TD-802
TD-802 is a CRBN-recruiting PROTAC androgen receptor (AR) degrader with liver microsomal stability and in vivo pharmacokinetic properties. TD-802 exhibits weak degrading activity against the AR-V7 splice variant, and its degradation process depends on the ubiquitin-proteasome system and Cullin-Ring ubiquitin ligase. TD-802 inhibits the proliferation of AR-dependent prostate cancer cells and the growth of AR-positive prostate cancer tumors in in vivo xenograft models.
(Pink: Androgen Receptor Target protein ligand; Blue: Cereblon E3 ligase ligand; Black: linker).
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- CAS No.: 2760703-21-5
- Formule: C52H61ClN10O6
- Masse moléculaire:957.56
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
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Cereblon |
AR-V7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | CC50 |
0.098 μM
Compound: 33c; TD-802
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Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability after 6 days by CellTiter-Glo assay
Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability after 6 days by CellTiter-Glo assay
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[PMID: 32961381] |
| VCaP | CC50 |
0.044 μM
Compound: 33c; TD-802
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Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 6 days by CellTiter-Glo assay
Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 6 days by CellTiter-Glo assay
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[PMID: 32961381] |
TD-802 (0.001-10 μM) potently induces androgen receptor degradation in LNCaP prostate cancer cells with a DC50 of 12.5 nM and a maximum degradation of 93%[1].
TD-802 (0.3 nM-10 μM; 6 days) inhibits proliferation of LNCaP prostate cancer cells with a CC50 of 0.098 μM and VCaP prostate cancer cells with a CC50 of 0.044 μM[1].
TD-802 (1 μM; 1-24 h) reduces androgen receptor levels in LNCaP prostate cancer cells by 80% within 4 hours of incubation[1].
TD-802 (1 μM; 30 min) demonstrates high stability in mouse liver microsomes, with 96.0% of the compound remaining after 30 minutes of incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP, VCaP prostate cancer cells
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Concentration:0.3 nM-10 μM
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Incubation Time:6 days
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Result:Exhibited a CC50 of 0.098 μM in LNCaP cells.
Exhibited a CC50 of 0.044 μM in VCaP cells.
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Cell Line:LNCaP prostate cancer cells
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Concentration:1 μM
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Incubation Time:1-24 h
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Result:Decreased AR levels by 80% after 4 h of incubation at 1 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB-17/IcrCrj-scid (male)[1]
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Dosage:30 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Reduced tumor growth compared to vehicle control.
Resulted in significantly lower tumor volume on the final study day (P = 0.0440 vs. control).
Caused no significant body weight loss or signs of morbidity/mortality.
Chemical Information
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CAS No. 2760703-21-5
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Masse moléculaire 957.56
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Formule C52H61ClN10O6
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SMILES
CC1([C@@H](C(C)([C@H]1OC2=CC(Cl)=C(C=C2)C#N)C)NC(C3=CC=C(C=C3)N4CCN(CC4)C5CC6(C5)CCN(CC6)C(C7CCN(CC7)C8=CC=C9N=NN(C(C9=C8)=O)C%10CCC(NC%10=O)=O)=O)=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TD-802 Related Classifications
HY-146397 Related Classifications
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