BRD9500

目录号: PL09675 纯度: ≥99%
BRD9500 是一种有效的,具有口服活性的磷酸二酯酶 3 (PDE3) 抑制剂,对 PDE3A 和 PDE3B 的 IC50 分别为 10 和 27 nM。具有抗肿瘤活性。
CAS No. :1630760-75-6
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中文名称
BRD9500
英文名称
BRD9500
英文别名
BRD9500;(R)-6-(3-fluoro-4-morpholinophenyl)-5-methyl-4,5-dihydropyridazin-3(2H)-one;(4R)-3-(3-fluoro-4-morpholin-4-ylphenyl)-4-methyl-4,5-dihydro-1H-pyridazin-6-one;1630760-75-6 (R-Isomer)
Cas No.
1630760-75-6
分子式
C15H18FN3O2
分子量
291.32
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
BRD9500 是一种有效的,具有口服活性的磷酸二酯酶 3 (PDE3) 抑制剂,对 PDE3A 和 PDE3B 的 IC50 分别为 10 和 27 nM。具有抗肿瘤活性。
产品详情
BRD9500 是一种有效的,具有口服活性的磷酸二酯酶 3 (PDE3) 抑制剂,对 PDE3A 和 PDE3B 的 IC50 分别为 10 和 27 nM。具有抗肿瘤活性。
生物活性
BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC 50 s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.
性状
Solid
IC50 & Target[1][2]
PDE3A 10 nM (IC50) PDE3B 27 nM (IC50
体外研究(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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 50 mg/mL (171.63 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[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.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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