LDN-212854 是一种骨形态发生蛋白 (BMP) 抑制剂，可有效抑制ALK2(IC50: 1.3 nM)。LDN-212854 还可抑制ALK1(IC50: 2.40 nM)。LDN-212854 可用于研究进行性骨化纤维发育不良和癌症，如肝细胞癌 (HCC)。
| 生物活性 | LDN-212854 is abone morphogenetic protein(BMP) inhibitor that potently inhibitsALK2(IC50: 1.3 nM). LDN-212854 also inhibitsALK1(IC50: 2.40 nM). LDN-212854 can be used in the research of fibrodysplasia ossificans progressive and cancers, such as hepatocellular carcinoma (HCC)[1][2]. |
| IC50& Target[1] | ACVR1 1.3 nM (IC50) | ALK1 2.4 nM (IC50) | BMPR1A 85.8 nM (IC50) | ALK4 2133 nM (IC50) | ALK5 9276 nM (IC50) |
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体外研究
(In Vitro) | LDN-212854 (0-3.815 μM) blocks the phosphorylation of SMAD1/5/8 induced by BMP7 in BMPR2–/–cells[1].
LDN-212854 (2.5 μM, 5 days ) inhibits cell proliferation in Huh7 and MT cells[2].
LDN-212854 (0.5 μM, 48 h ) suppresses ID1 and EpCAM expression in Huh7 and MT cells[2].
Western Blot Analysis[1] | Cell Line: | BMPR2-deficient pulmonary vascular smooth muscle cells | | Concentration: | 0, 1, 3, 6, 16, 39, 98, 244, 610, 1530, 3815 nM | | Incubation Time: | | | Result: | Inhibited the phosphorylation of SMAD1/5/8 induced by BMP7 with an IC50value of 37 nM. |
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体内研究
(In Vivo) | LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 4 weeks) potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva[1].
LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 10-14 days) suppresses HCC tumor progression through repression of ID1 in HCC xenografts model[2].
| Animal Model: | Murine inducible transgenic ALK2Q207D model of heterotopic ossification[1] | | Dosage: | 6 mg/kg | | Administration: | Intraperitoneal injection , twice daily for 4 weeks | | Result: | Prevented the formation of heterotopic bone and preserved limb range of motion with minimal or no impairment in the majority of mice. |
| Animal Model: | HCC xenografts (Huh7 or MT cell)[1] | | Dosage: | 6 mg/kg | | Administration: | Intraperitoneal injection, twice daily for 10-14 days. | | Result: | Inhibited tumor growth and showed less spheroid/colony formation ability than PBS-treated tumor cells. |
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| 中文名称 | 5-（6-（4-（哌嗪-1-基）苯基）吡唑并[1,5-a]嘧啶-3-基）喹啉 |
| 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 : ≥ 30 mg/mL(73.80 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.4601 mL | 12.3007 mL | 24.6015 mL | | 5 mM | 0.4920 mL | 2.4601 mL | 4.9203 mL | | 10 mM | 0.2460 mL | 1.2301 mL | 2.4601 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 (6.15 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.15 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 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 (6.15 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.15 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 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。 *以上所有助溶剂都可在本网站选购。
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