IDB-003
IDB-003 is an orally active inhibitor of the human ribosomal peptidyl transferase center (PTC). IDB-003 exhibits antiproliferative activity against MYC-dependent cancer cells. IDB-003 binds to PTC, maintains ribosomal RNA interactions, blocks translation via context-dependent nascent polypeptide chain interactions, depletes MYC and CCND1, activates JNK phosphorylation through ribosomal collision, and downregulates the MYC target pathway. IDB-003 inhibits the growth of triple-negative breast cancer xenografts in mice. IDB-003 can be used for the research of triple-negative breast cancer.
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- No. CAS: 3079716-11-0
- Fòrmula: C22H22FN3O4
- Peso molecular:411.43
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 22Rv1 | EC50 |
0.042 μM
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Antiproliferative activity against human 22Rv1 prostate cancer cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor assay.
Antiproliferative activity against human 22Rv1 prostate cancer cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor assay.
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41735331 |
| HCC1143 | EC50 |
0.132 μM
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Antiproliferative activity against human HCC-1143 triple-negative breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor assay.
Antiproliferative activity against human HCC-1143 triple-negative breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor assay.
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41735331 |
| LS-411N | EC50 |
0.021 μM
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Antiproliferative activity against human LS411N colorectal cancer cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor assay.
Antiproliferative activity against human LS411N colorectal cancer cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor assay.
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41735331 |
| MCF7 | EC50 |
0.096 μM
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Antiproliferative activity against human MCF7 HR+/HER2- breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor assay.
Antiproliferative activity against human MCF7 HR+/HER2- breast cancer cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor assay.
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41735331 |
| MRC5 | EC50 |
0.331 μM
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Antiproliferative activity against human MRC5 fibroblast cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor assay.
Antiproliferative activity against human MRC5 fibroblast cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor assay.
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41735331 |
IDB-003 (72 h) potently inhibits the proliferation of 22Rv1, HCC-1143, LS411N and MCF7 cancer cells (EC50 values 0.021-0.132 μM), while exhibits weak activity against MRC5 fibroblasts (EC50 0.331 μM)[1].
IDB-003 (1-10 μM; 2 h-<4 h) depletes the short-lived oncoproteins MYC and CCND1 in MCF7 cells: this depletion is achieved within 2-4 h at treatment concentrations of 1 μM and 10 μM, respectively, without altering the levels of the long-lived proteins CDK4 and tubulin[1].
IDB-003 (2-72 h) depletes MYC protein in HCC-1143 cells in a concentration-dependent manner within 2 h, which correlates with reduced cell viability after 72 h of treatment[1].
IDB-003 (1.27 μM; 60 min) induces context-dependent translation arrest in HCC-1143 cells, preferentially targeting nascent polypeptide chains with an aliphatic residue at position −1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 breast cancer cells
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Concentration:1 μM (15 min-8 h incubations); 10 μM (<4 h incubation)
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Incubation Time:15 min, 30 min, 1 h, 2 h, 4 h, 8 h (1 μM); <4 h (10 μM)
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Result:Depleted CCND1 rapidly (evident by 1-2 h) and reduced MYC levels (observable after 2 h) at 1 μM.
Depleted MYC rapidly within <4 hours at 10 μM.
Left abundance of longer-lived proteins CDK4 and tubulin stable over the same time course.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, 6-8 weeks old)[1]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:p.o.; twice daily; 28 days (3 mg/kg); p.o.; twice daily; 11 days, followed by 2-day holiday, then resuming twice daily for remainder of 28 days (10 mg/kg)
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Result:Achieved 58% tumor growth inhibition (TGI) compared to vehicle control.
Achieved 80% tumor growth inhibition (TGI) compared to vehicle control.
Downregulated MYC targets v1 pathway as the most significantly altered pathway in endpoint tumor samples.
Chemical Information
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No. CAS 3079716-11-0
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Peso molecular 411.43
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Fòrmula C22H22FN3O4
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SMILES
FC1=CC=CC(CNC(O[C@H]([C@H](CN2)O)[C@H]2CC3=CC=C(C4=CN=CO4)C=C3)=O)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IDB-003 Related Classifications
HY-186311 Related Classifications
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