PF-303
PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC50=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1609465-78-2
- 分子式: C22H21ClN6O2
- 分子量:436.89
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
48 nM
Compound: 10
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Inhibition of full-length human C-terminal His6-tagged BTK C481S mutant expressed in Sf9 insect cells using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay
Inhibition of full-length human C-terminal His6-tagged BTK C481S mutant expressed in Sf9 insect cells using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay
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[PMID: 30655951] |
化学情報
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CAS 番号 1609465-78-2
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分子量 436.89
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分子式 C22H21ClN6O2
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SMILES
NC(C1=C(N)N([C@H]2CN(CCC2)C#N)N=C1C3=CC=C(C=C3)OC4=CC=C(C=C4)Cl)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Benson M J, et al. Modeling the clinical phenotype of BTK inhibition in the mature murine immune system[J]. The Journal of Immunology, 2014, 193(1): 185-197. [Content Brief]
[2]. Schnute M E, et al. Aminopyrazole carboxamide bruton’s tyrosine kinase inhibitors. irreversible to reversible covalent reactive group tuning[J]. ACS Medicinal Chemistry Letters, 2018, 10(1): 80-85. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PF-303 関連分類
HY-164002 関連分類
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