DGY-06-116
目录号: PL11429 纯度: ≥99%
CAS No. :2556836-50-9
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中文名称
DGY-06-116
英文名称
DGY-06-116
英文别名
DGY-06-116;BDBM50514534;S9643;N-(2-chloro-6-methylphenyl)-2-[4-(4-methylpiperazin-1-yl)anilino]-4-[2-(prop-2-enoylamino)anilino]py
Cas No.
2556836-50-9
分子式
C32H33ClN8O2
分子量
597.11
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
DGY-06-116 是一种不可逆的共价选择性 Src 抑制剂,IC50 为 3 nM。DGY-06-116 抑制 FGFR1 的 IC50 为 8340 nM。
生物活性
DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC 50 of 3nM. DGY-06-116 inhibits FGFR1 with an IC 50 of 8340 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 3 nM (Src), 8340 nM (FGFR1)
体外研究(In Vitro)
DGY-06-116 potently inhibits Src kinase activity with an IC50 of 2.6 nM at 1 h incubation.
DGY-06-116 (Compound 15a; 0.01-10 μM; 72 hours) exhibits potent antiproliferative effects in nonsmall cell lung cancer (NSCLC) and triple negative breast cancer (TNBC) cell lines harboring SRC activation.
15a (1 μM; 2 hours) is capable of inducing potent SRC binding and inhibition of SRC signaling in NSCLC cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
DGY-06-116 (Compound 15a; 5 mg/kg for 3 times every 12 h via intraperitoneal injection) is able to inhibit SRC for an extended duration in adult C57B6 mice, likely due to its ability to covalently bind the target.
DGY-06-116 exhibits a short half-life and high exposure (T 1/2 =1.29 h, AUC=12 746.25 min·ng/mL) following i.p. administration (5 mg/kg) in B6 mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Guangyan Du, et al. Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine. J Med Chem. 2020 Feb 27;63(4):1624-1641.
[2]. Deepak Gurbani, et al. Structure and Characterization of a Covalent Inhibitor of Src Kinase. Front Mol Biosci. 2020 May 19;7:81.
溶解度数据
In Vitro: DMSO : 250 mg/mL (418.68 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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