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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1448346-43-7
- Formel: C29H22ClF4N5O3
- Molecular Weight:599.96
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
|
mIDH 6 nM (IC50) |
Cellular Effect
|
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. Nr. 1448346-43-7
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Molecular Weight 599.96
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Formel C29H22ClF4N5O3
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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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)