GLPBio

PROTAC AR/AR-V7 degrader-1

Catalog No.: GC73996Purity:>98.00%
PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively.

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PROTAC AR/AR-V7 degrader-1
Cas No.: 2841308-96-9
1 mgIn Stock
$135.00
1
5 mgIn Stock
$346.00
1

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    187(9):2288-2304 (2024)
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Description

PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker).

PROTAC AR/AR-V7 degrader-1 (27c) effectively suppresses transcriptional activity of the AR signaling pathway. PROTAC AR/AR-V7 degrader-1 (27c) exhibits an IC50 of 0.9 μM in 22RV1 cells[1].PROTAC AR/AR-V7 degrader-1 (27c) overcomes drug resistance in advanced PCa expressing AR splice variants[1].

References:
[1]. Maoxu Xiao, et al. Structure–Activity Relationship (SAR) Studies of Novel Monovalent AR/AR-V7 Dual Degraders with Potent Efficacy against Advanced Prostate Cancer. J. Med. Chem. 2024, 67, 7, 5567-5590.

Product Documents

Purity:>98.00%Appearance:A solid

Chemical Properties

CAS No.
2841308-96-9
Molecular Formula
C24H19F4N5O2
Molecular Weight
485.43
Solubility
DMSO : ≥ 100 mg/mL (206.00 mM)
Storage
4°C, protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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