AGI-14100
AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC50=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 1448346-43-7
- Formule: C29H22ClF4N5O3
- Masse moléculaire:599.96
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
mIDH 6 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | IC50 |
0.76 nM
Compound: 10; AGI-14100
|
Antiproliferative activity against human HT1080 cells transfected with IDH1 R132H mutant
Antiproliferative activity against human HT1080 cells transfected with IDH1 R132H mutant
|
[PMID: 29847930] |
| TF-1 | IC50 |
1.75 nM
Compound: 10; AGI-14100
|
Antiproliferative activity against human TF1 cells transfected with IDH1 R132H mutant
Antiproliferative activity against human TF1 cells transfected with IDH1 R132H mutant
|
[PMID: 29847930] |
| U-87MG ATCC | IC50 |
0.74 nM
Compound: 10; AGI-14100
|
Antiproliferative activity against human U87MG cells transfected with IDH1 R132H mutant
Antiproliferative activity against human U87MG cells transfected with IDH1 R132H mutant
|
[PMID: 29847930] |
Chemical Information
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CAS No. 1448346-43-7
-
Masse moléculaire 599.96
-
Formule C29H22ClF4N5O3
-
SMILES
O=C([C@@H](N1C2=NC=CC(C#N)=C2)CCC1=O)N([C@@H](C3=CC=CC=C3Cl)C(NC4CC(C4)(F)F)=O)C5=CC(F)=CC(F)=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)