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 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。

规格	价格	是否有货
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.

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

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

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

质量

浓度

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The dilution calculator equation

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

浓度

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浓度

体积

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Other Forms of Rapamycin:

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