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MedKoo product information:
SR13668
Description of SR13668: SR13668
is an Akt inhibitor, is also an orally bioavailable
indole-3-carbinol (I3C) analogue inhibitor of the serine/threonine
protein kinase Akt (protein kinase B) with potential antineoplastic
and antiangiogenic activities. Akt inhibitor SR13668 binds to and
inhibits the activity of Akt, which may result in inhibition of the
PI3K/Akt signaling pathway and tumor cell proliferation, and the
induction of tumor cell apoptosis. Activation of the PI3K/Akt
signaling pathway is frequently associated with tumorigenesis and
dysregulated PI3K/Akt signaling may contribute to tumor resistance
to a variety of antineoplastic agents. Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Thesaurus).
Current developer: Mayo Clinic.
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MedKoo Code#:
205672
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Name:
SR13668
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CAS#:
637774-61-9
Synonym:
SR13668; SR 13668; SR-13668;
CHEMBL245030; LS-190469;
2,10-dicarbethoxy-6-methoxy-5,7-dihydro-indolo[2,3-b] carbazole
IUPAC/Chemical name:
diethyl
6-methoxy-5,7-dihydroindolo[2,3-b]carbazole-2,10-dicarboxylate
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Chemical structure
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Theoretical analysis
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MedKoo Code#: 205672
Name: SR13668
CAS#: 637774-61-9
Chemical Formula: C25H22N2O5
Exact Mass: 430.15287
Molecular Weight: 430.45258
Elemental Analysis: C, 69.76; H, 5.15; N,
6.51; O, 18.58
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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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Highlights of recent research using this agent
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SR13668, a bis-indole with potent activity in vitro and in vivo
against various cancers and promising cancer chemopreventive activity,
was found to have very low oral bioavailability, <1%, in rats during
pilot pharmacokinetic studies.
1: Reid JM, Walden CA, Qin R, Ziegler KL, Haslam JL,
Rajewski RA, Warndahl R, Fitting CL, Boring D, Szabo E, Crowell J,
Perloff M, Jong L, Bauer BA, Mandrekar SJ, Ames MM, Limburg PJ; Cancer
Prevention Network. Phase 0 clinical chemoprevention trial of the Akt
inhibitor SR13668. Cancer Prev Res (Phila). 2011 Mar;4(3):347-53. PubMed
PMID: 21372034; PubMed Central PMCID: PMC3061470.
2: Cohen EE, Schilsky RL. The next phase of chemoprevention research.
Cancer Prev Res (Phila). 2011 Mar;4(3):293-5. PubMed PMID: 21372026.
3: Green CE, Swezey R, Bakke J, Shinn W, Furimsky A, Bejugam N, Shankar
GN, Jong L, Kapetanovic IM. Improved oral bioavailability in rats of
SR13668, a novel anti-cancer agent. Cancer Chemother Pharmacol. 2011
May;67(5):995-1006. Epub 2010 Jul 10. PubMed PMID: 20623225; PubMed
Central PMCID: PMC3061244.
4: Kapetanovic IM, Muzzio M, Hu SC, Crowell JA, Rajewski RA, Haslam JL,
Jong L, McCormick DL. Pharmacokinetics and enhanced bioavailability of
candidate cancer preventative agent, SR13668 in dogs and monkeys. Cancer
Chemother Pharmacol. 2010 May;65(6):1109-16. Epub 2009 Sep 16. PubMed
PMID: 19756605.
5: Jackson JP, Kabirov KK, Kapetanovic IM, Lyubimov A. In vitro
assessment of P450 induction potential of novel chemopreventive agents
SR13668, 9-cis-UAB30, and pentamethychromanol in primary cultures of
human hepatocytes. Chem Biol Interact. 2009 May 15;179(2-3):263-72. Epub
2008 Dec 16. PubMed PMID: 19135037.
6: Chao WR, Yean D, Amin K, Green C, Jong L. Computer-aided rational
drug design: a novel agent (SR13668) designed to mimic the unique
anticancer mechanisms of dietary indole-3-carbinol to block Akt
signaling. J Med Chem. 2007 Jul 26;50(15):3412-5. Epub 2007 Jun 29.
PubMed PMID: 17602463.
7: Doppalapudi RS, Riccio ES, Rausch LL, Shimon JA, Lee PS, Mortelmans
KE, Kapetanovic IM, Crowell JA, Mirsalis JC. Evaluation of
chemopreventive agents for genotoxic activity. Mutat Res. 2007 May
18;629(2):148-60. Epub 2007 Feb 25. PubMed PMID: 17387038.
8: He H, Cho HT, Li W, Kawakita T, Jong L, Tseng SC.
Signaling-transduction pathways required for ex vivo expansion of human
limbal explants on intact amniotic membrane. Invest Ophthalmol Vis Sci.
2006 Jan;47(1):151-7. PubMed PMID: 16384957; PubMed Central PMCID:
PMC1579252.
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