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KX2-391

现货
Catalog No.
B2282
高选择性的Src抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 760.00
现货
10mg
¥ 1,430.00
现货
50mg
¥ 4,110.00
现货
250mg
¥ 12,340.00
现货

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Background

KX2-391 is a highly selective inhibitor of Src kinase with IC50 value of 20nM [1].

KX2-391 is a non-ATP competitive inhibitor of Src. It is the first inhibitor that targets Src kinase within the substrate binding site. KX2-391 inhibits Src catalyzed trans-phosphorylation of FAK, Shc, paxillin as well as Src kinase autophosphorylation. KX2-391 has no effects on PDGFR, EGFR, JAK1, JAK2 and Lck demonstrating it as a selective inhibitor. It is also found to be an inhibitor of tubulin polymerization through binding to the unique confirmation on heterodimeric tubulin. In cellular assays, KX2-391 shows growth inhibition in NIH3T3/c-Src527F cells and SYF/c-Src527F cells with GI50 values of 23nM and 39nM, respectively [1, 2].

Since Src acts as a regulator in cell proliferation survival, motility and invasiveness, KX2-391 is potent against a variety of solid tumors and many leukemia tumors. It is shown to inhibit primary tumor growth and to suppress metastasis [2].

References:
[1] Fallah-Tafti A, Foroumadi A, Tiwari R, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: Synthesis, Src kinase inhibitory and anticancer activities. European journal of medicinal chemistry, 2011, 46(10): 4853-4858.
[2] Naing A, Cohen R, Dy G K, et al. A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket-directed SRC inhibitor, in patients with advanced malignancies. Investigational new drugs, 2013, 31(4): 967-973.

文献引用

1.Chen Y, Yu Y, et al. "Bradykinin promotes migration and invasion of hepatocellular carcinoma cells through TRPM7 and MMP2." Exp Cell Res. 2016 Sep 29. PMID:27693494

Chemical Properties

StorageStore at -20°C
M.Wt431.53
Cas No.897016-82-9
FormulaC26H29N3O3
Solubility≥121mg/mL in DMSO
Chemical NameN-benzyl-2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]acetamide
SDFDownload SDF
Canonical SMILESC1COCCN1CCOC2=CC=C(C=C2)C3=CN=C(C=C3)CC(=O)NCC4=CC=CC=C4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

细胞实验[1-3]:

细胞系

HCC细胞系Huh7、PLC/PRF/5、Hep3B和HepG2

溶解方法

该化合物在DMSO中的溶解度大于121mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

6,564 -0.012 nM,3天

应用

KX2-391抑制所有四种HCC细胞株Huh7、PLC/PRF/5、Hep3B和HepG2的GI50为9 nM、13 nM、26 nM和60 nM。在NIH3T3/c-Src527F和SYF/c-Src527F细胞中,KX2-391抑制细胞生长的GI50分别为23 nM和39 nM。KXO1(10-30 nM)可以将具有活化水平的SFK的一组人癌细胞系的细胞增殖率(GI50)减半,如HT-29人结肠癌细胞及NIH3T3/c-Src527F细胞。KXO1抑制HT-29和3T3/c-Src527F细胞的锚定依赖性生长。

动物实验[3]:

动物模型

携带50cc HT-29肿瘤的裸鼠

给药剂量

口服,5 mg/kg,每天2次

应用

在携带50cc HT-29肿瘤的裸鼠中,口服5 mg/kg KXO1 bid导致肿瘤生长减少70%,通过体重减轻测定证明其对宿主没有显著毒性。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Lau G M, Lau G M, Yu G L, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro[J]. Digestive diseases and sciences, 2009, 54(7): 1465-1474.

[2]. Fallah-Tafti A, Foroumadi A, Tiwari R, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities[J]. European journal of medicinal chemistry, 2011, 46(10): 4853-4858.

[3]. Bu Y, Gao L, Smolinski M, et al. KXO1 (KX2-391), a Src-family kinase inhibitor targeting the peptide-binding domain, suppresses oncogenic proliferation in vitro and in vivo[J]. 2008.

生物活性

描述 KX2-391 是一种Src (拟肽类)抑制剂,在癌细胞系中的GI50 值为9-60 nM。
靶点 Src (HuH7) Src (PLC/PRF/5) Src (Hep 3B) Src (Hep G2)    
IC50 9 nM(GI50) 13 nM(GI50) 26 nM(GI50) 60 nM(GI50)    

质量控制

化学结构

KX2-391

相关生物数据

KX2-391