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APL-4098
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Catalog No. T218287 Copy Product Info
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APL-4098 is an orally active, selective, ATP-competitive GCN2 inhibitor with a Ki of 4.39 nM and a Kd of 2.9 nM. It reduces the phosphorylation levels of eIF2α and the expression of ATF4. APL-4098 impairs mitochondrial function and exhibits cytotoxicity against primary acute myeloid leukemia cells. It is applicable in studies related to acute myeloid leukemia.
APL-4098
Cas No. 2752441-61-3
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | APL-4098 is an orally active, selective, ATP-competitive GCN2 inhibitor with a Ki of 4.39 nM and a Kd of 2.9 nM. It reduces the phosphorylation levels of eIF2α and the expression of ATF4. APL-4098 impairs mitochondrial function and exhibits cytotoxicity against primary acute myeloid leukemia cells. It is applicable in studies related to acute myeloid leukemia. |
| In vitro | APL-4098 reduces phosphorylation levels of eIF2α and expression of ATF4 protein in a dose-dependent manner in glutamine-deprived U2OS osteosarcoma cells when used at concentrations of 0-1 μM for 4 hours. At concentrations of 0.1-1 μM, it induces cell death in primary AML patient cells in vitro and exhibits cytotoxic effects on the leukemia stem cell (LSC)-enriched CD34+/CD38- subpopulation in certain samples. Additionally, APL-4098 at 250 nM for 6-24 hours decreases mitochondrial membrane potential in MOLM-16 acute myeloid leukemia (AML) cells. At 0-1 μM for 24 hours, it also dose-dependently inhibits mitochondrial respiration in MOLM-16 AML cells. |
| In vivo | APL-4098, administered orally at doses of 0.5-5 mg/kg once daily for 11 consecutive days, induces dose-dependent tumor growth inhibition in a subcutaneous AML CDX model. When given at 15 mg/kg orally once daily for 19 days, APL-4098 selectively eradicates the LSC-enriched CD34+/CD38− subpopulation in a patient-derived AML PDX model, with minimal impact on overall leukemia burden. |
| Molecular Weight | 434.83 |
| Formula | C17H12ClFN6O3S |
| Cas No. | 2752441-61-3 |
| Smiles | O=S(=O)(NC1=NC=CC(C#CC2=CN=C(N=C2)N)=C1F)C3=CC(Cl)=CN=C3OC |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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Related Tags: APL-4098 in vivo | APL-4098 in vitro | APL-4098 formula | APL-4098 molecular weight
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