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Art. -Nr.: HY-146397

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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. Nr.: 2760703-21-5
Formel: C₅₂H₆₁ClN₁₀O₆
Molecular Weight:957.56

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

TD-802 Chemical Structure

CAS. Nr.: 2760703-21-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: Androgen Receptor Target protein ligand; Blue: Cereblon E3 ligase ligand; Black: linker).

IC₅₀ & Target^[1]

Cereblon

AR-V7

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	CC₅₀	0.098 μM Compound: 33c; TD-802	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	[PMID: 32961381]
VCaP	CC₅₀	0.044 μM Compound: 33c; TD-802	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	[PMID: 32961381]

In Vitro

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.

Cell Proliferation Assay^[1]

Cell Line:

LNCaP, VCaP prostate cancer cells
Concentration:

0.3 nM-10 μM
Incubation Time:

6 days
Result:

Exhibited a CC₅₀ of 0.098 μM in LNCaP cells.
Exhibited a CC₅₀ of 0.044 μM in VCaP cells.

Western Blot Analysis^[1]

Cell Line:

LNCaP prostate cancer cells
Concentration:

1 μM
Incubation Time:

1-24 h
Result:

Decreased AR levels by 80% after 4 h of incubation at 1 μM.

In Vivo

TD-802 (30 mg/kg; i.p.; daily; 10 days) significantly inhibits the growth of VCaP prostate cancer xenografts in male SCID mice without causing measurable body weight loss^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CB-17/IcrCrj-scid (male)^[1]
Dosage:

30 mg/kg
Administration:

i.p.; daily; 10 days
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

CAS. Nr. 2760703-21-5
Molecular Weight 957.56
Formel C₅₂H₆₁ClN₁₀O₆
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Takwale AD, et al. Design and characterization of cereblon-mediated androgen receptor proteolysis-targeting chimeras. European journal of medicinal chemistry. 2020 Dec 15;208:112769. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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TD-802

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

TD-802 Related Classifications

HY-146397 Related Classifications