Ivosidenib (AG-120)

Catalog No.S8206 Batch:S820603

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Technical Data

Formula

C28H22ClF3N6O3
Molecular Weight 582.96 CAS No. 1448347-49-6
Solubility (25°C)* In vitro DMSO 100 mg/mL (171.53 mM)
Ethanol 100 mg/mL (171.53 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
Targets
IDH1 [1]
In vitro TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120.Treatment with AG-120 decreases intracellular 2-HG levels, inhibites growth factor independent proliferation and restores erythropoietin (EPO)-induced differentiation in TF-1 IDH1-R132H cells. Similarly, pharmacological inhibition of mutant IDH1 enzyme with AG-120 in primary human blast cells cultured ex vivo provides an effective way to lower intracellular 2-HG levels and induces myeloid differentiation[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    TF-1 cells

  • Concentrations

    0.5, 1.0, and 5.0 μM

  • Incubation Time

    6 days

  • Method

    TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120.

Customer Product Validation

Data from [Data independently produced by , , Oncol Rep, 2017, 38(6):3583-3591]

Data from [Data independently produced by , , ONCOLOGY REPORTS, 2017, 38: 3583-3591]

Selleck's Ivosidenib (AG-120) has been cited by 13 publications

Dysregulated Lipid Synthesis by Oncogenic IDH1 Mutation Is a Targetable Synthetic Lethal Vulnerability [ Cancer Discov, 2023, 13(2):496-515] PubMed: 36355448
ABCC1 and glutathione metabolism limit the efficacy of BCL-2 inhibitors in acute myeloid leukemia [ Nat Commun, 2023, 14(1):5709] PubMed: 37726279
ABCC1 and glutathione metabolism limit the efficacy of BCL-2 inhibitors in acute myeloid leukemia [ Nat Commun, 2023, 14(1):5709] PubMed: 37726279
Mutant IDH regulates glycogen metabolism from early cartilage development to malignant chondrosarcoma formation [ Cell Rep, 2023, 42(6):112578] PubMed: 37267108
Germline mutations in mitochondrial complex I reveal genetic and targetable vulnerability in IDH1-mutant acute myeloid leukaemia [ Nat Commun, 2022, 13(1):2614] PubMed: 35551192
Secondary IDH1 resistance mutations and oncogenic IDH2 mutations cause acquired resistance to ivosidenib in cholangiocarcinoma [ NPJ Precis Oncol, 2022, 6-1:61] PubMed: 36056177
Incorporation of SKI-G-801, a Novel AXL Inhibitor, With Anti-PD-1 Plus Chemotherapy Improves Anti-Tumor Activity and Survival by Enhancing T Cell Immunity [ Front Pharmacol, 2022, 13:871392] PubMed: 35418865
The long non-coding RNA CDK6-AS1 overexpression impacts on acute myeloid leukemia differentiation and mitochondrial dynamics [ iScience, 2021, 24(11):103350] PubMed: 34816103
Exosomal IDH1 increases the resistance of colorectal cancer cells to 5-Fluorouracil [ J Cancer, 2021, 12(16):4862-4872] PubMed: 34234856
Exosomal IDH1 increases the resistance of colorectal cancer cells to 5-Fluorouracil [ Journal of Cancer, 2021, 12(16): 4862-4872] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.