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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Axitinib购买自AbMole
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Axitinib购买自AbMole
细胞实验 | |
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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 | |
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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 |
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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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