Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H22N2O5 |
Molecular Weight | 430.4526 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCOC(=O)C1=CC2=C(NC3=C(OC)C4=C(C=C23)C5=C(N4)C=CC(=C5)C(=O)OCC)C=C1
InChI
InChIKey=BMTPVPNVQOYGAP-UHFFFAOYSA-N
InChI=1S/C25H22N2O5/c1-4-31-24(28)13-6-8-19-15(10-13)17-12-18-16-11-14(25(29)32-5-2)7-9-20(16)27-22(18)23(30-3)21(17)26-19/h6-12,26-27H,4-5H2,1-3H3
Molecular Formula | C25H22N2O5 |
Molecular Weight | 430.4526 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
SR-13668 is an indolocarbazole derivative patented by American nonprofit scientific research institute SRI International as a chemotherapeutic and chemopreventive agent for the treatment and prevention of cancers, such as breast and ovarian cancer. SR-13668 appears to inhibit Akt activation by blocking growth factor-stimulated Akt phosphorylation, and it does not target the ATP substrate binding site. Preclinical safety studies showed that SR-13668 is not genotoxic in Ames mutagenicity tests or in the mouse micronucleus test. In a 14-day toxicity study in which Sprague−Dawley rats have orally dosed with SR13668 no drug-related mortality, changes in body or organ weights, or other signs of significant toxicity were seen at any dose level. However, the compound is highly hydrophobic and its limited oral bioavailability has hindered its clinical translation.
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
In vitro assessment of P450 induction potential of novel chemopreventive agents SR13668, 9-cis-UAB30, and pentamethychromanol in primary cultures of human hepatocytes. | 2009 May 15 |
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Pharmacokinetics and enhanced bioavailability of candidate cancer preventative agent, SR13668 in dogs and monkeys. | 2010 May |
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Phase 0 clinical chemoprevention trial of the Akt inhibitor SR13668. | 2011 Mar |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21372034
38 mg
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 07:44:13 GMT 2023
by
admin
on
Sat Dec 16 07:44:13 GMT 2023
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Record UNII |
2P8KGO7903
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Record Status |
Validated (UNII)
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Record Version |
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