DGY-06-116 - CAS:2556836-50-9

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DGY-06-116

目录号 : KM5168 CAS No. : 2556836-50-9 纯度 : 98%

Data Sheet 产品使用指南

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。

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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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.

体外研究

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.

Cell Proliferation Assay

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

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

体内研究

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.

Animal Model:	Adult C57B6 mice
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; for 3 times every 12 h
Result:	Led to inhibition of p-SRC 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.

分子式

C₃₂H₃₃ClN₈O₂

分子量

597.11

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。
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。