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 activephosphodiesterases 3(PDE3) inhibitor withIC50s of 10 and 27 nM forPDE3AandPDE3B, respectively. Antitumor activity[1]. |
| IC50& Target[1] | PDE3A 10 nM (IC50) | PDE3B 27 nM (IC50) |
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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[1].
BRD9500 exhibits anEC50of 1 nM for SK-MEL-3 melanoma cell line viability[1].
BRD9500 exhibits anEC50of 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 | | Concentration: | 10 μM | | Incubation Time: | 8 hours | | Result: | SLFN12 coimmunoprecipitation was analyzed by immunoblotting with an anti-V5 antibody to detect the SLFN12-V5 fusion protein. The SLFN12-V5 was clearly detected with the anti-V5 antibody. |
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体内研究
(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. |
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| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(171.63 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.4327 mL | 17.1633 mL | 34.3265 mL | | 5 mM | 0.6865 mL | 3.4327 mL | 6.8653 mL | | 10 mM | 0.3433 mL | 1.7163 mL | 3.4327 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.58 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.58 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.58 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.58 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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