CEP-37440
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.
对SUM190细胞系增殖的IC50值为1000 nM.
黏着斑激酶FAK1是一种胞质酪氨酸激酶,位于粘着斑,控制包括细胞增殖\活力和存活的多个细胞信号通路.间变性淋巴瘤激酶1(ALK-1)是胰岛素受体酪氨酸激酶家族的一员.ALK突变与非小细胞肺癌(NSCLC)和其他实体瘤的发病有关.CEP-37440 是一种有效的ALK和FAK1的高选择性双重抑制剂.
体外试验:浓度为300 nM的CEP-37440能够减少三阴性FC-IBC02细胞系的增殖,1000 nM的CEP-37440能够完全抑制这些细胞的增殖.在敏感性IBC细胞系中,参与如细胞生长和增殖\细胞周期\细胞死亡和存活\细胞运动\细胞间信号转导和相互作用等细胞功能的基因可由CEP-37440差异性调节.其中,TGFβ1和MMP3 被CEP-37440下调,而DKK3\CAV1和TFPI2被CEP-37440上调,这可能是由其对ALK和FAK1的双重抑制作用导致的[1].
体内试验:在FC-IBC02 原位乳腺癌异种移植模型中,CEP-37440能够减少原始肿瘤的生长,并抑制脑内自发转移的发展[1].
临床试验:目前在临床I期试验中,CEP-37440作为一种ALK/FAK双重抑制剂,测定其对晚期或转移性实体瘤患者的最大耐受剂量(MTD)(NCT01922752).
参考文献:
[1] Abstract 3232: CEP-37440, a highly selective and potent dual inhibitor of ALK and FAK1 inhibits the proliferation of inflammatory breast cancer cells. Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 580.12 |
Cas No. | 1391712-60-9 |
Formula | C30H38ClN7O3 |
Solubility | insoluble in H2O; ≥11.37 mg/mL in EtOH; ≥9.25 mg/mL in DMSO with gentle warming |
Chemical Name | (Z)-2-((E)-(5-chloro-2-(((S)-6-(4-(2-hydroxyethyl)piperazin-1-yl)-1-methoxy-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)amino)pyrimidin-4(3H)-ylidene)amino)-N-methylbenzimidic acid |
SDF | Download SDF |
Canonical SMILES | C/N=C(O)/C1=CC=CC=C1/N=C(N2)\C(Cl)=CN=C2NC3=C(OC)C(CCC[C@@](N4CCN(CCO)CC4)([H])C5)=C5C=C3 |
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。 |
质量控制和MSDS
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