Pelitinib (EKB-569)
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.
Ponatinib(也称EKB-569),一种3-氰基喹啉,是有效的表皮生长因子受体(EGF-R)酪氨酸激酶不可逆抑制剂,可以抑制EGF-R活性,其体外IC50值为38.5 nM[1]。
据发现,Ponatinib对过表达EGF-R的肿瘤细胞显现出有效的抗增殖活性,包括NHEK、A431和MDA-468细胞,其对应的IC50值分别为61 nM、125 nM和260 nM。同时,在A431和NHEK细胞中,Ponatinib也能有效抑制EGF诱导的VEGFR(EGFR)磷酸化,其IC50值范围为20 nM ~ 80 nM[2]。
参考文献:
[1] Torrance CJ, Jackson PE, Montgomery E, Kinzler KW, Vogelstein B, Wissner A, Nunes M, Frost P, Discafani CM. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6(9):1024-8.
[2] Nunes M, Shi C, Greenberger LM. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Mol Cancer Ther. 2004 Jan;3(1):21-7.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 467.92 |
Cas No. | 257933-82-7 |
Formula | C24H23ClFN5O2 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥11.7 mg/mL in DMSO |
Chemical Name | (E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide |
SDF | Download SDF |
Canonical SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)C=CCN(C)C |
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 | Pelitinib是有效的EGFR不可逆抑制剂,其IC50值为38.5 nM。 | |||||
靶点 | EGFR | |||||
IC50 | 38.5 nM |
质量控制和MSDS
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