Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C21H16FN7O |
| Molecular Weight | 401.3964 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H](NC1=C2NC=NC2=NC=N1)C3=NC4=C(C=C(F)C=C4)C(=O)N3C5=CC=CC=C5
InChI
InChIKey=DOCINCLJNAXZQF-LBPRGKRZSA-N
InChI=1S/C21H16FN7O/c1-12(27-19-17-18(24-10-23-17)25-11-26-19)20-28-16-8-7-13(22)9-15(16)21(30)29(20)14-5-3-2-4-6-14/h2-12H,1H3,(H2,23,24,25,26,27)/t12-/m0/s1
GS-9820 (formerly CAL-120) is an oral, small molecule delta selective Phosphatidylinositol 3-kinases (PI3 kinase) inhibitor, a first in class compound, with greater than 200-fold selectivity in cell-based assays for the delta isoform as compared to other class isoforms. GS-9820 is designed to induce cancer cell death and inhibit signaling pathways associated with cancer cell dependence on the tumor microenvironment. GS-9820 is on the phase I of clinical trial, where has to be determined the appropriate dosing regimen of drug in subjects with lymphoid malignancies.
Approval Year
Sample Use Guides
200 mg administered twice a day. Escalation will proceed to the maximum tolerated dose (MTD), defined as the highest tested dose associated with a rate of dose-limiting toxicities (DLT) of < 33% during the first 4 weeks of therapy.
Route of Administration:
Oral
GS-9820 (ACALISIB) was characterized using in vitro activity assays in the presence of 10 uM GS-9820. GS-9820 was more selective for PI3Kδ relative to other PI3K class I enzymes (IC50: PI3Kα, 5,441 nm; PI3Kβ, 3,377 nm; PI3Kγ, 1,389 nm; and PI3Kδ, 12.7 nm). GS-9820 was also 103-fold more selective against PI3Kδ than against related kinases, such as CIIβ, hVPS34, DNAPK, and mammalian target of rapamycin.
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C129825
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NCI_THESAURUS |
C2152
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admin on Sat Dec 16 10:31:50 GMT 2023 , Edited by admin on Sat Dec 16 10:31:50 GMT 2023
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9812
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11618268
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870281-34-8
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100000175794
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OVW60IDW1D
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DB15407
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C103277
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CHEMBL3545397
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ACTIVE MOIETY
