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.
For research use only. We do not sell to patients.
- CAS No.: 1448346-43-7
- Formula: C29H22ClF4N5O3
- Molecular Weight:599.96
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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mIDH 6 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | IC50 |
0.76 nM
Compound: 10; AGI-14100
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Antiproliferative activity against human HT1080 cells transfected with IDH1 R132H mutant
Antiproliferative activity against human HT1080 cells transfected with IDH1 R132H mutant
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[PMID: 29847930] |
| TF-1 | IC50 |
1.75 nM
Compound: 10; AGI-14100
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Antiproliferative activity against human TF1 cells transfected with IDH1 R132H mutant
Antiproliferative activity against human TF1 cells transfected with IDH1 R132H mutant
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[PMID: 29847930] |
| U-87MG ATCC | IC50 |
0.74 nM
Compound: 10; AGI-14100
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Antiproliferative activity against human U87MG cells transfected with IDH1 R132H mutant
Antiproliferative activity against human U87MG cells transfected with IDH1 R132H mutant
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[PMID: 29847930] |
Chemical Information
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CAS No. 1448346-43-7
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Molecular Weight 599.96
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AGI-14100 Related Classifications
HY-120181 Related Classifications
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