Axitinib是一种多靶点抑制剂，作用于VEGFR-1， VEGFR-2，VEGFR-3，PDGFR-β和c-KIT时，其IC50分别为0.1 nM， 0.2 nM， 0.1-0.3 nM， 1.6 nM和1.7 nM。
别名：AG-013736
Axitinib是一种多靶点抑制剂，作用于VEGFR-1， VEGFR-2，VEGFR-3，PDGFR-β和c-KIT时，其IC50分别为0.1 nM， 0.2 nM， 0.1-0.3 nM， 1.6 nM和1.7 nM。Axitinib是受体激酶抑制剂，作用于VEGFR-1, VEGFR-2，VEGFR-3， PDGFR-β和c-KIT时IC50分别为0.1 , 0.2, 0.1-0.3, 1.6 和1.7 nM 。Axitinib可以阻断VEGFR的自磷酸化作用，VEGF调节的内皮细胞活力，微管形成，及下游信号。Axitinib抑制多种细胞系的增殖，如作用于IGR-N91, IGR-NB8, SH-SY5Y ，无VEGF刺激的HUVEC时IC50分别为>1000 nM, 849 nM, 274 nM和573 nM。
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Axitinib购买自AbMole
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Nutlin-3-Induced Sensitization of Non-Small Cell Lung Cancer Stem Cells to Axitinib-Induced Apoptosis Through Repression of Akt1/Wnt Signaling.
Axitinib购买自AbMole
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Complementary actions of dopamine D2 receptor agonist and anti-vegf therapy on tumoral vessel normalization in a transgenic mouse model
Axitinib购买自AbMole
 . figure 6.[1].jpg) |
数据来源 | Int J Cancer (2017) . Figure 6. Axitinib (20 mg/kg, Abmole Bioscience) |
| 方法 | ||
| 细胞系/动物模型 | Hmga2/T mice | |
| 浓度 | 20mg/kg | |
| 处理时间 | 6 weeks | |
| 实验结果 | Together, these results show that, while bromocriptine and/or axitinib were able to correct structuralabnormalities of tumoral vessels with a similar efficacy, only the combination treatment restored their function. |
 . figure 5..jpg) |
数据来源 | Int J Cancer (2017) . Figure 5. Axitinib (20 mg/kg, Abmole Bioscience) |
| 方法 | ||
| 细胞系/动物模型 | Hmga2/T mice | |
| 浓度 | 20mg/kg | |
| 处理时间 | 6 weeks | |
| 实验结果 | Analysis of pituitary vasculature in various conditions and morphometric measurements of blood vessels demonstrate that D2R agonist or axitinib had an equivalent capacity to improve structural defects present in tumoral blood vessels and that the combination treatment did not lead to a significant advantage. |
 . figure 4..jpg) |
数据来源 | Int J Cancer (2017) . Figure 4. Axitinib (20 mg/kg, Abmole Bioscience) |
| 方法 | ||
| 细胞系/动物模型 | Hmga2/T mice | |
| 浓度 | 20mg/kg | |
| 处理时间 | 6 weeks | |
| 实验结果 | Importantly, the expression of Angpt1 and Prok1, which was upregulated in response to bromocriptine treatment, was unchanged and remained low after axitinib treatment (Fig. 4d). |
| 细胞实验 | |
|---|---|
| 细胞系 | HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cell lines |
| 方法 | MTS cell proliferation assay HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cell lines were seeded at 5,000 cells per well in a 96-well plate and left to settle overnight in EMBV R-2 or DMEM with 10% fetal calf serum. The cells were treated with axitinib at concentrations ranging from 1 nmol/l to 10 lmol/l. Cell viability was determined after 72 hr using MTS tetrazolium substrate (CellTiter 96 Aqueous One Solution Cell Proliferation Assay; Promega Corporation, Charbonnieres, France) and colorimetric measurement at 490 nm in an automatic plate reader (Elx808; Fisher Bioblock Scientific SAS, Illkirch, France). IC50 values were calculated using GraphPadV R Prism software (version 3.00). |
| 浓度 | 1 nM - 10 μM |
| 处理时间 | 72 hr |
| 动物实验 | |
|---|---|
| 动物模型 | IGR-N91 xenografts with female SPF-Swiss athymic nude mice at 6–8 weeks of age |
| 配制 | 0.5% CMC |
| 剂量 | 30 mg/kg BID for 2 weeks |
| 给药处理 | oral gavage |
| 分子量 | 386.47 |
| 分子式 | C22H18N4OS |
| CAS号 | 319460-85-0 |
| 溶解性（25°C） | DMSO ≥ 20 mg/mL |
| 储存条件 |
粉末型式 -20°C 3年；4°C 2年 溶于溶剂 -80°C 6个月；-20°C 1个月 |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
以下数据基于产品分子量，对于具体产品，请根据在不同溶剂中的溶解度和COA中的说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.5875 mL | 12.9376 mL | 25.8752 mL |
| 5 mM | 0.5175 mL | 2.5875 mL | 5.175 mL |
| 10 mM | 0.2588 mL | 1.2938 mL | 2.5875 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
| 其他相关的VEGFR/PDGFR产品 |
|---|
| Toceranib phosphate
Toceranib phosphate is a multitargeted indolinone receptor tyrosine kinase (RTK) inhibitor with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. |
| Seralutinib (GB002)
Seralutinib (PK10571, GB002) is a novel PDGFR kinase inhibitor with IC50s of 8 nM and 10 nM for PDGFRα and PDGFRβ in enzyme assays, respectively. |
| SU5204
SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively. |
| CS-2660 (JNJ-38158471)
CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM，while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3. |
| Vorolanib (X-82)
Vorolanib is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities. |
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