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Cat. No.: HY-120181

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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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

AGI-14100 Chemical Structure

CAS No.: 1448346-43-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

mIDH

6 nM (IC₅₀)

All Isocitrate Dehydrogenase (IDH) Isoforms :

IDH1
IDH2

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

CAS No. 1448346-43-7
Molecular Weight 599.96
Formula 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Popovici-Muller J, et al. Discovery of AG-120 (Ivosidenib): a first-in-class mutant IDH1 inhibitor for the treatment of IDH1 mutant cancers[J]. ACS medicinal chemistry letters, 2018, 9(4): 300-305. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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