Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zimlovisertib (PF-06650833) is an effective, selective and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) (IC50s: 0.2 and 2.4 nM in the cell and PBMC assay).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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2 mg | 在庫あり | ¥ 9,000 | |||
5 mg | 在庫あり | ¥ 14,500 | |||
10 mg | 在庫あり | ¥ 27,000 | |||
25 mg | 在庫あり | ¥ 54,000 | |||
50 mg | 在庫あり | ¥ 104,500 | |||
100 mg | 在庫あり | ¥ 181,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 15,500 |
説明 | Zimlovisertib (PF-06650833) is an effective, selective and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) (IC50s: 0.2 and 2.4 nM in the cell and PBMC assay). |
ターゲット&IC50 | IRAK4:0.2 nM |
In vitro | The kinome selectivity profile of PF06650833 (Compound 40) is assessed in a panel of 278 kinases at 200 nM inhibitor concentration using the ATP Km for each kinase. Approximately 100% inhibition is observed for IRAK4. Lactam PF06650833 is assessed in a whole-cell functional VEGF2R assay (PAE-KDR cell line). No activity is observed at concentrations up to and including 30 μM. In a voltage clamp assay, PF06650833 inhibits hERG current by 25% at 100 μM. |
In vivo | PF06650833 (0.3-30 mg/kg; p.o; for 2.5 hours; male SD rats) treatment significantly inhibits LPS-induced TNF-α in a dose dependent manner. Mean exposures of PF06650833 in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of PF06650833 at 0.3, 1, 3, and 30 mg/kg. The fraction unbound in rat plasma of PF06650833 is 0.3. |
動物実験 | Animal Model: Male Sprague-Dawley rats. Dosage: 0.1 mg/kg, 1 mg/kg, 3 mg/kg, 30 mg/kg. Administration: Oral administration; for 2.5 hours |
別名 | PF-06650833, PF06650833 |
分子量 | 361.37 |
分子式 | C18H20FN3O4 |
CAS No. | 1817626-54-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (276.72 mM)
You can also refer to dose conversion for different animals. 詳細
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Zimlovisertib 1817626-54-2 Immunology/Inflammation NF-Κb IRAK Interleukin-1 receptor associated kinase inhibit Inhibitor PF-06650833 PF 06650833 IL-1R associated kinase PF06650833 inhibitor