Axitinib (AG 013736)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Axitinib是一种选择性的和可口服的血管内皮生长因子(VEGF)受体酪氨酸激酶1/2/3抑制剂[1]。
在细胞中,axitinib抑制VEGFR-1、2和3的磷酸化,IC50值分别为0.1 nM、0.2 nM和0.1-0.3 nM。在HUVEC细胞中,axitinib抑制VEGFR-2刺激的细胞存活,比对FGFR-1的选择性高1000倍。Axitinib也可以显著抑制VEGF下游信号分子的磷酸化,包括Akt、eNOS 和ERK1/2。在体内,axitinib抑制VEGFR-2的磷酸化,EC50值为0.49 nM。在M24met、HCT-116和SN12C人异种移植小鼠中,axitinib延迟肿瘤生长[1]。
参考文献:
[1] Hu-Lowe D D, Zou H Y, Grazzini M L, et al. 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, 3. Clinical Cancer Research, 2008, 14(22): 7272-7283.
- 1. Schwartz, Hannah, et al. "In vitro Methods to Better Evaluate Drug Responses in Cancer." UMass Chan Medical School. September 8, 2022.
- 2. Paik ES, Kim TH, et al. "Preclinical assessment of the VEGFR inhibitor axitinib as a therapeutic agent for epithelial ovarian cancer." Sci Rep. 2020;10(1):4904. > PMID: 32184452
- 3. Anna V. Ivanina, Ballav Borah, et al. "The Role of the Vascular Endothelial Growth Factor (VEGF) Signaling in Biomineralization of the Oyster Crassostrea gigas." Front. Mar. Sci., 28 August 2018.
Storage | Store at -20°C |
M.Wt | 386.47 |
Cas No. | 319460-85-0 |
Formula | C22H18N4OS |
Synonyms | AG 013736 |
Solubility | insoluble in H2O; ≥19.3 mg/mL in DMSO; ≥3.52 mg/mL in EtOH |
Chemical Name | N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide |
SDF | Download SDF |
Canonical SMILES | CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验: [1] | |
细胞系 |
过表达RTK的PAE细胞,人脐静脉内皮细胞(HUVEC) |
制备方法 |
该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
细胞受体激酶磷酸化实验: 37℃,1 mmol/L Na3VO4存在下45分钟 |
实验结果 |
在转染或内源性RTK表达细胞中,axitinib有效地阻断生长因子刺激的VEGFR-2和VEGFR-3的磷酸化,平均IC50值分别为0.2和0.1至0.3 nmol/L。Axitinib抑制VEGF刺激的HUVEC存活,IC50值为0.17 nmol/L。 |
动物实验: [2] | |
动物模型 |
雌性nu/nu小鼠或重度联合免疫缺陷beige小鼠(年龄7-10周) |
给药剂量 |
Axitinib作为悬浮液以5 mL/kg的剂量口服,每日两次 |
实验结果 |
Axitinib以剂量依赖性方式抑制MV522中的肿瘤生长,基于剂量和相应的TGI(肿瘤生长抑制)之间的关系,ED50值为8.8 mg/kg,每日两次。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Hu-Lowe D D, Zou H Y, Grazzini M L, et al.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, 3. Clinical Cancer Research, 2008, 14(22): 7272-7283. |
描述 | Axitinib是一种多靶点抑制剂,作用于VEGFR1,VEGFR2,VEGFR3,PDGFRβ和c-Kit,IC50值分别为 0.1 nM,0.2 nM,0.1-0.3 nM,1.6 nM和1.7 nM。 | |||||
靶点 | VEGFR1/FLT1 | VEGFR2/Flk1 | VEGFR2/KDR | VEGFR3 | PDGFRβ | c-Kit |
IC50 | 0.1 nM | 0.18 nM | 0.2 nM | 0.1 nM-0.3 nM | 1.6 nM | 1.7 nM |
质量控制和MSDS
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