| Identification | Back Directory | [Name]
3(2H)-Pyridazinone, 6-[3-fluoro-4-(4-morpholinyl)phenyl]-4,5-dihydro-5-methyl-, (5R)- | [CAS]
1630760-75-6 | [Synonyms]
BRD9500
3(2H)-Pyridazinone, 6-[3-fluoro-4-(4-morpholinyl)phenyl]-4,5-dihydro-5-methyl-, (5R)- | [Molecular Formula]
C15H18FN3O2 | [MOL File]
1630760-75-6.mol | [Molecular Weight]
291.32 |
| Hazard Information | Back Directory | [Description]
BRD9500 is a potent PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing (EC50 =1 nM). BRD9500, was active in an SK-MEL-3 xenograft_x000D_
model of cancer. | [Uses]
BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity[1]. | [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. |
| [IC 50]
PDE3A: 10 nM (IC50); PDE3B: 27 nM (IC50) | [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. DOI:10.1021/acsmedchemlett.9b00360 |
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