SKLB610
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SKLB610是VEGFR的选择性抑制剂,IC50值为2.2 μM[1]。
VEGFR(血管内皮生长因子受体)的配体是VEGF,通过与VEGF结合,在刺激细胞应答中发挥重要作用。研究表明,在多种癌症中,VEGFR异常表达,其抑制剂被视为有前景的临床治疗方式[1,2]。
SKLB610是VEGF诱导的VEGFR2磷酸化的强效抑制剂。在人肿瘤细胞系中,SKLB610抑制细胞增殖,IC50值为2.2 μM 到25.6 μM。在HUVECs中,SKLB610抑制VEGF刺激的细胞增殖以及VEGFR2磷酸化,以剂量依赖性方式抑制细胞毛细血管形成[1]。SKLB610在水、乙醇、乙酸乙酯、0.5%的Tween 80和纳米混悬剂的溶解度分别为0.34 μg/ml、16500 μg/ml、380 μg/ml、23 μg/ml和103 μg/ml [2,3]。
在HCT116皮下异种移植小鼠模型中,剂量为12.5 mg/kg、25 mg/kg 和 50 mg/kg 的SKLB610治疗10天,浓度依赖性的显著延迟肿瘤生长。另外,经过30天的治疗,50 mg/kg剂量的SKLB610抑制77.1%的肿瘤体积 [1]。
参考文献:
[1]. Cao, Z.X., et al., SKLB610: a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo. Cell Physiol Biochem, 2011. 27(5): p. 565-74.
[2]. Luo, X., et al., Pharmacokinetic studies of a novel multikinase inhibitor for treating cancer by HPLC-UV. J Chromatogr Sci, 2013. 51(1): p. 17-20.
[3]. Huang, Y., et al., The preparation and evaluation of water-soluble SKLB610 nanosuspensions with improved bioavailability. AAPS PharmSciTech, 2013. 14(3): p. 1236-43.
Physical Appearance | A solid |
Storage | Store at 4°C |
M.Wt | 415.11 |
Cas No. | 1125780-41-7 |
Formula | C21H16F3N3O3 |
Synonyms | SKLB610; SKLB 610; SKLB-610 |
Solubility | insoluble in H2O; ≥20.75 mg/mL in DMSO; ≥23 mg/mL in EtOH with ultrasonic |
Chemical Name | N-methyl-4-(4-(3-(trifluoromethyl)benzamido)phenoxy)picolinamide |
SDF | Download SDF |
Canonical SMILES | FC(F)(F)C1=CC=CC(C(NC2=CC=C(OC3=CC=NC(C(NC)=O)=C3)C=C2)=O)=C1 |
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。 |
Description | SKLB610是血管发生相关的酪氨酸激酶的新型多靶点抑制剂。 | |||||
靶点 | FGFR | |||||
IC50 |
质量控制和MSDS
- 批次:
化学结构
![SKLB610](http://www.apexbt.com//media/diy/images/struct/A8237.png)
相关生物数据
![SKLB610 SKLB610](http://www.apexbt.com/media/diy/images/wb/A8237_1.jpg)
相关生物数据
![SKLB610 SKLB610](http://www.apexbt.com/media/diy/images/wb/A8237_2.jpg)