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.
For research use only. We do not sell to patients.
- CAS No.: 1609465-78-2
- Formula: C22H21ClN6O2
- Molecular Weight:436.89
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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] |
Chemical Information
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CAS No. 1609465-78-2
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Molecular Weight 436.89
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-303 Related Classifications
HY-164002 Related Classifications
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