产品
编 号：F622473
分子式：C15H18FN3O2
分子量：291.32
分子式：C15H18FN3O2
分子量：291.32
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1630760-75-6
产品详情
生物活性：
BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.
体内研究：
BRD9500 (10, 20, and 50 mg/kg; orally) inhibits SK-MEL-3 melanoma growth in mice.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.Animal Model:Female NMRI nude mice bearing SK-MEL-3 melanoma cells tumor xenografts
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.
体外研究：
BRD9500 is a DNMDP analog. DNMDP potently and selectively inhibits PDE3A and PDE3B and kills cancer cells by inducing PDE3A/B interactions with SFLN12. BRD9500 exhibits an EC50 of 1 nM for SK-MEL-3 melanoma cell line viability. BRD9500 exhibits an EC50 of 1.6 nM for HeLa viability.BRD9500 (10 μM; 8 hours) stabilizes the PDE3A-SLFN12 interaction in HeLa cells.
BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.
体内研究：
BRD9500 (10, 20, and 50 mg/kg; orally) inhibits SK-MEL-3 melanoma growth in mice.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.Animal Model:Female NMRI nude mice bearing SK-MEL-3 melanoma cells tumor xenografts
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.
体外研究：
BRD9500 is a DNMDP analog. DNMDP potently and selectively inhibits PDE3A and PDE3B and kills cancer cells by inducing PDE3A/B interactions with SFLN12. BRD9500 exhibits an EC50 of 1 nM for SK-MEL-3 melanoma cell line viability. BRD9500 exhibits an EC50 of 1.6 nM for HeLa viability.BRD9500 (10 μM; 8 hours) stabilizes the PDE3A-SLFN12 interaction in HeLa cells.
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