BWA-522

Name: BWA-522
Brand: MedChemExpress
SKU: HY-149433
Rating: 4.5 (0 reviews)

Cat. No.: HY-149433 Pureza: 98.04%: Ficha de datos
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BWA-522 is an orally active PROTAC degrader targeting full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer.
(Pink: Androgen Receptor ligand (HY-109070); Blue: Cereblon ligand (HY-14658); Black: linker).

Para uso exclusivo en investigación. No vendemos a pacientes.

BWA-522 Estructura química

No. CAS : 3042820-12-9

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
1 mg	En stock	Estimated Time of Arrival: December 31
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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Based on 1 Customer Validation

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Ver todas las isoformas

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Descripciòn

BWA-522 is an orally active PROTAC degrader targeting full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer^[1]. (Pink: Androgen Receptor ligand (HY-109070); Blue: Cereblon ligand (HY-14658); Black: linker).

IC₅₀ & Target^[1]

Cereblon

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	4.08 μM Compound: 28; BWA-522	Antiproliferative activity against enzalutamide-resistant human 22Rv1 cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Antiproliferative activity against enzalutamide-resistant human 22Rv1 cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 37556600]
LNCaP	IC₅₀	1.07 μM Compound: 28; BWA-522	Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 37556600]
VCaP	IC₅₀	5.59 μM Compound: 28; BWA-522	Antiproliferative activity against human VCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Antiproliferative activity against human VCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 37556600]

In Vitro

BWA-522 (0.03-30 μM; 3-48 h) dose- and time-dependently degrades both AR-FL and AR-V7 in LNCaP, VCaP, and 22Rv1 prostate cancer cells via the ubiquitin proteasome system and CRBN/cullin 4A ubiquitin ligase, with DC₅₀ values ranging from 0.67 to 3.45 μM^[1].
BWA-522 (6 days) potently inhibits the growth of AR-dependent LNCaP, VCaP, and Enzalutamide (HY-70002)-resistant 22Rv1 prostate cancer cells with IC₅₀ values ranging from 1.07 to 5.59 μM, while sparing AR-independent and normal prostate cells^[1].
BWA-522 (1-10 μM; 2 weeks) dose-dependently inhibits long-term colony formation of LNCaP and 22Rv1 prostate cancer cells^[1].
BWA-522 (1-10 μM; 48 h) dose-dependently suppresses AR downstream signaling proteins and induces apoptosis in LNCaP and VCaP prostate cancer cells^[1].
BWA-522 has a low risk of cardiotoxicity, as it exhibits minimal inhibition of the hERG channel with an IC₅₀ greater than 10 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:	LNCaP, VCaP, and 22Rv1 prostate cancer cells
Concentration:	10 μM
Incubation Time:	3, 6, 9, 12, 24, 48 h
Result:	Time-dependently degraded both AR-FL and AR-V7.

Western Blot Analysis^[1]

Cell Line:	LNCaP, VCaP human prostate cancer cells
Concentration:	1, 5, 10 μM
Incubation Time:	48 h
Result:	Reduced TMPRSS2, FKBP51, and PSA levels. Induced significant cleavage of PARP-1 and caspase-3 .

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	CL	F
Mice^[1]	2 mg/kg	i.v.	8.2 ± 1.0 h	0.1 ± 0.0 h	782 ± 275 ng/mL	3018 ± 326 ng·h/mL	594 ± 49 mL/h/kg	/
Mice^[1]	10 mg/kg	p.o.	7.9 ± 0.7 h	4.7 ± 1.2 h	376 ± 55 ng/mL	5947 ± 729 ng·h/mL	/	40.5 ± 4.6 %
Dog^[1]	1 mg/kg	i.v.	9.9 ± 1.1 h	0.1 ± 0.0 h	150.0 ± 24.8 ng/mL	919.0 ± 181.0 ng·h/mL	932.0 ± 227.0 mL/h/kg	/
Dog^[1]	5 mg/kg	p.o.	31.2 ± 15.9 h	2.8 ± 2.2 h	97.3 ± 56.4 ng/mL	1411.0 ± 678.0 ng·h/mL	/	69.3 ± 0.5 %

In Vivo

BWA-522 (20-60 mg/kg; p.o.; daily; 28 days) inhibits tumor growth inhibition in LNCaP xenograft-bearing NOD SCID mice, while 60 mg/kg daily achieves 76% tumor growth inhibition, with good in vivo tolerability^[1].

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

Animal Model:	LNCaP xenograft-bearing NOD SCID mice (6 weeks old)^[1]
Dosage:	20 mg/kg; 60 mg/kg
Administration:	p.o.; daily; 28 days
Result:	Achieved 26% tumor growth inhibition relative to vehicle control at 20 mg/kg. Achieved 76% tumor growth inhibition relative to vehicle control at 60 mg/kg. Caused no noticeable body weight loss throughout the study.

Peso molecular

771.34

Fòrmula

C₄₃H₅₁ClN₄O₇

No. CAS

3042820-12-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C1=CC=C(OC[C@H](O)CCl)C=C1)(C)C(C=C2)=CC=C2OCC3CCN(CC4CCN(C5=CC=C6C(C(N(C7CCC(NC7=O)=O)C6=O)=O)=C5)CC4)CC3

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 90 mg/mL (116.68 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	1.2964 mL	6.4822 mL	12.9645 mL
5 mM	0.2593 mL	1.2964 mL	2.5929 mL
10 mM	0.1296 mL	0.6482 mL	1.2964 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.

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Pureza y Documentación

Purity: 98.04%

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Ficha de datos (270 KB) SDS (254 KB)

COA (242 KB) HNMR (407 KB) RP-HPLC (262 KB) MS (73 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Zhang B, et al. Discovery of BWA-522, a First-in-Class and Orally Bioavailable PROTAC Degrader of the Androgen Receptor Targeting N-Terminal Domain for the Treatment of Prostate Cancer. J Med Chem. 2023;66(16):11158-11186. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.2964 mL	6.4822 mL	12.9645 mL	32.4111 mL
	5 mM	0.2593 mL	1.2964 mL	2.5929 mL	6.4822 mL
	10 mM	0.1296 mL	0.6482 mL	1.2964 mL	3.2411 mL
	15 mM	0.0864 mL	0.4321 mL	0.8643 mL	2.1607 mL
	20 mM	0.0648 mL	0.3241 mL	0.6482 mL	1.6206 mL
	25 mM	0.0519 mL	0.2593 mL	0.5186 mL	1.2964 mL
	30 mM	0.0432 mL	0.2161 mL	0.4321 mL	1.0804 mL
	40 mM	0.0324 mL	0.1621 mL	0.3241 mL	0.8103 mL
	50 mM	0.0259 mL	0.1296 mL	0.2593 mL	0.6482 mL
	60 mM	0.0216 mL	0.1080 mL	0.2161 mL	0.5402 mL
	80 mM	0.0162 mL	0.0810 mL	0.1621 mL	0.4051 mL
	100 mM	0.0130 mL	0.0648 mL	0.1296 mL	0.3241 mL

BWA-522 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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BWA-522

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BWA-522 Related Antibodies

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas PROTACs:

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BWA-522 Related Antibodies

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Complete Stock Solution Preparation Table

BWA-522 Related Classifications

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