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Purity: ≥98%
Ivosidenib (formerly known as AG-120 or RG-120; trade name: Tibsovo®) is a novel, small molecule, orally bioavailable inhibitor of mutated cytosolic isocitrate dehydrogenase 1 (IDH1) developed by Agios Pharmaceuticals and has been approved for the treatment of cancer in patients with IDH1 mutations. The mutated form of the IDH1 enzyme produces a metabolite, 2-hydroxyglutarate (2-HG), which is thought to play a role in the formation and progression of acute myeloid leukaemia (AML), gliomas and other cancers. Elevated 2-HG levels interfere with cellular metabolism and epigenetic regulation, thereby contributing to oncogenesis. Ivosidenib targets the IDH1 metabolic pathway to prevent a build-up of the oncometabolite 2-HG. On 7/20/2018, FDA approved Ivosidenib to treat patients with relapsed or refractory acute myeloid leukemia.
| ln Vitro |
Ivosidenib (AG-120) (0-13 μM; 48 hours) suppresses many IDH1-R132 mutants with comparable potency and IC50 values: IDH1-R132H (IC50=12 nM); IDH1-R132C (IC50=13 nM); IDH1-R132G (IC50=8 nM); IDH1-R132L (IC50=13 nM); and IDH1-R132S (IC50=12 nM), respectively [1].
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| ln Vivo |
Twelve hours after therapy, AG-120 (gavage delivery; 50 mg/kg and 150 mg/kg) produced maximal inhibition (92.0% and 95.2% at the 50 mg/kg and 150 mg/kg dosages, respectively) and rapidly decreased tumor 2-HG concentrations [1].
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| Animal Protocol |
Animal/Disease Models: Female BALB/c nude mice were inoculated with HT1080 cells [1]
Doses: 50 mg/kg and 150 mg/kg Route of Administration: intragastric (po) (po)administration; 50 mg/kg and 150 mg/kg Experimental Results: Mouse tumors were shown 2-HG was Dramatically diminished. |
| References |
[1]. Popovici-Muller J, et al. Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1Mutant Cancers. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305.
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| Molecular Formula |
C28H22CLF3N6O3
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|---|---|
| Molecular Weight |
582.97
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| CAS # |
1448347-49-6
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| Related CAS # |
(R,S)-Ivosidenib;2070009-31-1;IDH1 Inhibitor 8;1448346-63-1
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| SMILES |
O=C([C@H](CC1)N(C2=NC=CC(C#N)=C2)C1=O)N([C@@H](C3=CC=CC=C3Cl)C(NC4CC(F)(F)C4)=O)C5=CC(F)=CN=C5
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| Chemical Name |
(S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide
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| Synonyms |
RG-120; AG120; trade name: Tibsovo®, AG-120; AG 120; RG 120; RG120
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| 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)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (3.57 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (3.57 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7154 mL | 8.5768 mL | 17.1535 mL | |
| 5 mM | 0.3431 mL | 1.7154 mL | 3.4307 mL | |
| 10 mM | 0.1715 mL | 0.8577 mL | 1.7154 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.
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.
(2) Be sure to add the solvent(s) in order.
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