Axitinib

Cat. No. 4350 5 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent VEGFR-1, -2 and -3 inhibitor

化学名： N-Methyl-[[3[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide

纯度： ≥99% (HPLC)

引用文献 (5)

文献 (1)

通路 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for Axitinib

Axitinib is a potent inhibitor of VEGFR-2, -3, and -1 (IC₅₀ values are 0.2, 0.1-0.3, and 1.2 nM respectively). Axitinib exhibits minimal activity against a panel of ~100 protein kinases. Axitinib inhibits angiogenesis and vascular permeability. Also a high affinity BCR-ABL1 (T315I) inhibitor (K_i = 149 pM for autophosphorylated ABL1 (T315I)). Axitinib blocks proliferation of Ba/F3 cells expressing BCR-ABL1 (T315I). Axitinib (10 mg/kg) decreases T-cell exhaustion and tumor and T-cell hypoxia and improves survival in mice in vivo. Orally available.

许可信息

Sold for research purposes under agreement from Pfizer Inc.

化合物库 for Axitinib

Axitinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。

技术数据 for Axitinib

分子量	386.47
公式	C₂₂H₁₈N₄OS
储存	Store at +4°C
纯度	≥99% (HPLC)
CAS Number	319460-85-0
PubChem ID	6450551
InChI Key	RITAVMQDGBJQJZ-FMIVXFBMSA-N
Smiles	O=C(NC)C1=C(SC2=CC=C(C(/C=C/C4=CC=CC=N4)=NN3)C3=C2)C=CC=C1

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 Axitinib

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	9.66	25

制备储备液 for Axitinib

以下数据基于产品分子量 386.47。 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
0.25 mM	10.35 mL	51.75 mL	103.5 mL
1.25 mM	2.07 mL	10.35 mL	20.7 mL
2.5 mM	1.04 mL	5.18 mL	10.35 mL
12.5 mM	0.21 mL	1.04 mL	2.07 mL

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产品说明书 for Axitinib

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Axitinib

参考文献是支持产品生物活性的出版物。

Hu-Lowe et al (2008) Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2 and 3. Clin.Cancer Res. 14 7272 PMID: 19010843

Ma and Waxman (2008) Modulation of the antitumor activity of metronomic cyclophosph. by the angiogenesis inhibitor axitinib. Mol.Cancer Ther. 7 79 PMID: 18202011

Pemovska et al (2015) Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation. Nature 519 102 PMID: 25686603

Scharping (2021) Mitochondrial stress induced by continuous stimulation under hypoxia rapidly drives T cell exhaustion. Nat.Immunol. 22 205 PMID: 33398183

If you know of a relevant reference for Axitinib, please let us know.

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关键词: Axitinib, Axitinib supplier, Axitinib, inhibits, VEGFR-1, VEGFR-2, VEGFR-3, inhibitors, VEGF, receptor, receptors, vascular, endothelial, growth, factor, BCR-ABL, VEGFR, 4350, Tocris Bioscience

5 篇 Axitinib 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Axitinib 的部分引用包括：

Jung Yoon et al (2022) The Potential of Transforming Growth Factor-beta Inhibitor and Vascular Endothelial Growth Factor Inhibitor as Therapeutic Agents for Uterine Leiomyoma. Int J Med Sci 19 1779-1786 PMID: 36313223

Salgado-Pabón et al (2013) Superantigens are critical for Staphylococcus aureus Infective endocarditis, sepsis, and acute kidney injury. MBio 4 PMID: 23963178

Andrea et al (2015) VEGF and LPS synergistically silence inflammatory response to Plasmodium berghei infection and protect against cerebral malaria. Pathog Glob Health 109 255-65 PMID: 26392042

Neelam et al (2013) Lenticular cytoprotection. Part 1: the role of hypoxia inducible factors-1α and -2α and vascular endothelial growth factor in lens epithelial cell survival in hypoxia. Mol Vis 19 1 PMID: 23335846

Tseng et al (2012) Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior. Sci Rep 9 1113 PMID: 23064517

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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。

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for Axitinib

VEGF Signaling Pathway

VEGF signaling pathway is involved in embryonic vascular development (vasculogenesis) and in the formation of new blood vessel (angiogenesis). It also induces cell migration, proliferation and survival.