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 |
|---|---|---|
| High-throughput screening compatible cell-based assay for interrogating activated notch signaling. | 2009 Feb |
|
| Drugging the PI3 kinome: from chemical tools to drugs in the clinic. | 2010 Mar 15 |
|
| Physical association of PDK1 with AKT1 is sufficient for pathway activation independent of membrane localization and phosphatidylinositol 3 kinase. | 2010 Mar 26 |
|
| Pharmacokinetic-pharmacodynamic modeling of tumor growth inhibition and biomarker modulation by the novel phosphatidylinositol 3-kinase inhibitor GDC-0941. | 2010 Sep |
|
| Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941. | 2010 Sep |
|
| Targeting a common collaborator in cancer development. | 2010 Sep 8 |
|
| Effect of PI3K- and mTOR-specific inhibitors on spontaneous B-cell follicular lymphomas in PTEN/LKB1-deficient mice. | 2011 Mar 29 |
|
| Modulators of sensitivity and resistance to inhibition of PI3K identified in a pharmacogenomic screen of the NCI-60 human tumor cell line collection. | 2012 |
|
| Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. | 2012 Jan 1 |
|
| 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 |
|
| Mechanisms of apoptosis induction by simultaneous inhibition of PI3K and FLT3-ITD in AML cells in the hypoxic bone marrow microenvironment. | 2013 Feb 1 |
|
| Simultaneous inhibition of pan-phosphatidylinositol-3-kinases and MEK as a potential therapeutic strategy in peripheral T-cell lymphomas. | 2013 Jan |
|
| 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
by
admin
on
Edited
Fri Dec 15 21:13:30 UTC 2023
by
admin
on
Fri Dec 15 21:13:30 UTC 2023
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ICY00EMP8P
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Validated (UNII)
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