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
- プロトコル
- 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
製品説明
Cellular Effect
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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.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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