AGI-5198

Alias: IDH C35; AGI5198; IDH-C35; IDHC35; AGI-5198; AGI 5198;
Cat No.:V0855 Purity: ≥98%
AGI-5198 (also know as IDH-C35; IDHC35; AGI-5198; AGI 5198) is a novel, highly potent and selective inhibitor of IDH1 (isocitrate dehydrogenase 1) R132H/R132C mutants with potential anticancer activity.
AGI-5198 Chemical Structure CAS No.: 1355326-35-0
Product category: Dehydrogenase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

AGI-5198 (also know as IDH-C35; IDHC35; AGI-5198; AGI 5198) is a novel, highly potent and selective inhibitor of IDH1 (isocitrate dehydrogenase 1) R132H/R132C mutants with potential anticancer activity. It inhibits IDH1 R132H/R132C with IC50 of 0.07 μM/0.16 μM, respectively. AGI-5198 demonstrates significant in vivo antitumor efficacy in IDH1 mutant glioma xenografts.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
The amount of R-2HG in TS603 glioma cell pellets was measured, and the results showed that AGI-5198 inhibited the mutant IDH1 enzyme in a dose-dependent manner. In two patient-derived glioma cell lines (TS676 and TS516) that express exclusively wild-type IDH1 alleles, AGI-5198 has no effect on colony formation [1]. When exposed to ionizing radiation (IR), cancer cells heterozygous for the IDH1 (R132H) mutation show reduced IDH-mediated NADPH generation and consequently increased amounts of reactive oxygen species, or DNA, compared to IDH1 wild-type cells. Double-strand breaks and cell death are also observed. These effects are reversed by AGI-5198, an IDH1 (R132H) inhibitor [2].
ln Vivo
In human glioma xenografts, AGI-5198 (450 mg/kg, po) inhibits tumor growth by 50% to 60%. Mice treated with AGI-5198 had tumors that stained less strongly with anti-Ki-67 antibodies. Glioma xenografts of the IDH1 wild-type grow unaffected by AGI-5198 [1].
Animal Protocol
Dissolved in 0.5% MC and 0.2% Tween 80; 150 mg/kg, 450 mg/kg per day; oral gavage
IDH1 mutant glioma xenografts
References
[1]. Rohle D, et al. An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells. Science. 2013 May 3;340(6132):626-30.
[2]. Molenaar RJ, et al. Radioprotection of IDH1-Mutated Cancer Cells by the IDH1-Mutant Inhibitor AGI-5198. Cancer Res. 2015 Nov 15;75(22):4790-802
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H31FN4O2
Molecular Weight
462.56
CAS #
1355326-35-0
SMILES
O=C(NC1CCCCC1)C(N(C2=CC=CC(F)=C2)C(CN3C=CN=C3C)=O)C4=CC=CC=C4C
InChi Key
FNYGWXSATBUBER-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H31FN4O2/c1-19-9-6-7-14-24(19)26(27(34)30-22-11-4-3-5-12-22)32(23-13-8-10-21(28)17-23)25(33)18-31-16-15-29-20(31)2/h6-10,13-17,22,26H,3-5,11-12,18H2,1-2H3,(H,30,34)
Chemical Name
N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide
Synonyms
IDH C35; AGI5198; IDH-C35; IDHC35; AGI-5198; AGI 5198;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 24 mg/mL (51.9 mM)
Water:<1 mg/mL
Ethanol: 14 mg/mL (30.3 mM)
Solubility (In Vivo)
0.5% methylcellulose+0.2% Tween 80: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1619 mL 10.8094 mL 21.6188 mL
5 mM 0.4324 mL 2.1619 mL 4.3238 mL
10 mM 0.2162 mL 1.0809 mL 2.1619 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • AGI-5198

    AGI-5198 impairs growth of IDH1-mutant glioma xenografts in mice.Science.2013 May 3;340(6132):626-30.
  • AGI-5198 promotes astroglial differentiation in R132H-IDH1 mutant cells.Science.2013 May 3;340(6132):626-30.
  • Dose-dependent inhibition of histone methylation in IDH1-mutant gliomas after shortterm treatment with AGI-5198.Science.2013 May 3;340(6132):626-30.
  • An R132H-IDH1 inhibitor blocks R-2HG production and soft-agar growth of IDH1-mutant glioma cells.Science.2013 May 3;340(6132):626-30.
  • AGI-5198

  • AGI-5198

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