AIM-100
(Synonyms: 5,6-二苯基-N-[[(2S)-四氢-2-呋喃基]甲基]呋喃并[2,3-D]嘧啶-4-胺,AIM 100;AIM100) 目录号 : GC16228
An ACK1/TNK2 inhibitor
Cas No.:873305-35-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
AIM-100 is a small inhibitor of Ack1 tyrosine kinase with IC50 value of 24 nM [1].
AIM-100 mimicked ATP and inhibited the activity of Ack1 significantly and specifically. It showed no inhibition activity for the other 30 kinases including PI3-kinase and AKT, and showed a five-fold higher IC50 value for Lck. In MEF cells treated with EGF, AIM-100 caused a remarkable decrease of the activation of Ack1. In the human prostate cancer cells LNCaP and LAPC4, AIM-100 treatment resulted in an increase of G0/G1 cell phase and subsequent cell growth suppression. These effects of AIM-100 also exerted in the pancreatic cancer cells. AIM-100 induced apoptosis in Panc-1 cells at concentration of 10 μM. Moreover, AIM-100 inhibited cell growth with GI50 values of 7 to 8 μM in CD-18, Panc-1, OV90, MCF-7 and MDA-MB-468 cancer cells [1, 2].
References:
1. Mahajan K, Challa S, Coppola D, et al. Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity. The Prostate, 2010, 70(12): 1274-1285.
2. Mahajan K, Coppola D, Chen Y, et al. Ack1 tyrosine kinase activation correlates with pancreatic cancer progression. The American journal of pathology, 2012, 180(4): 1386-1393.
| Cas No. | 873305-35-2 | SDF | |
| 别名 | 5,6-二苯基-N-[[(2S)-四氢-2-呋喃基]甲基]呋喃并[2,3-D]嘧啶-4-胺,AIM 100;AIM100 | ||
| 化学名 | N-[[(2S)-oxolan-2-yl]methyl]-5,6-diphenylfuro[2,3-d]pyrimidin-4-amine | ||
| Canonical SMILES | C1CC(OC1)CNC2=C3C(=C(OC3=NC=N2)C4=CC=CC=C4)C5=CC=CC=C5 | ||
| 分子式 | C23H21N3O2 | 分子量 | 371.43 |
| 溶解度 | ≥ 36 mg/mL in DMSO with gentle warming, ≥ 35.8 mg/mL in EtOH with gentle warming | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6923 mL | 13.4615 mL | 26.923 mL |
| 5 mM | 0.5385 mL | 2.6923 mL | 5.3846 mL |
| 10 mM | 0.2692 mL | 1.3461 mL | 2.6923 mL |
| 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 | g | |
每只动物给药体积 | ul | |
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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。