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- 2025年12月05日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
2173556-69-7
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1681.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥750.0 |
| 规格： | 5 mg | 产品价格： | ￥1800.0 |
| 规格： | 10 mg | 产品价格： | ￥2700.0 |
| 规格： | 25 mg | 产品价格： | ￥4590.0 |
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PK68
CAS No. : 2173556-69-7
MCE 国际站：PK68
产品活性：PK68 是一种高效、特异性的受体相互作用激酶 1 (RIPK1) 的 II 型抑制剂，具有口服活性。其 IC50 值约 90 nM，可抑制 RIPK1 依赖性坏死。PK68 对 TNF 诱导的全身炎症反应综合征有较强的改善作用，可用于炎症紊乱和肿瘤转移的研究。
研究领域：Apoptosis
作用靶点：RIP kinase
In Vitro: PK68 has highly potent inhibition of TNF-induced necroptosis with EC50 values of 23 nM and 13 nM in human and mouse cells, respectively.
PK68 is a highly selective inhibitor of RIPK1 kinase activity with IC50 value of 90 nM.
PK68 (100 nM, 1 h) blocks necroptosis through the suppression of RIPK3 function or signaling upstream of RIPK3 activation.
In Vivo: PK68 (5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days) or (2 mg/kg, i.v.; 10 mg/kg, p.o.; for 14 days) exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice.
PK68 (1 mg/kg, i.p.) ameliorates TNF-induced systemic inflammatory response syndrome.
PK68 (5 mg/kg, i.v.) inhibits RIPK1 that results in attenuated tumor cell transmigration across the endothelial barrier and preventive suppression of tumor metastasis.
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文献和实验.1 14.9 14.7 14.6 14.5 14.5 14.4 14.3 14.2 14.2 14.1 14.0 13.9 3 4 10.6 9.98 9.60 9.36 9.20 9.07 8.98 8.90 8.84 8.75 8.66 8.56 8.46 8.36 8.26 4 5 8.43 7.76 7.39 7.16 6.98 6.85 6.76 6.68 6.62 6.52 6.43 6.33 6.23 6.12 6.01 5 6 7.26 6.60 5.23
54 13 58 18 24 76 15 54 55 95 52 23 27 42 37 86 53 48 55 90 65 72 96 57 69 36 10 96 46 92 42 45 97 60 49 04 91 24 00 39 68 29 61 66 37 32 20 30 77 84 57 03 29 10 45 65 04 26 11 04 96 67 24 25 29 94 98 94 24 68 49 69 10 82 53 75 91 93 30 34 25 20 57
8.79 8.74 8.71 8.69 8.67 8.66 3 4 7.71 6.94 6.59 6.39 6.26 6.16 6.09 6.04 6.00 5.96 5.91 5.87 5.84 5.82 5.80 4 5 6.61 5.79 5.41 5.19 5.05 4.95 4.88 4.82 4.77 4.74 4.68 4.64 4.60 4.58 4.56 5 6 5.99 5.14 4.76 4.53 4.39 4.28 4.21 4.15 4.10 4.06 4.00
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