PF 06465469

Pricing Availability   Qty
说明: Potent ITK inhibitor; also inhibits BTK
化学名: (R)-3-(1-(1-Acryloylpiperidin-3-yl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-N-(3-methyl-4-(1-methylethyl))benzamide
纯度: ≥95% (HPLC)
说明书
引用文献 (2)
评论

生物活性 for PF 06465469

PF 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).

许可信息

Sold for research purposes under agreement from Pfizer Inc.

技术数据 for PF 06465469

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.

溶解性数据 for PF 06465469

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 2.62 5 温和加热

制备储备液 for PF 06465469

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.

选择批次从而根据批次分子量重新计算:
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

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参考文献 for PF 06465469

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.

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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

2 篇 PF 06465469 的引用文献

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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