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Src Inhibitor 1

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Chemical Structure| 179248-59-0 同义名 : Src Kinase Inhibitor 1;Src-l1;Src I1;Src Kinase Inhibitor I
CAS号 : 179248-59-0
货号 : A523201
分子式 : C22H19N3O3
纯度 : 99%
分子量 : 373.405
MDL号 : MFCD01815300
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 8 mg/mL(21.42 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The Src family of nonreceptor tyrosine kinases regulates numerous cellular processes, including proliferation, differentiation, migration, survival and angiogenesis. In solid tumors, Src is frequently aberrantly active, and promotes tumor progression and metastasis[3]. Six of Src family kinases (Fyn, Lyn, Fgr, Hck, Src and Yes), are present in megakaryocytes (Mks). Src kinases are negative factors of megakaryocytopoiesis induced by thrombopoietin. The inhibitors of Src kinases might be useful as agents inducing maturation of Mks[4]. Src is highly expressed in CNS neurons and contributes not only to developmental proliferation and differentiation but also to high-order brain functions, such as those contributing to alcohol consumption. Src knock-out mice exhibit no CNS abnormalities, presumably due to compensation by other Src family kinases (SFKs), but have a shortened lifespan and osteopetrosis-associated defects, impeding investigations of the role of Src on behavior in adult mice[5]. Src-I1, is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency[6]. Src-I1 is competitive with both ATP and peptide binding sites of the kinase. The IC50 values are 44 and 88 nM for Src and Lck, respectively[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.68mL

0.54mL

0.27mL

13.39mL

2.68mL

1.34mL

26.78mL

5.36mL

2.68mL
参考文献

[1]Bain J, Plater L, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.

[2]Tian G, Cory M, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.

[3] Ami N Shah,et al. Src, chemoresistance and epithelial to mesenchymal transition: are they related? Anticancer Drugs. 2007 Apr;18(4):371-5.

[4]Joanna Kamińska,et al. Src kinases in the process of maturation megakryocyte progenitors. Postepy Biochem. 2008;54(4):378-83.

[5]Goro Kato. Nonphosphorylatable Src Ser75 Mutation Increases Ethanol Preference and Consumption in Mice. eNeuro.2019 Apr 5;6(2):ENEURO.0418-18.2019.

[6]Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.

[7]Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.