Ivosidenib [1448347-49-6]
Cat# HY-18767-5mg
Size : 5mg
Brand : MedChemExpress
Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity.
For research use only. We do not sell to patients.
Ivosidenib Chemical Structure
CAS No. : 1448347-49-6
Based on 10 publication(s) in Google Scholar
Other Forms of Ivosidenib:
- (R,S)-Ivosidenib In-stock
- IDH1 Inhibitor 8 In-stock
View All Isocitrate Dehydrogenase (IDH) Isoform Specific Products:
Description |
Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity[1]. |
IC50 & Target |
12 nM (mouse IDH1R132H)[1] |
||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
In Vitro |
Ivosidenib (AG-120) (0-13 μM; 48 hours) inhibits several IDH1-R132 mutants with potency similar IC50 values: IDH1-R132H (IC50=12 nM); IDH1-R132C (IC50=13 nM); IDH1-R132G (IC50=8 nM); IDH1-R132L (IC50=13 nM); IDH1-R132S (IC50=12 nM), respectively[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
In Vivo |
AG-120 (gavage administration; 50 mg/kg and 150 mg/kg) declines tumor 2-HG concentration rapidly, with maximum inhibition (92.0% and 95.2% at the 50 mg/kg and 150 mg/kg doses, respectively) achieved at -12 h post dose[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
|
||||||||||||
Clinical Trial |
|
||||||||||||
Molecular Weight |
582.96 |
||||||||||||
Formula |
C28H22ClF3N6O3 |
||||||||||||
CAS No. |
1448347-49-6 |
||||||||||||
Appearance |
Solid |
||||||||||||
Color |
White to off-white |
||||||||||||
SMILES |
ClC1=C([C@H](N(C2=CC(F)=CN=C2)C([C@H]3N(C4=NC=CC(C#N)=C4)C(CC3)=O)=O)C(NC5CC(F)(F)C5)=O)C=CC=C1 |
||||||||||||
Shipping | Room temperature in continental US; may vary elsewhere. |
||||||||||||
Storage |
|
||||||||||||
Solvent & Solubility |
In Vitro:
DMSO : ≥ 39 mg/mL (66.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) *"≥" means soluble, but saturation unknown. Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
|
||||||||||||
Purity & Documentation | |||||||||||||
References |
|
Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
---|
DMSO | 1 mM | 1.7154 mL | 8.5769 mL | 17.1538 mL | 42.8846 mL |
5 mM | 0.3431 mL | 1.7154 mL | 3.4308 mL | 8.5769 mL | |
10 mM | 0.1715 mL | 0.8577 mL | 1.7154 mL | 4.2885 mL | |
15 mM | 0.1144 mL | 0.5718 mL | 1.1436 mL | 2.8590 mL | |
20 mM | 0.0858 mL | 0.4288 mL | 0.8577 mL | 2.1442 mL | |
25 mM | 0.0686 mL | 0.3431 mL | 0.6862 mL | 1.7154 mL | |
30 mM | 0.0572 mL | 0.2859 mL | 0.5718 mL | 1.4295 mL | |
40 mM | 0.0429 mL | 0.2144 mL | 0.4288 mL | 1.0721 mL | |
50 mM | 0.0343 mL | 0.1715 mL | 0.3431 mL | 0.8577 mL | |
60 mM | 0.0286 mL | 0.1429 mL | 0.2859 mL | 0.7147 mL |
Ivosidenib Related Classifications
- Metabolic Enzyme/Protease
- Isocitrate Dehydrogenase (IDH)