KX2-391
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.
KX2-391 是一种高选择性的Src 激酶抑制剂,IC50值为20 nM [1]。
KX2-391 是一种非ATP 竞争性Src抑制剂。KX2-391是第一种靶向Src激酶底物结合位点的抑制剂。KX2-391 抑制Src 催化的FAK、Shc、paxillin转磷酸化以及Src 激酶自磷酸化。KX2-391 对PDGFR、EGFR、JAK1、JAK2 和Lck 没有影响,证明其为选择性抑制剂。KX2-391还是一种微管蛋白聚合抑制剂,通过与异二聚体微管蛋白上特定的位点结合而起抑制作用。在细胞实验中,KX2-391在NIH3T3/c-Src527F和SYF/c-Src527F 细胞中显示出生长抑制作用,GI50 值分别为23 nM 和39 nM [ 1 ,2 ] 。
由于Src 是细胞增殖、存活、迁移和侵袭的调节因子,KX2-391 针对各种实体瘤和许多白血病肿瘤是有效的。已经证实KX2-391抑制原发性肿瘤生长并抑制肿瘤转移[ 2 ]。
参考文献:
[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.
- 1. Michaela T. Reichmann, Liku B Tezera, et al. "Integrated transcriptomic analysis of human tuberculosis granulomas and a biomimetic model identifies therapeutic targets." J Clin Invest. 2021 Aug 2;131(15):e148136. PMID:34128839
- 2. 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
Storage | Store at -20°C |
M.Wt | 431.53 |
Cas No. | 897016-82-9 |
Formula | C26H29N3O3 |
Solubility | insoluble in H2O; ≥121 mg/mL in DMSO; ≥2.44 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | N-benzyl-2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]acetamide |
SDF | Download SDF |
Canonical SMILES | C1COCCN1CCOC2=CC=C(C=C2)C3=CN=C(C=C3)CC(=O)NCC4=CC=CC=C4 |
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。 |
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. |
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) |
质量控制和MSDS
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