Peficitinib (ASP015K) 是一种具有口服活性的JAK抑制剂，对 JAK1、JAK2、JAK3 和 Tyk2 的IC50值分别为 3.9、5.0、0.7 和 4.8 nM。
| 生物活性 | Peficitinib (ASP015K) is an orally activeJAKinhibitor, withIC50s of 3.9, 5.0, 0.7 and 4.8 nM forJAK1,JAK2,JAK3andTyk2, respectively[1]. |
| IC50& Target[1] | JAK3 0.7 nM (IC50) | JAK1 3.9 nM (IC50) | Tyk2 4.8 nM (IC50) | JAK2 5 nM (IC50) |
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体外研究
(In Vitro) | Peficitinib hydrobromide (0-100 nM; 3 days) inhibits IL-2-induced T cell proliferation in a concentration-dependent manner[1].
Peficitinib hydrobromide (10-1000 nM) inhibits IL-2-induced STAT5 phosphorylation in a concentration-dependent manner with a mean IC50of 124 nM in rat whole blood, and inhibits STAT5 phosphorylation with a mean IC50of 127 nM in human lymphocytes[1].
Cell Proliferation Assay[1] | Cell Line: | Splenocytes from male Lewis rats | | Concentration: | 0-100 nM | | Incubation Time: | 3 days | | Result: | Inhibited IL-2-induced T cell proliferation in a concentration-dependent manner with an IC50of 10 nM. |
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体内研究
(In Vivo) | Peficitinib hydrobromide (1-30 mg/kg; p.o.; once daily for 24 days) shows dose-dependent efficacy both in prophylactic and therapeutic dosing regimens in an adjuvant-induced arthritis rat model[1].
| Animal Model: | Seven-weeks-old female Lewis rats, adjuvant-induced arthritis (AIA) model[1] | | Dosage: | 1, 3, 10, and 30 mg/kg | | Administration: | Oral administration, once daily for 24 days | | Result: | Significantly inhibited the increase in paw volume at doses of 1 mg/kg or greater with an ED50value of 2.7 mg/kg (95% confidence interval: 1.5–4.2 mg/kg). Significantly reduced the bone destruction score at 10 mg/kg or greater and almost fully ameliorated both paw swelling and bone destruction scores at 30 mg/kg. |
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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 : ≥ 60 mg/mL(183.83 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.0638 mL | 15.3191 mL | 30.6382 mL | | 5 mM | 0.6128 mL | 3.0638 mL | 6.1276 mL | | 10 mM | 0.3064 mL | 1.5319 mL | 3.0638 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 (7.66 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.66 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 (7.66 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.66 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。 *以上所有助溶剂都可在本网站选购。
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