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Cat. No.: HY-163641

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AR Degrader-1

AR Degrader-1 is a molecular glue degrader targeting the androgen receptor (AR). AR Degrader-1 induces androgen receptor degradation by recruiting the DCAF16 E3 ligase substrate receptor, thereby triggering ubiquitination and proteasomal degradation. AR Degrader-1 exhibits relatively selective degradation of the androgen receptor in prostate cancer cells, reducing the levels of only a small number of other proteins. AR Degrader-1 can be used in studies related to prostate cancer.

For research use only. We do not sell to patients.

Formula: C₂₄H₂₇ClN₆O₄S
Molecular Weight:531.03

Storage:

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

Data Sheet (274 KB)

AR Degrader-1 Chemical Structure

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Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

In Vitro

AR Degrader-1 (ML 2–9) (0.1-10 μM; 24 h) induces dose-dependent degradation of androgen receptor in LNCaP prostate cancer cells, with a hook effect at 10 μM^[1].
AR Degrader-1 (10 μM; 24 h) induces selective degradation of androgen receptor in LNCaP prostate cancer cells, with only 7 off-target proteins reduced by >2-fold at 10 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:

LNCaP prostate cancer cells
Concentration:

0.1 μM; 1 μM; 5 μM; 10 μM
Incubation Time:

24 h
Result:

Significantly degraded androgen receptor in LNCaP cells, with a hook effect observed at the highest concentration tested.

Chemical Information

Molecular Weight 531.03
Formula C₂₄H₂₇ClN₆O₄S
SMILES

O=C(C1=NN=C(N2CCN(S(=O)(C=C)=O)CC2)C=C1)N[C@H]3CC[C@H](OC4=CC=C(C#N)C(Cl)=C4)CC3
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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)

References

[1]. Lim M, et al. DCAF16-Based Covalent Handle for the Rational Design of Monovalent Degraders. ACS central science. 2024 Jul 24;10(7):1318-1331. [Content Brief]

Calculators

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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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100 mg

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