1. PROTAC Vitamin D Related/Nuclear Receptor Apoptosis
  2. PROTACs Androgen Receptor Apoptosis
  3. PROTAC AR Degrader-8

PROTAC AR Degrader-8 (Compound NP18) is the PROTAC degrader for androgen receptor (AR), that degrades AR-FL with DC50 of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model. (Pink: ligand for target protein AR ligand-33 (HY-170330); Black: linker (HY-W007731); Blue: ligand for E3 ligase Cereblon (HY-14658))

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

PROTAC AR Degrader-8 Chemical Structure

PROTAC AR Degrader-8 Chemical Structure

CAS No. : 3044108-04-2

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Based on 1 publication(s) in Google Scholar

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Description

PROTAC AR Degrader-8 (Compound NP18) is the PROTAC degrader for androgen receptor (AR), that degrades AR-FL with DC50 of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model[1]. (Pink: ligand for target protein AR ligand-33 (HY-170330); Black: linker (HY-W007731); Blue: ligand for E3 ligase Cereblon (HY-14658))

Molecular Weight

703.78

Formula

C40H41N5O7

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCOC4=CC=C(C(C)(C5=CC=C(OCC6=NC(N7CCOCC7)=CC=C6)C=C5)C)C=C4)=O

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Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (142.09 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 1.4209 mL 7.1045 mL 14.2090 mL
5 mM 0.2842 mL 1.4209 mL 2.8418 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. 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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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. 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 1.4209 mL 7.1045 mL 14.2090 mL 35.5225 mL
5 mM 0.2842 mL 1.4209 mL 2.8418 mL 7.1045 mL
10 mM 0.1421 mL 0.7104 mL 1.4209 mL 3.5522 mL
15 mM 0.0947 mL 0.4736 mL 0.9473 mL 2.3682 mL
20 mM 0.0710 mL 0.3552 mL 0.7104 mL 1.7761 mL
25 mM 0.0568 mL 0.2842 mL 0.5684 mL 1.4209 mL
30 mM 0.0474 mL 0.2368 mL 0.4736 mL 1.1841 mL
40 mM 0.0355 mL 0.1776 mL 0.3552 mL 0.8881 mL
50 mM 0.0284 mL 0.1421 mL 0.2842 mL 0.7104 mL
60 mM 0.0237 mL 0.1184 mL 0.2368 mL 0.5920 mL
80 mM 0.0178 mL 0.0888 mL 0.1776 mL 0.4440 mL
100 mM 0.0142 mL 0.0710 mL 0.1421 mL 0.3552 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 Degrader-8
Cat. No.:
HY-170329
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