| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C43H51ClN4O7 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
BWA-522 is an orally active PROTAC degrader that targets full-length androgen receptor (AR-FL) and the AR-V7 splice variant. It antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses downstream AR signaling proteins, and induces apoptosis in cancer cells, while inhibiting tumor growth in an LNCaP xenograft mouse model, and can be used in prostate cancer research[1]. It is supplied as a light yellow to yellow solid (C43H51ClN4O7, MW 771.34) at 98.04% purity.
Physical & Chemical Properties
| CAS Number | 3042820-12-9 |
|---|---|
| Molecular Formula | C43H51ClN4O7 |
| Molecular Weight | 771.34 g/mol |
| Purity | 98.04% |
| 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 |
| Target | Cereblon |
| Signaling Pathway | PROTAC; Vitamin D Related/Nuclear Receptor; Apoptosis |
| Solubility | In Vitro: DMSO: 90 mg/mL (116.68 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 90 mg/mL (116.68 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
In LNCaP, VCaP, and 22Rv1 prostate cancer cells, BWA-522 (0.03-30 μM; 3-48 h) degrades both AR-FL and AR-V7 in a dose- and time-dependent manner via the ubiquitin proteasome system together with CRBN/cullin 4A ubiquitin ligase, yielding DC50 values of 0.67 to 3.45 μM[1]. After 6 days, BWA-522 potently inhibits the growth of AR-dependent LNCaP and VCaP cells and of Enzalutamide-resistant 22Rv1 prostate cancer cells (IC50 values of 1.07 to 5.59 μM) and spares AR-independent and normal prostate cells[1]. Over 2 weeks, BWA-522 (1-10 μM) inhibits long-term colony formation of LNCaP and 22Rv1 prostate cancer cells in a dose-dependent manner[1]. In LNCaP and VCaP prostate cancer cells, BWA-522 (1-10 μM; 48 h) suppresses AR downstream signaling proteins and induces apoptosis, both dose-dependently[1]. BWA-522 carries a low cardiotoxicity risk, showing minimal hERG channel inhibition with an IC50 above 10 μM[1].
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. |
In Vivo
In NOD SCID mice bearing LNCaP xenografts, BWA-522 (20-60 mg/kg; p.o.; daily; 28 days) inhibits tumor growth, with 60 mg/kg daily reaching 76% tumor growth inhibition and good in vivo tolerability[1].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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