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Submit ReviewAZD 4547
说明： Potent and selective FGFR inhibitor
化学名： rel-N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]benzamide
纯度： ≥98% (HPLC)
生物活性 for AZD 4547
AZD 4547 is a potent and selective FGFR1, FGFR3 and FGFR2 tyrosine kinase inhibitor (IC50 values are 0.2 1.8, and 2.5 nM, respectively). It shows selectivity for FGFR across a range of unrelated tyrosine and serine/threonine kinases, including IGFR (>2,900-fold), CDK2 (>50,000-fold), and p38 (>50,000-fold). In vitro, it has antiproliferative effects on tumor cell lines with deregulated FGFR expression. In vivo, AZD 4547 exhibits dose-dependent inhibition of tumor growth in an FGFR-driven human tumor xenograft mice model. It suppresses osteoclastogenesis and tumor-induced osteolysis in an orthotopic breast cancer bone metastasis mouse model. AZD 4547 is orally bioavailable.
技术数据 for AZD 4547
| 分子量 | 463.56 |
| 公式 | C26H33N5O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1035270-39-3 |
| PubChem ID | 51039095 |
| InChI Key | VRQMAABPASPXMW-HDICACEKSA-N |
| Smiles | C[C@H]1CN(C2=CC=C(C=C2)C(NC3=NNC(CCC4=CC(OC)=CC(OC)=C4)=C3)=O)C[C@H](N1)C |
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 AZD 4547
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 9.27 | 20 |
制备储备液 for AZD 4547
以下数据基于产品分子量 463.56。 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 |
|---|---|---|---|
| 0.2 mM | 10.79 mL | 53.93 mL | 107.86 mL |
| 1 mM | 2.16 mL | 10.79 mL | 21.57 mL |
| 2 mM | 1.08 mL | 5.39 mL | 10.79 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.16 mL |
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产品说明书 for AZD 4547
参考文献 for AZD 4547
参考文献是支持产品生物活性的出版物。
Gavine et al (2012) AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 72 2045 PMID: 22369928
Kang et al (2019) A selective FGFR inhibitor AZD4547 suppresses RANKL/M-CSF/OPG-dependent ostoclastogenesis and breast cancer growth in the metastatic bone microenvironment. Sci.Rep. 9 8726 PMID: 31217507
If you know of a relevant reference for AZD 4547, please let us know.
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关键词: AZD 4547, AZD 4547 supplier, AZD4547, potent, selective, tyrosine, kinases, inhibitors, inhibits, FGFR, orally, bioavailable, osteolysis, cancer, osteoclastogenesis, 7823, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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