Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H27N7O3S2 |
| Molecular Weight | 513.636 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(=O)(=O)N1CCN(CC2=CC3=NC(=NC(N4CCOCC4)=C3S2)C5=CC=CC6=C5C=NN6)CC1
InChI
InChIKey=LHNIIDJUOCFXAP-UHFFFAOYSA-N
InChI=1S/C23H27N7O3S2/c1-35(31,32)30-7-5-28(6-8-30)15-16-13-20-21(34-16)23(29-9-11-33-12-10-29)26-22(25-20)17-3-2-4-19-18(17)14-24-27-19/h2-4,13-14H,5-12,15H2,1H3,(H,24,27)
| Molecular Formula | C23H27N7O3S2 |
| Molecular Weight | 513.636 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Pictilisib is an oral potent inhibitor of class I PI3K with nanomolar activities against p110alpha, p110beta, p110delta, and p110gamma. The drug was developed for the treatment of solid tumors and reached phase II in patients with breast cancer and lung carcinoma, however its development was terminated.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. | 2009 Jul |
|
| Inhibition profiles of phosphatidylinositol 3-kinase inhibitors against PI3K superfamily and human cancer cell line panel JFCR39. | 2010 Apr |
|
| Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors. | 2010 Feb 1 |
|
| PIKing the right patient. | 2010 Jul 15 |
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| Predictive biomarkers of sensitivity to the phosphatidylinositol 3' kinase inhibitor GDC-0941 in breast cancer preclinical models. | 2010 Jul 15 |
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| Physical association of PDK1 with AKT1 is sufficient for pathway activation independent of membrane localization and phosphatidylinositol 3 kinase. | 2010 Mar 26 |
|
| Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. | 2010 Nov 24 |
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| Pharmacokinetic-pharmacodynamic modeling of tumor growth inhibition and biomarker modulation by the novel phosphatidylinositol 3-kinase inhibitor GDC-0941. | 2010 Sep |
|
| Effect of PI3K- and mTOR-specific inhibitors on spontaneous B-cell follicular lymphomas in PTEN/LKB1-deficient mice. | 2011 Mar 29 |
|
| GDC-0941 sensitizes breast cancer to ABT-737 in vitro and in vivo through promoting the degradation of Mcl-1. | 2011 Oct 1 |
|
| Comprehensive analysis of kinase inhibitor selectivity. | 2011 Oct 30 |
|
| PI3K inhibition enhances doxorubicin-induced apoptosis in sarcoma cells. | 2012 |
|
| The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition. | 2012 Apr 10 |
|
| Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatments in PTEN-deficient mice lymphoma. | 2012 Feb |
|
| The novel dual PI3K/mTOR inhibitor GDC-0941 synergizes with the MEK inhibitor U0126 in non-small cell lung cancer cells. | 2012 Feb |
|
| Genetic disruption of the PI3K regulatory subunits, p85α, p55α, and p50α, normalizes mutant PTPN11-induced hypersensitivity to GM-CSF. | 2012 Jul |
|
| GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of docetaxel in human breast cancer models by increasing cell death in vitro and in vivo. | 2012 Jul 15 |
|
| Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. | 2012 May |
|
| Regulation of CD38 expression in human airway smooth muscle cells: role of class I phosphatidylinositol 3 kinases. | 2012 Oct |
|
| Single cell network profiling assay in bladder cancer. | 2013 Apr |
|
| A potent combination of the novel PI3K Inhibitor, GDC-0941, with imatinib in gastrointestinal stromal tumor xenografts: long-lasting responses after treatment withdrawal. | 2013 Feb 1 |
|
| Conditional activation of Pik3ca(H1047R) in a knock-in mouse model promotes mammary tumorigenesis and emergence of mutations. | 2013 Jan 17 |
|
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. | 2013 Nov |
|
| The PI3K inhibitor GDC-0941 combines with existing clinical regimens for superior activity in multiple myeloma. | 2014 Jan 16 |
|
| Utilization of human nuclear receptors as an early counter screen for off-target activity: a case study with a compendium of 615 known drugs. | 2015 Jun |
Sample Use Guides
Patients with breast cancer receive paclitaxel (90 mg/m2 weekly for 3 weeks in every 28-day cycle) with 260 mg pictilisib (daily on days 1-5 every week).
Route of Administration:
Oral
| Substance Class |
Chemical
Created
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admin
on
Edited
Fri Dec 15 21:13:30 GMT 2023
by
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on
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ICY00EMP8P
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