PF-3644022
- CAS号:1276121-88-0
- 英文名:PF 3644022
- 中文名:PF-3644022
- CBNumber:CB52596685
- 分子式:C21H18N4OS
- 分子量:374.46
- MOL File:1276121-88-0.mol
- 熔点 :>180°C (dec.)
- 沸点 :703.3±60.0 °C(Predicted)
- 密度 :1.298±0.06 g/cm3(Predicted)
- 储存条件 :2-8°C(protect from light)
- 溶解度 :DMSO (Slightly), Methanol (Slightly)
- 形态 :Solid
- 酸度系数(pKa) :13.51±0.40(Predicted)
- 颜色 :Off-White to Yellow
- 海关编码 :2934999090
PF-3644022性质、用途与生产工艺
- 生物活性 PF-3644022 是一种有效的，选择性的，口服活性的，具有 ATP 竞争性的 MAPKAPK2 (MK2) 抑制剂，IC50 为 5.2 nM，Ki 为 3 nM。PF-3644022 还抑制 MK3 和 p38 调节/激活激酶 (PRAK)，IC50 分别为 53 nM 和 5.0 nM。PF-3644022 有效抑制 TNFα 的产生并具有抗炎作用。
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靶点
IC50: 5.2 nM (MK2), 5.0 nM (PRAK) and 53 nM (MK3).
Ki: 3 nM (MK2) -
体外研究
The inhibitory activity of PF-3644022 against other MAPKAP kinase family members is evaluated. Other than MNK2 with an IC 50 of 148 nM, other family members are largely not inhibited, showing at least several hundred-fold selectivity versus MK2.
In the human U937 monocytic cell line or peripheral blood mononuclear cells, PF-3644022 potently inhibits TNFα production with similar activity ( IC 50 of 160 nM). PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC 50 values of 1.6 and 10.3 μM, respectively. Inhibition of TNFα in U937 cells and blood correlates closely with inhibition of phospho-heat shock protein 27, a target biomarker of MK2 activity. -
体内研究
PF-3644022 (3-100 mg/kg; oral gavage; twice a day; for 12 days; Lewis rats) treatment shows dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing, with ED 50 value of 20 mg/kg.
Animal Model: Female Lewis rats (125-140 g) injected with streptococcal cell wall Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg Administration: Oral gavage; twice a day; for 12 days Result: Showed dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing.
- 更新日期：2024/11/08
- 产品编号：HY-107427
- 产品名称：PF-3644022 PF-3644022
- CAS编号：1276121-88-0
- 包装：1mg
- 价格：1440元
- 更新日期：2024/11/08
- 产品编号：HY-107427
- 产品名称：PF-3644022 PF-3644022
- CAS编号：1276121-88-0
- 包装：5mg
- 价格：3000元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
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