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MedKoo product information:
PX-12
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MedKoo Code#: 202340
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Name: PX-12
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CAS#: 141400-58-0
Synonym:
CA Index Name: 1H-Imidazole, 2-[(1-methylpropyl)dithio]-; Other
Names: PX 12.
IUPAC/Chemical name:
2-(sec-butyldisulfanyl)-1H-imidazole.
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Chemical structure |
Theoretical analysis
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Chemical Formula: C7H12N2S2
Exact Mass: 188.04419
Molecular Weight: 188.31
m/z: 188.04419 (100.0%), 190.03999 (9.0%),
189.04754 (7.6%), 189.04358 (1.6%)
Elemental Analysis: C, 44.65; H, 6.42; N,
14.88; S, 34.05
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Availability and price:
This agent is not in stock, which may be available through custom synthesis. To inquire quotation and lead time or to ask questions, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Information about this agent
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Thioredoxin-1 (Trx-1) is a small redox protein that
is over-expressed in many human tumors, where it is associated with
aggressive tumor growth and decreased patient survival. Trx-1 is
secreted by tumor cells and is present at increased levels in the plasma
of cancer patients. PX-12 is an irreversible inhibitor of Trx-1
currently in clinical development as an antitumor agent.The research
results suggest that the lowering of elevated levels of plasma Trx-1 in
cancer patients may provide a surrogate for the inhibition of tumor
Trx-1 by PX-12. Furthermore, PX-12 decreases plasma VEGF levels which
may contribute to the antitumor activity of PX-12. See:
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1432091/.
Current developer:
Biomira Inc; Oncothyreon Inc.
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Tommasi, N. Thioredoxin system modulation by plant and fungal secondary
metabolites. Current Medicinal Chemistry (2010), 17(5), 479-494. CODEN:
CMCHE7 ISSN:0929-8673. CAN 152:396831 AN 2010:258754
2. Rickles, Richard; Lee, Margaret S. -Adrenergic receptor agonists
for the treatment of B-cell proliferative disorders. PCT Int. Appl.
(2009), 111 pp. CODEN: PIXXD2 WO 2009151569 A2 20091217 CAN 152:67621 AN
2009:1566750
3. Witczak, Zbigniew J. 1,5-C-Thio-sugars as selective inhibitors of
thioredoxins. Abstracts of Papers, 238th ACS National Meeting,
Washington, DC, United States, August 16-20, 2009 (2009), CARB-128.
CODEN: 69LVCL AN 2009:980954
4. Kirkpatrick, Lynn. Compositions and methods for using asymmetric
disulfides for treating cancer. PCT Int. Appl. (2009), 39 pp. CODEN:
PIXXD2 WO 2009082686 A1 20090702 CAN 151:93997 AN 2009:799277
5. Rickles, Richard; Lee, Margaret S. Use of adenosine A2A receptor
agonists and phosphodiesterase (PDE) inhibitors for the treatment of
B-cell proliferative disorders, and combinations with other agents. PCT
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150:160095 AN 2009:86451
6. Rickles, Richard; Pierce, Laura; Lee, Margaret S. Combinations for
the treatment of B-cell proliferative disorders. PCT Int. Appl. (2009),
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2009:83374
7. Huber, Kelly; Patel, Poulam; Zhang, Lei; Evans, Helen; Westwell,
Andrew D.; Fischer, Peter M.; Chan, Stephen; Martin, Stewart.
2-[(1-Methylpropyl)dithio]-1H-imidazole inhibits tubulin polymerization
through cysteine oxidation. Molecular Cancer Therapeutics (2008), 7(1),
143-151. CODEN: MCTOCF ISSN:1535-7163. CAN 148:322142 AN 2008:64825
8. Ramanathan, Ramesh K.; Kirkpatrick, D. Lynn; Belani, Chandra P.;
Friedland, David; Green, Sylvan B.; Chow, H-H. Sherry; Cordova,
Catherine A.; Stratton, Steven P.; Sharlow, Elizabeth R.; Baker, Amanda;
Dragovich, Tomislav. A Phase I Pharmacokinetic and Pharmacodynamic Study
of PX-12, a Novel Inhibitor of Thioredoxin-1, in Patients with Advanced
Solid Tumors. Clinical Cancer Research (2007), 13(7), 2109-2114. CODEN:
CCREF4 ISSN:1078-0432. CAN 147:314431 AN 2007:369854
9. Galmarini, Carlos M. Drug evaluation: the thioredoxin inhibitor PX-12
in the treatment of cancer. Current Opinion in Investigational Drugs
(Thomson Scientific) (2006), 7(12), 1108-1115. CODEN: COIDAZ
ISSN:1472-4472. CAN 146:219923 AN 2007:71951
10. Kirkpatrick, Lynn; Pestano, Linda Anne. Determination of HIF-1
inhibitor treatment response. U.S. Pat. Appl. Publ. (2006), 28 pp.,
Cont.-in-part of U.S. Ser. No. 929,156. CODEN: USXXCO US 2006275836 A1
20061207 CAN 146:20274 AN 2006:1286049
11. Baker, Amanda F.; Dragovich, Tomislav; Tate, Wendy R.; Ramanathan,
Ramesh K.; Roe, Denise; Hsu, Chiu-Hsieh; Kirkpatrick, D. Lynn; Powis,
Garth. The antitumor thioredoxin-1 inhibitor PX-12 (1-methylpropyl
2-imidazolyl disulfide) decreases thioredoxin-1 and VEGF levels in
cancer patient plasma. Journal of Laboratory and Clinical Medicine
(2006), 147(2), 83-90. CODEN: JLCMAK ISSN:0022-2143. CAN 145:95883 AN
2006:110292
12. Jordan, Benedicte F.; Runquist, Matthew; Raghunand, Natarajan;
Gillies, Robert J.; Tate, Wendy R.; Powis, Garth; Baker, Amanda F. The
Thioredoxin-1 Inhibitor 1-Methylpropyl 2-Imidazolyl Disulfide (PX-12)
Decreases Vascular Permeability in Tumor Xenografts Monitored by Dynamic
Contrast Enhanced Magnetic Resonance Imaging. Clinical Cancer Research
(2005), 11(2, Pt. 1), 529-536. CODEN: CCREF4 ISSN:1078-0432. CAN
142:385270 AN 2005:271357
13. Bergink, Arjan P.; van Meurs, Joyce B.; Loughlin, John; Arp, Pascal
P.; Fang, Yue; Hofman, Albert; van Leeuwen, Johannes P. T. M.; van Duijn,
Cornelia M.; Uitterlinden, Andre G.; Pols, Huibert A. P. Estrogen
receptor gene haplotype is associated with radiographic osteoarthritis
of the knee in elderly men and women. Arthritis & Rheumatism (2003),
48(7), 1913-1922. CODEN: ARHEAW ISSN:0004-3591. CAN 139:259400 AN
2003:612865
14. Welsh, Sarah J.; Williams, Ryan R.; Birmingham, Anne; Newman, David
J.; Kirkpatrick, D. Lynn; Powis, Garth. The thioredoxin redox inhibitors
1-methylpropyl-2-imidazolyl disulfide and pleurotin inhibit
hypoxia-induced factor 1 and vascular endothelial growth factor
formation. Molecular Cancer Therapeutics (2003), 2(3), 235-243. CODEN:
MCTOCF ISSN:1535-7163. CAN 139:143631 AN 2003:238985
15. Husbeck, Bryan; Powis, Garth. The redox protein thioredoxin-1
regulates the constitutive and inducible expression of the estrogen
metabolizing cytochromes P450 1B1 and 1A1 in MCF-7 human breast cancer
cells. Carcinogenesis (2002), 23(10), 1625-1630. CODEN: CRNGDP
ISSN:0143-3334. CAN 138:53510 AN 2002:799915
16. Kirkpatrick, D. Lynn; Powis, Garth; Miller, Raymond A. DNA arrays
for determining drug selectivity. PCT Int. Appl. (2001), 37 pp. CODEN:
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17. Shirato, Yoshimi; Shimokawa, Kenji; Shimura, Mitsunori. Adsorptive
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JKXXAF JP 02138137 A 19900528 Heisei. CAN 113:134638 AN 1990:534638
18. Broncel Marlena; Kozirog Marzena; Duchnowicz Piotr; Koter-Michalak
Maria; Sikora Joanna; Chojnowska-Jezierska Julita Aronia melanocarpa
extract reduces blood pressure, serum endothelin, lipid, and oxidative
stress marker levels in patients with metabolic syndrome. Medical
science monitor : international medical journal of experimental and
clinical research (2010), 16(1), CR28-34.
19. Bayes M; Rabasseda X; Prous J R Gateways to clinical trials. Methods
and findings in experimental and clinical pharmacology (2007), 29(5),
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20. Kiviharju Kristiina; Moilanen Ulla; Leisola Matti; Eerikainen Tero A
chemostat study of Streptomyces peucetius var. caesius N47. Applied
microbiology and biotechnology (2007), 73(6), 1267-74.
21. Bayes M; Rabasseda X; Prous J R Gateways to clinical trials. Methods
and findings in experimental and clinical pharmacology (2004), 26(3),
211-44.
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