1. PROTAC Neuronal Signaling GPCR/G Protein Apoptosis
  2. PROTACs Adrenergic Receptor Apoptosis
  3. PROTAC AR/AR-V7 degrader-1

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).

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

PROTAC AR/AR-V7 degrader-1 Chemical Structure

PROTAC AR/AR-V7 degrader-1 Chemical Structure

CAS No. : 2841308-96-9

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5 mg USD 480 In-stock
10 mg USD 768 In-stock
25 mg USD 1500 In-stock
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Based on 1 publication(s) in Google Scholar

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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)[1].

In Vitro

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].

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

Molecular Weight

485.43

Formula

C24H19F4N5O2

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C1C(C)(C)N(CCNC2=C(C=CC=N3)C3=C(F)C=C2)C(N1C4=CC(C(F)(F)F)=C(C#N)C=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (206.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0600 mL 10.3001 mL 20.6003 mL
5 mM 0.4120 mL 2.0600 mL 4.1201 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0600 mL 10.3001 mL 20.6003 mL 51.5007 mL
5 mM 0.4120 mL 2.0600 mL 4.1201 mL 10.3001 mL
10 mM 0.2060 mL 1.0300 mL 2.0600 mL 5.1501 mL
15 mM 0.1373 mL 0.6867 mL 1.3734 mL 3.4334 mL
20 mM 0.1030 mL 0.5150 mL 1.0300 mL 2.5750 mL
25 mM 0.0824 mL 0.4120 mL 0.8240 mL 2.0600 mL
30 mM 0.0687 mL 0.3433 mL 0.6867 mL 1.7167 mL
40 mM 0.0515 mL 0.2575 mL 0.5150 mL 1.2875 mL
50 mM 0.0412 mL 0.2060 mL 0.4120 mL 1.0300 mL
60 mM 0.0343 mL 0.1717 mL 0.3433 mL 0.8583 mL
80 mM 0.0258 mL 0.1288 mL 0.2575 mL 0.6438 mL
100 mM 0.0206 mL 0.1030 mL 0.2060 mL 0.5150 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PROTAC AR/AR-V7 degrader-1
Cat. No.:
HY-162412
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