1630760-75-6
1630760-75-6 structure
- Name: BRD9500
- Chemical Name: BRD9500
- CAS Number: 1630760-75-6
- Molecular Formula: C15H18FN3O2
- Molecular Weight: 291.32
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
- Create Date: 2020-11-28 16:47:45
- Modify Date: 2025-09-24 08:29:38
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BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity[1].
| Name | BRD9500 |
|---|
| Description | BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity[1]. |
|---|---|
| Related Catalog | |
| Target |
PDE3A:10 nM (IC50) PDE3B:27 nM (IC50) |
| In Vitro | BRD9500 is a DNMDP analog. DNMDP potently and selectively inhibits PDE3A and PDE3B and kills cancer cells by inducing PDE3A/B interactions with SFLN12[1]. BRD9500 exhibits an EC50 of 1 nM for SK-MEL-3 melanoma cell line viability[1]. BRD9500 exhibits an EC50 of 1.6 nM for HeLa viability[1]. BRD9500 (10 μM; 8 hours) stabilizes the PDE3A-SLFN12 interaction in HeLa cells[1]. Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 10 μM Incubation Time: 8 hours Result: SLFN12 coimmunoprecipitation was analyzed by immunoblotting with an anti-V5 antibody to detect the SLFN12-V5 fusion protein. The SLFN12-V5 was clearly detected with the anti-V5 antibody. |
| In Vivo | BRD9500 (10, 20, and 50 mg/kg; orally) inhibits SK-MEL-3 melanoma growth in mice[1]. BRD9500 shows high plasma levels in mice after iv (1 mg/kg) as well as po (2 mg/kg) dosing over eight hours making it a valuable candidate for in vivo xenograft testing[1]. Animal Model: Female NMRI nude mice bearing SK-MEL-3 melanoma cells tumor xenografts[1] Dosage: 10, 20, and 50 mg/kg Administration: Orally at 10 and 20 mg/kg twice daily (2QD) and at 50 mg/kg once per day (QD). Result: Achieved the strongest antitumor activity at 50 mg/kg. All treatments were well tolerated without critical body weight loss or toxicities. |
| References |
| Molecular Formula | C15H18FN3O2 |
|---|---|
| Molecular Weight | 291.32 |