acetone or chloroform.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Keep cool and dry.
HAZARD:
TOXIC.
IDENTITY:
Determined by
1
H-NMR: Identical to standard reference.
Product Description
Antitumor antibiotic.
Product Specific Literature References
Nomenclature of the Actinomycins:
S.A. Waksman, et al.; PNAS
44
, 602 (1958)
Abstract
Actinomycin D, C2 and VII, inhibitors of Grb2-SHC interaction produced by Streptomyces:
J. Y. Nam, et al.; Bioorg. Med. Chem. Lett.
8
, 2001 (1998)
Abstract
Further Categories Containing This Product:
Transcription Inhibitors / Related Products
ALX-380-077
Revised 30-Oct-07
Actinomycin C3
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antitumor Antibiotics
Ordering Information
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ALX-380-077-M001
1 mg
70.00 USD
Product Specification
FORMULA:
C
64
H
90
N
12
O
16
MW:
1283.5
MERCK INDEX:
14:
1606
SOURCE/HOST:
Isolated from
Streptomyces sp.
PURITY:
≥98% (solvent free)
APPEARANCE:
Orange crystals.
SOLUBILITY:
Soluble in methanol, acetone or chloroform.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Keep cool and dry.
HAZARD:
TOXIC.
IDENTITY:
Determined by
1
H-NMR: Identical to standard reference.
Product Description
Antitumor antibiotic.
Product Specific Literature References
Nomenclature of the Actinomycins:
S.A. Waksman, et al.; PNAS
44
, 602 (1958)
Abstract
Further Categories Containing This Product:
Transcription Inhibitors / Related Products
ALX-380-009
Revised 26-Jun-08
Actinomycin D
SYNONYMS
Actinomycin IV
Actinomycin C
1
Dactinomycin
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antitumor Antibiotics
Ordering Information
Product Numbers:
Format:
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ALX-380-009-M005
5 mg
50.00 USD
ALX-380-009-M025
25 mg
200.00 USD
ALX-380-009-M100
100 mg
540.00 USD
Product Specification
FORMULA:
C
62
H
86
N
12
O
16
MW:
1255.5
CAS NUMBER:
50-76-0
MERCK INDEX:
14:
2800
RTECS:
AU1575000
SOURCE/HOST:
Isolated from
Streptomyces parvulus.
PURITY:
≥98%
APPEARANCE:
Red shiny crystals.
SOLUBILITY:
Soluble in DMSO, 100% ethanol or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
USE/STABILITY:
Sensitive to strong acids and bases.
HANDLING:
Protect from light. Hygroscopic.
HAZARD:
VERY TOXIC.
Product Description
Antitumor antibiotic. DNA intercalating agent. Cytotoxic inducer of apoptosis against tumor cells. Inhibitor of RNA synthesis.
For nomenclature see S.A. Waksman, E. Katz & L.C. Vining; PNAS
44
, 602 (1958)
Product Specific Literature References
Apoptosis induced by Actinomycin D, Camptothecin or Aphidicolin can occur in all phases of the cell cycle:
J.M. Glynn, et al.; Biochem. Soc. Trans.
20
, 84S (1992)
Abstract
Influence of DNA base sequence on the binding energetics of actinomycin D:
S.A. Bailey, et al.; Biochemistry
32
, 5881 (1993)
Abstract
Nitric oxide ameliorates actinomycin D/endotoxin-induced apoptotic liver failure in mice:
M. Akahori, et al.; J. Surg. Res.
85
, 286 (1999)
Abstract
Tumor necrosis factor-alpha plus actinomycin D-induced apoptosis of L929 cells is prevented by nitric oxide
:
S. Hakoda, et al.; Surg. Today
29
, 1059 (1999)
Abstract
Actinomycin D induces apoptosis and inhibits growth of pancreatic cancer cells:
J. Kleeff, et al.; Int. J. Cancer
86
, 399 (2000)
Abstract
Actinomycin D inhibiting K562 cell apoptosis elicited by salvicine but not decreasing its cytotoxicity
:
C. Qing, et al.; Acta Pharmacol. Sin.
24
, 415 (2003)
Abstract
;
Full Text
Actinomycin D induces histone gamma-H2AX foci and complex formation of gamma-H2AX with Ku70 and nuclear DNA helicase II:
H.E. Mischo, et al.; J. Biol. Chem.
280
, 9586 (2005)
Abstract
Actinomycin D upregulates proapoptotic protein Puma and downregulates Bcl-2 mRNA in normal peripheral blood lymphocytes:
I. Kalousek, et al.; Anticancer Drugs
18
, 763 (2007)
Abstract
Actinomycin D enhances TRAIL-induced caspase-dependent and -independent apoptosis in SH-SY5Y neuroblastoma cells:
M.J. Wang, et al.; Neurosci. Res.
59
, 40 (2007)
Abstract
Related Products
ALX-380-283
7-Amino-actinomycin D
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers)
•
Antibiotics - Apoptosis Inducers & Inhibitors
•
Transcription Inhibitors / Related Products
ALX-380-083
Revised 30-Oct-07
Actinomycin X0β
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antitumor Antibiotics
Ordering Information
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ALX-380-083-C200
200 µg
70.00 USD
Product Specification
FORMULA:
C
62
H
86
N
12
O
17
MW:
1271.5
SOURCE/HOST:
Isolated from
Streptomyces sp.
PURITY:
≥98% (contains traces of ethyl acetate or cyclohexane)
APPEARANCE:
Orange crystals.
SOLUBILITY:
Soluble in methanol, acetone or chloroform.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Keep cool and dry.
HAZARD:
TOXIC.
IDENTITY:
Detemined by
1
H-NMR: Identical to standard reference.
Product Description
Antitumor antibiotic.
Product Specific Literature References
Nomenclature of the Actinomycins:
S.A. Waksman, et al.; PNAS
44
, 602 (1958)
Abstract
Identification of actinomycins by high performance liquid chromatography and fast atom bombardment mass spectrometry:
S. Cho, et al.; Arch. Pharm. Res.
17
, 424 (1994)
Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors
•
Transcription Inhibitors / Related Products
ALX-380-084
Revised 30-Oct-07
Actinomycin X0δ
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antitumor Antibiotics
Ordering Information
Product Numbers:
Format:
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ALX-380-084-C200
200 µg
70.00 USD
Product Specification
FORMULA:
C
62
H
86
N
12
O
17
MW:
1271.5
SOURCE/HOST:
Isolated from
Streptomyces sp.
PURITY:
≥98% (contains traces of ethyl acetate or cyclohexane)
APPEARANCE:
Red crystals.
SOLUBILITY:
Soluble in methanol, acetone or chloroform.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Keep cool and dry.
HAZARD:
TOXIC.
IDENTITY:
Determined by
1
H-NMR: Identical to standard reference.
Product Description
Antitumor antibiotic.
Product Specific Literature References
Identification of actinomycins by high performance liquid chromatography and fast atom bombardment mass spectrometry:
S. Cho, et al.; Arch. Pharm. Res.
17
, 424 (1994)
Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors
•
Transcription Inhibitors / Related Products
ALX-380-080
Revised 03-Apr-08
Actinomycin X2
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antitumor Antibiotics
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
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ALX-380-080-M001
1 mg
70.00 USD
Product Specification
FORMULA:
C
62
H
84
N
12
O
17
MW:
1269.4
SOURCE/HOST:
Isolated from
Streptomyces sp
.
PURITY:
≥95% (solvent free)
APPEARANCE:
Orange crystals.
SOLUBILITY:
Soluble in methanol, acetone or chloroform.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Keep cool and dry.
HAZARD:
TOXIC.
IDENTITY:
Determined by
1
H-NMR: Identical to standard reference.
Product Description
Antitumor antibiotic. Has higher cytotoxicity toward cultured human leukemia (HL-60) cells than actinomycin D (Prod. No. ALX-380-009). Induces cell death via apoptosis.
Product Specific Literature References
Nomenclature of the Actinomycins:
S.A. Waksman, et al.; PNAS
44
, 602 (1958)
Abstract
Correlation of actinomycin X2 to the lipid profile in static and shaken cultures of Streptomyces nasri strain YG62:
M.Y. el-Naggar, et al.; Microbios.
100
, 117 (1999)
Abstract
Characterization of Streptomyces MITKK-103, a newly isolated actinomycin X2-producer:
K. Kurosawa, et al.; Appl. Microbiol. Biotechnol.
72
, 145 (2006)
Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors
•
Transcription Inhibitors / Related Products
ALX-380-085
Revised 30-Oct-07
Actinomycin Z1
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
