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.
For research use only. We do not sell to patients.
- CAS No.: 3079716-11-0
- Formula: C22H22FN3O4
- Molecular Weight:411.43
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 22Rv1 | EC50 |
0.042 μM
|
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.
|
41735331 |
| HCC1143 | EC50 |
0.132 μM
|
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.
|
41735331 |
| LS-411N | EC50 |
0.021 μM
|
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.
|
41735331 |
| MCF7 | EC50 |
0.096 μM
|
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.
|
41735331 |
| MRC5 | EC50 |
0.331 μM
|
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.
|
41735331 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF7 breast cancer cells
-
Concentration:1 μM (15 min-8 h incubations); 10 μM (<4 h incubation)
-
Incubation Time:15 min, 30 min, 1 h, 2 h, 4 h, 8 h (1 μM); <4 h (10 μM)
-
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude mice (female, 6-8 weeks old)[1]
-
Dosage:3 mg/kg; 10 mg/kg
-
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)
-
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
-
CAS No. 3079716-11-0
-
Molecular Weight 411.43
-
Formula C22H22FN3O4
-
SMILES
FC1=CC=CC(CNC(O[C@H]([C@H](CN2)O)[C@H]2CC3=CC=C(C4=CN=CO4)C=C3)=O)=C1
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)