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Submit ReviewPF 06465469 is a potent inhibitor of interleukin-2 inducible T cell kinase (ITK) (IC50 = 2 nM). Also exhibits inhibitory activity against Bruton's tyrosine kinase (BTK) (IC50 = 2 nM). Displays nanomolar potencies in a cell-based IP1 assay and human whole blood assay (IC50 values are 31 and 48 nM respectively).
Sold for research purposes under agreement from Pfizer Inc.
分子量 | 523.63 |
公式 | C30H33N7O2 |
储存 | Store at +4°C |
纯度 | ≥95% (HPLC) |
CAS Number | 1407966-77-1 |
PubChem ID | 71450146 |
InChI Key | CGJVMKJGKFEHTL-HSZRJFAPSA-N |
Smiles | NC1=C2C(N([C@@H]4CCCN(C(C=C)=O)C4)N=C2C3=CC(C(NC5=CC(C)=C(C(C)C)C=C5)=O)=CC=C3)=NC=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 2.62 | 5 温和加热 |
以下数据基于产品分子量 523.63。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.05 mM | 38.19 mL | 190.97 mL | 381.95 mL |
0.25 mM | 7.64 mL | 38.19 mL | 76.39 mL |
0.5 mM | 3.82 mL | 19.1 mL | 38.19 mL |
2.5 mM | 0.76 mL | 3.82 mL | 7.64 mL |
参考文献是支持产品生物活性的出版物。
Zapf et al (2012) Covalent inhibitors of interleukin-2 inducible T cell kinase (Itk) with nanomolar potency in a whole-blood assay. J.Med.Chem. 55 10047 PMID: 23098091
If you know of a relevant reference for PF 06465469, please let us know.
关键词: PF 06465469, PF 06465469 supplier, PF06465469, Pfizer, interleukin-2, IL-2, inducible, T, cell, kinase, ITK, inhibitors, inhibits, potent, Brutons, tyrosine, BTK, Tyrosine, Kinase, (BTK), 4710, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PF 06465469 的部分引用包括:
Mamand et al (2018) Comparison of interleukin-2-inducible kinase (ITK) inhibitors and potential for combination therapies for T-cell lymphoma. Sci Rep 8 14216 PMID: 30242208
Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261
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