Telatinib (BAY 57-9352)
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.
Telatinib (BAY 57-9352)是VEGFR2、VEGFR3、c-Kit和PDGFRα的选择性抑制剂,其IC50值分别为6 nM、4 nM、1 nM和15 nM [1]。
血管内皮生长因子(VEGFR)是VEGF的受体,在刺激血管生成和血管再生中起重要作用。血小板衍生生长因子(PDGF)是生长因子中的一员,参与血管形成。C-Kit是生长因子受体。诸多研究表明VEGFR、c-Kit和PDGFR的异常与多种肿瘤相关[1,2,3]。
Telatinib是高效的VEGFR2/3、c-Kit和PDGFRα抑制剂。在一系列肿瘤细胞系(MDA-MB-231乳腺癌、Colo-205结肠癌、DLD-1结肠癌和H460非小细胞肺癌)中,Telatinib能够抑制参与血管生成进程的VEGFR-2自磷酸化和PDGF-β [2]。
Telatinib用于多种癌症治疗的临床试验,目前取得了可喜的成果[2-4]。
也有报道Telatinib能够恢复肿瘤细胞对抗肿瘤药物的敏感性,并通过抑制ABCG2表达显著降低细胞活力[3]。
参考文献:
[1]. Steeghs, N., et al., Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res, 2008. 14(11): p. 3470-6.
[2]. Strumberg, D., et al., Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours. Br J Cancer, 2008. 99(10): p. 1579-85.
[3]. Sodani, K., et al., Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. Biochem Pharmacol, 2014. 89(1): p. 52-61.
[4]. Eskens, F.A., et al., Phase I dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-Kit, in patients with advanced or metastatic solid tumors. J Clin Oncol, 2009. 27(25): p. 4169-76.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 409.83 |
Cas No. | 332012-40-5 |
Formula | C20H16ClN5O3 |
Synonyms | BAY 579352;BAY 57 9352 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥20.5 mg/mL in DMSO |
Chemical Name | 4-[[4-(4-chloroanilino)furo[2,3-d]pyridazin-7-yl]oxymethyl]-N-methylpyridine-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | CNC(=O)C1=NC=CC(=C1)COC2=NN=C(C3=C2OC=C3)NC4=CC=C(C=C4)Cl |
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 | Telatinib是VEGFR2/3、c-Kit和PDGFRβ的高效抑制剂,其IC50值分别为6 nM/4 nM、 1 nM和15 nM。 | |||||
靶点 | c-Kit | VEGFR3 | VEGFR2 | PDGFRα | ||
IC50 | 1 nM | 4 nM | 6 nM | 15 nM |