SKLB1002
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.
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
