9-ING-41 - CAS:1034895-42-5

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9-ING-41

目录号 : KM4536 CAS No. : 1034895-42-5 纯度 : 98%

Data Sheet SDS 产品使用指南

9-ING-41 是一种基于马来酰亚胺的 ATP 竞争性和选择性的糖原合酶激酶-3β (GSK-3β) 抑制剂，IC₅₀ 为 0.71 μM。9-ING-41 显著导致癌细胞的细胞周期停滞，自噬和凋亡。9-ING-41 具有抗癌活性，并具有增强化疗药物抗肿瘤作用的潜力。

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5mg		In-stock
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

9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC₅₀ of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs.

IC₅₀&Target

GSK-3β

0.71 μM (IC₅₀)

体外研究

9-ING-41 (2, 4 μM; 48 hours) decreases neuroblastoma cell viability induces apoptosis.
9-ING-41 (1, 2 μM; 24 hours) is a potent cell cycle-blocking agent for lymphoma cells.
9-ING-41 (10 μM; for 72 hours) increases the expression of LC3, an autophagy marker.
9-ING-41 (compound 26; 5 μM; for 6, 12, 24, 36 h) results in a pronounced decrease in NFκB-mediated expression of XIAP, the most potent antiapoptotic protein, leading to subsequent apoptosis in BXPC3 pancreatic cancer cells.
9-ING-41 (0.5, 1.0, 1.5, 2.0 μM) inhibits the proliferation rate of all TCL and MCL lines with concentrations as low as 1.0 mM.
9-ING-41 (10 μM; for 72 hours) causes cell cycle blockage at G2/M after 24 hours. 9-ING-41 treatment induces apoptotic cell death in bladder cancer cells.
9-ING-41 (25 μM; for 96 hours) significantly decreases expression of Cdk1 and Cyclin B1 proteins and leads to a decreased expression of antiapoptotic molecules, Bcl-2 and XIAP.
9-ING-41 (0.1-1 µM) inhibits GSK-3 leading to a decreased expression of the NF-κB target XIAP and significant apoptosis in neuroblastoma cells as shown by PARP cleavage, an apoptosis marker.

Cell Viability Assay

Cell Line:	TCL and MCL lines
Concentration:	2, 4 μM
Incubation Time:	48 hours
Result:	Induced apoptosis.

Cell Cycle Analysis

Cell Line:	Lymphoma cells (Jeko, Mino, and OCI-Ly cell lines)
Concentration:	1, 2 μM
Incubation Time:	24 hours
Result:	Led to cell cycle arrest in G2/M.

Cell Autophagy Assay

Cell Line:	T24 cancer cells
Concentration:	25 μM
Incubation Time:	24 hours
Result:	Showed extensive vacuolation and formation of autophagosome like structures in the cytoplasm. Showed an increased expression of LC3, an autophagy marker.

Western Blot Analysis

Cell Line:	SK-N-DZ and SK-N-BE neuroblastoma cells
Concentration:	0.1, 1 µM
Incubation Time:	48 hours
Result:	Inhibited GSK-3 leading to a decreased expression of the NF-κB target XIAP.

体内研究

9-ING-41 (40 mg/kg/every other day; for 17 days) has single-agent antitumor activity in a mouse model of MCL.

Animal Model:	NSG (NOD.Cg-PrkdcIl2rg/SzJ) mice
Dosage:	40 mg/kg
Administration:	Every other day; for 17 days
Result:	Had single-agent antitumor activity in a mouse model of MCL.

分子式

C₂₂H₁₃FN₂O₅

分子量

404.35

CAS号

1034895-42-5

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 : 50 mg/mL (123.66 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4731 mL	12.3655 mL	24.7310 mL
5 mM	0.4946 mL	2.4731 mL	4.9462 mL
10 mM	0.2473 mL	1.2366 mL	2.4731 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: 2.5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.18 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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。

临床试验

纯度： 98%

Data Sheet

SDS

产品使用指南

暂无相关参考文献

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器