PROTAC AR Degrader-8

Name: PROTAC AR Degrader-8
Brand: MedChemExpress
SKU: HY-170329
Rating: 4.5 (1 reviews)

Cat. No.: HY-170329 Purity: 99.98%: Data Sheet
COA

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PROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC₅₀s 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 values 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. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer.
(Pink: Androgen Receptor ligand (HY-170330); Blue: Cereblon ligand (HY-14658); Black: linker).

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

PROTAC AR Degrader-8 Chemical Structure

CAS No. : 3044108-04-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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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Biological Activity
Purity & Documentation
References
Customer Review

Description

PROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC₅₀s 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 values 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. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer^[1]. (Pink: Androgen Receptor ligand (HY-170330); Blue: Cereblon ligand (HY-14658); Black: linker).

In Vitro

PROTAC AR Degrader-8 (NP18) (0.01-100 μM; 4 days) potently inhibits the viability of AR-dependent prostate cancer 22Rv1 and LNCaP cells with IC₅₀ values of 0.038 μM and 0.176 μM respectively, while showing weak activity against AR-independent and normal epithelial cells^[1].
PROTAC AR Degrader-8 (0.001-5 μM; 1 μM; 0-24 h) induces potent, time- and dose-dependent degradation of AR-FL in LNCaP cells (DC₅₀ = 0.14 μM) and both AR-FL (DC₅₀ = 0.018 μM) and AR-V7 (DC₅₀ = 0.026 μM) in 22Rv1 cells^[1].
PROTAC AR Degrader-8 (100 nM; 24 h) reduces nuclear localization and expression of both AR-FL and AR-V7 in 22Rv1 cells^[1].
PROTAC AR Degrader-8 (100-500 nM; 24 h) blocks the AR/AR-V7 signaling pathway in 22Rv1 cells by suppressing target gene expression without altering AR mRNA levels^[1].
PROTAC AR Degrader-8 (100 nM; 12 h) induces AR-FL and AR-V7 degradation in 22Rv1 cells via a CRBN-dependent ubiquitin-proteasome system^[1].
PROTAC AR Degrader-8 (0.001-5 μM; 24 h) selectively degrades AR-FL and AR-V7 in 22Rv1 cells without affecting homologous nuclear receptor proteins^[1].
PROTAC AR Degrader-8 (1-100 nM; 14 days) potently inhibits long-term colony formation of 22Rv1 prostate cancer cells in a dose-dependent manner^[1].
PROTAC AR Degrader-8 (100-500 nM; 48 h) dose-dependently induces apoptosis in 22Rv1 prostate cancer cells, with apoptosis rates of 26.86% at 100 nM and 32.51% at 500 nM^[1].
PROTAC AR Degrader-8 (100-500 nM; 24 h) induces G2/M phase cell cycle arrest in 22Rv1 prostate cancer cells, with 15.45% and 21.54% of cells in G2/M at 100 nM and 500 nM respectively^[1].
PROTAC AR Degrader-8 (0.1-10 μM) has an excellent hERG safety profile, with minimal inhibition of hERG channels even at 10 μM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	22Rv1, LNCaP, DU-145, RWPE-1, MCF-10A
Concentration:	0.01 μM; 0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time:	4 days
Result:	Inhibited 22Rv1 cell viability with an IC₅₀ of 0.038 μM. Inhibited LNCaP cell viability with an IC₅₀ of 0.176 μM. Showed IC₅₀ values >80 μM for DU-145, RWPE-1, and MCF-10A cells.

Immunofluorescence^[1]

Cell Line:	22Rv1
Concentration:	100 nM
Incubation Time:	24 h
Result:	Caused a significant decrease in both nuclear localization and expression levels of AR-FL and AR-V7.

Real Time qPCR^[1]

Cell Line:	22Rv1
Concentration:	100 nM, 500 nM
Incubation Time:	24 h
Result:	Dose-dependently suppressed the expression of PSA, TMPRSS2, KLK2, and UBE2C genes. Showed no significant alteration of AR mRNA levels at either 100 nM or 500 nM concentration.

Western Blot Analysis^[1]

Cell Line:	22Rv1
Concentration:	100 nM
Incubation Time:	12 h
Result:	Had its induced degradation of AR-FL and AR-V7 significantly blocked by nNP18, thalidomide, MLN4924, and MG132.

Western Blot Analysis^[1]

Cell Line:	22Rv1
Concentration:	0.001 μM, 0.005 μM, 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM
Incubation Time:	24 h
Result:	Showed no obvious degradation of ERα, GR, PR, or PPARγ at concentrations effective for AR-FL and AR-V7 degradation.

Cell Proliferation Assay^[1]

Cell Line:	22Rv1
Concentration:	1, 10, 100 nM
Incubation Time:	14 days
Result:	Dose-dependently reduced colony formation of 22Rv1 cells, with a significant reduction at 100 nM.

Apoptosis Analysis^[1]

Cell Line:	22Rv1
Concentration:	100 nM, 500 nM
Incubation Time:	48 h
Result:	Induced apoptosis in 22Rv1 cells at a rate of 26.86% (100 nM) and 32.51% (500 nM).

Cell Cycle Analysis^[1]

Cell Line:	22Rv1
Concentration:	100 nM, 500 nM
Incubation Time:	24 h
Result:	Increased accumulation of 22Rv1 cells in the G2/M phase, with percentages of 15.45% (100 nM) and 21.54% (500 nM) compared to 8.61% in the vehicle group.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	C₀	V_ss	V_z	CL
Rat^[1]	2 mg/kg	i.v.	2.64 h	0.083 h	6443.30 ng/mL	2208.53 ng·h/mL	2220.92 ng·h/mL	0.54 h	0.62 h	13935.03 ng/mL	571.03 mL/kg	3570.81 mL/kg	904.46 mL/h/kg

In Vivo

PROTAC AR Degrader-8 (NP18) (10 mg/kg; i.p.; once daily; 21 days) significantly suppresses 22Rv1 prostate cancer xenograft growth in BALB/c-nu mice, reducing tumor growth rate to 67% of controls, while maintaining a favorable safety profile^[1].
PROTAC AR Degrader-8 (25-50 ng per zebrafish; yolk sac injection) exerts a dose-dependent inhibitory effect on prostate cancer patient-derived xenografts in zebrafish, with near-complete ablation of tumor fluorescence at the 50 ng dose^[1].

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

Animal Model:	BALB/c-nu nude mice (male, 6-8 weeks old, 18-22 g) injected with 22Rv1 cells^[1]
Dosage:	10 mg/kg
Administration:	i.p.; once daily; 21 days
Result:	Reduced tumor growth rate to 67% of control levels. Significantly degraded AR-FL and AR-V7 proteins in tumor tissue. Caused no marked pathological damage in heart, liver, spleen, lung, or kidney tissues. Increased mouse body weight steadily during treatment.

Molecular Weight

703.78

Formula

C₄₀H₄₁N₅O₇

CAS No.

3044108-04-2

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

Shipping

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
10 mM	0.1421 mL	0.7104 mL	1.4209 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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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (246 KB) HNMR (233 KB) RP-HPLC (257 KB) LCMS (108 KB)

Handling Instructions (2659 KB)

References

[1]. Ha S, et al. Discovery of a highly potent, N-terminal domain-targeting degrader of AR-FL/AR-V7 for the treatment of prostate cancer. Eur J Med Chem. 2025;282:117079. [Content Brief]

Complete Stock Solution Preparation Table

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