BRD9500

Modify Date: 2025-09-24 08:29:38

BRD9500 Structure
BRD9500 structure
Common Name BRD9500
CAS Number 1630760-75-6 Molecular Weight 291.32
Density N/A Boiling Point N/A
Molecular Formula C15H18FN3O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of BRD9500


BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity[1].

 Names

Name BRD9500

 BRD9500 Biological Activity

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

[1]. Timothy A Lewis, et al. Optimization of PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing. ACS Med Chem Lett. 2019 Oct 18;10(11):1537-1542.

 Chemical & Physical Properties

Molecular Formula C15H18FN3O2
Molecular Weight 291.32
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