2. Cell Cycle/DNA Damage
  3. Eukaryotic Initiation Factor (eIF)
  4. APL-4098

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. APL-4098 reduces the phosphorylation level of eIF2α and the expression level of ATF4. APL-4098 impairs mitochondrial function and exerts cytotoxic effects on primary acute myeloid leukemia cells. APL-4098 is applicable to research related to acute myeloid leukemia.

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APL-4098

APL-4098 Chemical Structure

CAS No. : 2752441-61-3

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APL-4098 Related Antibodies

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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. APL-4098 reduces the phosphorylation level of eIF2α and the expression level of ATF4. APL-4098 impairs mitochondrial function and exerts cytotoxic effects on primary acute myeloid leukemia cells. APL-4098 is applicable to research related to acute myeloid leukemia[1].

IC50 & Target[1]

eIF2

 

In Vitro

APL-4098 (0.012-1 μmol/L; 4 h) dose-dependently reduces eIF2α phosphorylation and ATF4 protein expression in glutamine-deprived U2OS osteosarcoma cells[1].
APL-4098 (100 nmol/L, 300 nmol/L, 1 μmol/L) induces cell death ex vivo in primary patient-derived AML cells (cohort 2), including cytotoxic effects on the LSC-enriched CD34+/CD38- subpopulation in some samples[1].
APL-4098 (250 nmol/L; 6, 18, 24 h) reduces mitochondrial membrane potential in MOLM-16 AML cells after 6, 18, and 24 hours of treatment[1].
APL-4098 (up to 1 μmol/L; 24 h) dose-dependently inhibits mitochondrial respiration (including basal and maximal OCR) in MOLM-16 AML cells after 24 hours of treatment[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

APL-4098 Related Antibodies
Parmacokinetics
Species Dose Route CL Vd T1/2 Bioavailability
Rat[1] 1 mg/kg i.v. 0.08 mL/min/kg 0.11 L/kg 18.1 h /
Rat[1] 3 mg/kg p.o. / / / 66 %
In Vivo

APL-4098 (0.5-5 mg/kg; p.o.; once daily; for 11 consecutive days) induces dose-dependent tumor growth inhibition in a subcutaneous AML CDX model[1].
APL-4098 (15 mg/kg; p.o.; once daily; for 19 consecutive days) selectively eliminates the LSC-enriched CD34+/CD38− subset in patient-derived AML PDX models, while exerting minimal effects on the overall leukemia burden[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD/SCID (female, 6-8 weeks old, subcutaneous AML CDX model)[1]
Dosage: 0.5 mg/kg; 1.5 mg/kg; 5 mg/kg
Administration: p.o.; once daily; 11 days
Result: Achieved 46.2% TGI at 0.5 mg/kg with low unbound plasma exposure.
Showed intermediate TGI at 1.5 mg/kg with increased unbound plasma exposure.
Reached 98.3% TGI at 5 mg/kg with the highest unbound plasma exposure.
Caused no notable consistent adverse events, including no relevant effect on body weight or survival.
Animal Model: NOG (female, 6-8 weeks old, patient-derived AML PDX model)[1]
Dosage: 15 mg/kg
Administration: p.o.; once daily; 19 days
Result: Exerted minimal effect on bulk leukemia (percentage of viable hCD45+ cells).
Pronounced and selectively depleted the LSC-enriched CD34+/CD38- subpopulation, significantly reducing cell numbers relative to vehicle control.
Caused no apparent cytotoxicity in experimental animals.
Molecular Weight

434.83

Formula

C17H12ClFN6O3S
CAS No.
SMILES

COC1=C(C=C(C=N1)Cl)S(=O)(NC2=NC=CC(C#CC3=CN=C(N=C3)N)=C2F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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APL-4098 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

APL-40982752441-61-3APL4098APL 4098Eukaryotic Initiation Factor (eIF)patient-derived xenograft modelsmitochondrial functionCD34+/CD38- subpopulationMOLM-16 AML cellsGCN2cell line-derived xenograft modelsacute myeloid leukemia cellseIF2αATF4mitochondrial oxidative phosphorylationInhibitorinhibitorinhibit

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