AN5777
Based on 1 Customer Validation
AN5777 is a GSPT1 Molecular glue degrader with a DC50 of less than 10 μM. AN5777 degrades GSPT1 in a CRBN-dependent manner via the ubiquitin-proteasome system. AN5777 induces G1 phase arrest and Apoptosis in cancer cells. AN5777 is applicable to research related to acute myeloid leukemia, multiple myeloma, and chronic myeloid leukemia.
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- Pureza : 98.37%
- No. CAS: 491586-42-6
- Fòrmula: C19H17N3O2
- Peso molecular:319.36
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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
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Chemical Information
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Ver todos los productos específicos de isoformas Eukaryotic Release Factor (eRF)
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
eRF3a/GSPT1 ＜10 μM (DC50) |
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-266 | IC50 |
3.8 μM
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Antiproliferative activity against human multiple myeloma U266 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay.
Antiproliferative activity against human multiple myeloma U266 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay.
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38795517 |
| U-937 | IC50 |
4.49 μM
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Antiproliferative activity against human myeloid leukemia U937 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay.
Antiproliferative activity against human myeloid leukemia U937 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay.
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38795517 |
| K562 | IC50 |
16.74 μM
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Antiproliferative activity against human chronic myeloid leukemia K562 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay.
Antiproliferative activity against human chronic myeloid leukemia K562 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay.
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38795517 |
| OCI-AML2 | IC50 |
2.64 μM
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Antiproliferative activity against human acute myeloid leukemia OCI-AML-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay.
Antiproliferative activity against human acute myeloid leukemia OCI-AML-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay.
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38795517 |
In Vitro
AN5777 (48 h) potently inhibits the proliferation of U266, U937, and OCI-AML-2 cells, with the strongest activity against OCI-AML-2 cells (IC50 = 2.64 μM), and exhibits moderate activity against K562 cells (IC50 = 16.74 μM)[1].
AN5777 (5-40 μM; 8 h) preferentially downregulates GSPT1 protein levels in a dose-dependent manner in U937 and OCI-AML-2 cells after 8 h of treatment[1].
AN5777 (20-40 μM; 8 h) induces GSPT1 degradation in U937, OCI-AML-2, and 293FT cells through the ubiquitin-proteasome system, dependent on the CRL4CRBN complex[1].
AN5777 (5-20 μM; 24 h) induces dose-dependent G1 phase arrest in U937 and OCI-AML-2 cells after 24 h of treatment, associated with upregulated P21 and downregulated C-Myc[1].
AN5777 degrades GSPT1 in a CRBN-dependent manner, inhibits proliferation of OCI-AML-2 and U937 acute myeloid leukemia cells with IC50 values of 2.64 μM and 4.49 μM respectively, and induces G1 phase arrest and apoptosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human multiple myeloma U266 cells, human myeloid leukemia U937 cells, human chronic myeloid leukemia K562 cells, human acute myeloid leukemia OCI-AML-2 cells
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Concentration:range of concentrations
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Incubation Time:48 h
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Result:Inhibited proliferation of U266 cells with an IC50 of 3.8 μM.
Inhibited proliferation of U937 cells with an IC50 of 4.49 μM.
Inhibited proliferation of K562 cells with an IC50 of 16.74 μM.
Inhibited proliferation of OCI-AML-2 cells with an IC50 of 2.64 μM.
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Cell Line:human myeloid leukemia U937 cells, human acute myeloid leukemia OCI-AML-2 cells
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Concentration:10 μM; 5-40 μM
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Incubation Time:8 h
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Result:Reduced GSPT1 protein levels in both U937 and OCI-AML-2 cells at 10 μM for 8 h.
Induced dose-dependent downregulation of GSPT1 at concentrations from 5 to 40 μM for 8 h.
Caused weaker downregulation of IKZF1 and CK1α at higher concentrations, indicating preferential targeting of GSPT1.
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Cell Line:human myeloid leukemia U937 cells, human acute myeloid leukemia OCI-AML-2 cells
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Concentration:5-20 μM
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Incubation Time:24 h
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Result:Increased the proportion of cells in G1 phase and decreased the proportion in G2/M phase in both U937 and OCI-AML-2 cells in a dose-dependent manner.
Increased levels of the cell cycle inhibitor P21 and reduced levels of C-Myc, confirmed via Western blot analysis.
Chemical Information
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No. CAS 491586-42-6
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Appearance Solid
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Peso molecular 319.36
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Fòrmula C19H17N3O2
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Color Off-white to gray
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SMILES
CC1=C(N=C(C)C(C(N/N=C/C2=CC=CC=C2O)=O)=C3)C3=CC=C1
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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 (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AN5777 Related Classifications
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