BRD9500 |
| Catalog No.GC60661 |
BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1630760-75-6
Sample solution is provided at 25 µL, 10mM.
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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].
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
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]
[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.
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