DGY-06-116

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

DGY-06-116  纯度: 99.38%

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。

DGY-06-116

DGY-06-116 Chemical Structure

CAS No. : 2556836-50-9

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DGY-06-116 相关产品

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生物活性

DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC50 of 3nM. DGY-06-116 inhibits FGFR1 with an IC50 of 8340 nM[1].

IC50 & Target

IC50: 3 nM (Src), 8340 nM (FGFR1)[1]
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[2].
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[1].
15a (1 μM; 2 hours) is capable of inducing potent SRC binding and inhibition of SRC signaling in NSCLC cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: H1975 (nonsmall cell lung cancer, NSCLC), HCC827 (NSCLC), and MDA-MB-231 (triple negative breast cancer, TNBC) cell lines
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Induced strong growth inhibitory effects across all three cell lines with GR50 values of 0.3, 0.5, and 0.3 μM for H1975, HCC827, and MDA-MB-231, respectively.

Western Blot Analysis[1]

Cell Line: H1975 and HCC827 NSCLC cells
Concentration: 1 μM
Incubation Time: 2 hours
Result: Inhibited p-SRCY416 signaling in both H1975 and HCC827 cells.

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[1].
DGY-06-116 exhibits a short half-life and high exposure (T1/2=1.29 h, AUC=12 746.25 min·ng/mL) following i.p. administration (5 mg/kg) in B6 mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult C57B6 mice[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; for 3 times every 12 h
Result: Led to inhibition of p-SRCY416 at 2 and 4 h postdosing, compared to the vehicle controls.
Demonstrated SRC binding and inhibition at both 2 and 4 h postdosing compared to the vehicle controls.

分子量

597.11

Formula

C32H33ClN8O2
CAS 号

2556836-50-9
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (418.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6747 mL 8.3737 mL 16.7473 mL
5 mM 0.3349 mL 1.6747 mL 3.3495 mL
10 mM 0.1675 mL 0.8374 mL 1.6747 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.48 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.48 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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