1. PROTAC Vitamin D Related/Nuclear Receptor
  2. PROTACs Androgen Receptor
  3. PROTAC AR-V7 degrader-1

PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM.

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

PROTAC AR-V7 degrader-1 Chemical Structure

PROTAC AR-V7 degrader-1 Chemical Structure

CAS No. : 2767440-24-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 825 In-stock
Solution
10 mM * 1 mL in DMSO USD 825 In-stock
Solid
5 mg USD 590 In-stock
10 mg USD 950 In-stock
25 mg USD 1850 In-stock
50 mg USD 3000 In-stock
100 mg USD 4800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM[1].

IC50 & Target[1]

VHL

 

Molecular Weight

789.02

Formula

C41H52N6O6S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CCCCOC1=CC=C(C2=CSC(N3CCOCC3)=N2)C=C1)N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(N[C@H](C5=CC=C(C=C5)C6=C(N=CS6)C)C)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (139.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2674 mL 6.3370 mL 12.6740 mL
5 mM 0.2535 mL 1.2674 mL 2.5348 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 1.2674 mL 6.3370 mL 12.6739 mL 31.6849 mL
5 mM 0.2535 mL 1.2674 mL 2.5348 mL 6.3370 mL
10 mM 0.1267 mL 0.6337 mL 1.2674 mL 3.1685 mL
15 mM 0.0845 mL 0.4225 mL 0.8449 mL 2.1123 mL
20 mM 0.0634 mL 0.3168 mL 0.6337 mL 1.5842 mL
25 mM 0.0507 mL 0.2535 mL 0.5070 mL 1.2674 mL
30 mM 0.0422 mL 0.2112 mL 0.4225 mL 1.0562 mL
40 mM 0.0317 mL 0.1584 mL 0.3168 mL 0.7921 mL
50 mM 0.0253 mL 0.1267 mL 0.2535 mL 0.6337 mL
60 mM 0.0211 mL 0.1056 mL 0.2112 mL 0.5281 mL
80 mM 0.0158 mL 0.0792 mL 0.1584 mL 0.3961 mL
100 mM 0.0127 mL 0.0634 mL 0.1267 mL 0.3168 mL
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PROTAC AR-V7 degrader-1 Related Classifications

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-V7 degrader-1
Cat. No.:
HY-145479
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