Ivosidenib [1448347-49-6]

Katalog-Nummer T3617-25mg

Size : 25mg

Marke : TargetMol


Ivosidenib

(Synonyms: AG-120) Copy Product Info
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Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. It specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of the oncometabolite 2-hydroxyglutarate (2 hG), which may induce cellular differentiation and inhibit cellular proliferation in IDH1-expressing tumor cells.
Ivosidenib
Cas No. 1448347-49-6
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.98%
ee:99.97%
Color:White
COA HNMR CSFC LCMS

Product Information

Bioactivity
Description
Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. It specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of the oncometabolite 2-hydroxyglutarate (2 hG), which may induce cellular differentiation and inhibit cellular proliferation in IDH1-expressing tumor cells.
Targets & IC50
IDH1 (R132H):12 nM
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].
SynonymsAG-120
Cell Research
TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120. (Only for Reference)
Chemical Properties
Molecular Weight582.961
FormulaC28H22ClF3N6O3
Cas No.1448347-49-6
SmilesFC1=CN=CC(=C1)N([C@H](C(=O)NC1CC(F)(F)C1)C1=CC=CC=C1Cl)C(=O)[C@@H]1CCC(=O)N1C1=NC=CC(=C1)C#N
Relative Density.1.51 g/cm3 (Predicted)
Storage & Solubility Information
StorageStore at low temperature Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 100.00 mg/mL (171.54 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 237.00 mg/mL (406.55 mM), Sonication is recommended.
In Vivo Formulation
20% Cremophor EL: 5.50 mg/mL (9.43 mM)
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.7154 mL8.5769 mL17.1538 mL85.7690 mL
5 mM0.3431 mL1.7154 mL3.4308 mL17.1538 mL
10 mM0.1715 mL0.8577 mL1.7154 mL8.5769 mL
20 mM0.0858 mL0.4288 mL0.8577 mL4.2885 mL
50 mM0.0343 mL0.1715 mL0.3431 mL1.7154 mL
100 mM0.0172 mL0.0858 mL0.1715 mL0.8577 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.