research use only
Cat.No.S8206
| Related Targets | HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite |
|---|---|
| Other Dehydrogenase Inhibitors | Vorasidenib (AG-881) (R)-GNE-140 CPI-613 (Devimistat) Sodium Dichloroacetate (DCA) Gossypol Acetate AGI-5198 AGI-6780 Emodin NCT-503 Brequinar |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| HT1080 | Function assay | Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as reduction in 2-hydroxyglutarate production, IC50 = 0.0075 μM. | 29079473 | |||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 100 mg/mL
(171.53 mM)
Ethanol : 100 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 582.96 | Formula | C28H22ClF3N6O3 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 1448347-49-6 | Download SDF | Storage of Stock Solutions |
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| Targets/IC50/Ki |
IDH1
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|---|---|
| In vitro |
TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with Ivosidenib (AG-120). This compound decreases intracellular 2-HG levels, inhibites growth factor independent proliferation and restores erythropoietin (EPO)-induced differentiation in TF-1 IDH1-R132H cells. Similarly, its pharmacological inhibition of mutant IDH1 enzyme in primary human blast cells cultured ex vivo provides an effective way to lower intracellular 2-HG levels and induces myeloid differentiation.
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References |
(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06127407 | Not yet recruiting | Locally Advanced or Metastatic Conventional Chondrosarcoma With an IDH1 Mutation Untreated or Previously Treated With 1 Systemic Treatment Regimen |
Servier Bio-Innovation LLC|Institut de Recherches Internationales Servier|Servier |
June 7 2024 | Phase 3 |
| NCT06377579 | Not yet recruiting | AML Adult |
French Innovative Leukemia Organisation|Acute Leukemia French Association |
May 15 2024 | -- |
| NCT06181734 | Recruiting | Acute Myeloid Leukemia (AML) |
iOMEDICO AG |
December 20 2023 | -- |
| NCT05907057 | Recruiting | Acute Myeloid Leukemia (AML) |
Servier Affaires Médicales|Servier |
June 14 2023 | Phase 3 |
| NCT04955938 | Recruiting | IDH Mutation|IDH1 Mutation|IDH2 Gene Mutation|Blood Cancer|Myeloproliferative Neoplasm |
University of Chicago |
October 29 2021 | Phase 1 |
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