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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.37%
- CAS 番号: 491586-42-6
- 分子式: C19H17N3O2
- 分子量:319.36
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Eukaryotic Release Factor (eRF) アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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 |
体外実験
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.
化学情報
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CAS 番号 491586-42-6
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性状 Solid
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分子量 319.36
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AN5777 関連分類
HY-161696 関連分類
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