AKN-028
Based on 1 Customer Validation
AKN-028, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.72%
- No. CAS: 1175017-90-9
- Fòrmula: C17H14N6
- Peso molecular:302.33
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
IC50: 6 nM (FLT3), 140 nM (CLK1), 220 nM (RPS6KA), 520 nM (VEGFR2), and 120 nM (FGFR2)[1]
AKN-028 (0.1 nM-100 μM; 15 h; mouse embryonal fibroblasts and human acute megakaryoblastic leukemia M07 cells) inhibits FLT3 and KIT autophosphorylation in a dose-dependent manner[1].
AKN-028 (10 μM; 72 h; tumor cell lines) is cytotoxic to AML cell lines and induces apoptosis in the AML cell line MV4-11[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse embryonal fibroblasts either overexpressing FLT-wt, FLT3-TKD or FLT3-ITD and human acute megakaryoblastic leukemia M07 cells overexpressing KIT
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Concentration:0.1 nM-100 μM
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Incubation Time:15 hours
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Result:Inhibited FLT3 and KIT autophosphorylation.
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Cell Line:Tumor cell lines
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Concentration:10 μM
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Incubation Time:72 hours
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Result:Had cytotoxic activity was highest in MV4-11 and MOLM-13 (IC50<50 nM), followed by the three other AML cell lines (IC50=0.5-6 μM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57 black mice with MV4-11 xenografts[1]
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Dosage:15 mg/kg
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Administration:Subcutaneous injection; twice daily, for 6 days
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Result:Inhibited tumor growth and did not affect body weight.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1175017-90-9
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Appearance Solid
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Peso molecular 302.33
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Fòrmula C17H14N6
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Color Light brown to brown
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SMILES
NC1=NC=C(N=C1NC2=CC3=C(C=C2)NC=C3)C4=CC=NC=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AKN-028 Related Classifications
HY-118304 Related Classifications
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