SKLB1002
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SKLB1002是有效的VEGF受体2抑制剂,其IC50值为32 nM[1].
VEGF受体2(VEGFR2)是血管内皮生长因子(VEGF)的主要受体之一,在血管生成和VEGF刺激的培养内皮细胞的增殖\迁移以及出芽方面起着重要作用[1].
SKLB1002是一种有效的VEGFR2抑制剂.在人脐静脉内皮细胞(HUVEC)中,SKLB1002显著抑制VEGF诱导的HUVEC增殖,其IC50值为11.9 μM.此外,SKLB1002呈剂量依赖性地抑制HUVEC迁移\侵袭以及管形成.SKLB1002(10 μM)显著抑制VEGF诱导的VEGFR2\ERK\Src以及FAK磷酸化[1].
在斑马鱼胚胎中,SB1002(2.5 μM)显著抑制节间血管生长.在SW620或HepG2细胞异种移植小鼠中,SB1002(100 mg/kg)显著抑制肿瘤体积,并抑制60%的肿瘤生长.此外,SKLB1002降低微血管密度[1].在4T1肿瘤小鼠模型中,SKLB1002显著降低肿瘤血管密度[2].
参考文献:
[1]. Zhang S, Cao Z, Tian H, et al. SKLB1002, a novel potent inhibitor of VEGF receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo. Clin Cancer Res, 2011, 17(13): 4439-4450.
[2]. Shen G, Li Y, Du T, et al. SKLB1002, a novel inhibitor of VEGF receptor 2 signaling, induces vascular normalization to improve systemically administered chemotherapy efficacy. Neoplasma, 2012, 59(5): 486-493.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 320.39 |
Cas No. | 1225451-84-2 |
Formula | C13H12N4O2S2 |
Solubility | insoluble in H2O; ≥5 mg/mL in EtOH with gentle warming and ultrasonic; ≥8 mg/mL in DMSO |
Chemical Name | 2-(6,7-dimethoxyquinazolin-4-yl)sulfanyl-5-methyl-1,3,4-thiadiazole |
SDF | Download SDF |
Canonical SMILES | CC1=NN=C(S1)SC2=NC=NC3=CC(=C(C=C32)OC)OC |
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 | SKLB1002是有效的VEGF受体2(VEGFR2)抑制剂,其IC50值为32 nM. | |||||
靶点 | VEGFR2 | |||||
IC50 | 32 nM |
质量控制和MSDS
- 批次:
化学结构
![SKLB1002](http://www.apexbt.com//media/diy/images/struct/B1305.png)