BRD9500

• CAT Number: I023681
• CAS Number: 1630760-75-6
• Molecular Formula: C15H18FN3O2
• Molecular Weight: 291.32
• Purity: ≥95%
• Synonyms: (4R)-3-(3-fluoro-4-morpholin-4-ylphenyl)-4-methyl-4,5-dihydro-1H-pyridazin-6-one
• InChI: InChI=1S/C15H18FN3O2/c1-10-8-14(20)17-18-15(10)11-2-3-13(12(16)9-11)19-4-6-21-7-5-19/h2-3,9-10H,4-8H2,1H3,(H,17,20)/t10-/m1/s1
• InChIKey: GJGGSLDXABLZLP-SNVBAGLBSA-N
• SMILES: CC1CC(=O)NN=C1C2=CC(=C(C=C2)N3CCOCC3)F

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].
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].

Reference

[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.
 [Content Brief]