AIM-100

CAS号

873305-35-2

分子式

C23H21N3O2

主要靶点

ACK

仅限科研使用

Cat No : CM02470

Print datasheet

Synonyms

anticancer|AIM100|AIM-100|AIM 100|Ack1|ACK1|Activated Cdc42 kinase 1|ATM|PSA|NKX3.1|inhibit|Inhibitor|Tyr267|Tyr-phosphorylation|TNK2|TMPRSS2



产品信息

CAS号 873305-35-2
分子式 C23H21N3O2
主要靶点 ACK
主要通路 蛋白酪氨酸激酶
分子量 371.43
纯度 98.75%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 anticancer|AIM100|AIM-100|AIM 100|Ack1|ACK1|Activated Cdc42 kinase 1|ATM|PSA|NKX3.1|inhibit|Inhibitor|Tyr267|Tyr-phosphorylation|TNK2|TMPRSS2

靶点活性

Ack1:24 nM

体外活性

AIM-100不仅抑制了Ack1的激活,还抑制了AKT酪氨酸磷酸化,导致细胞周期在G1阶段停滞[1]。它还能够抑制AR Tyr(267)的磷酸化和其对ATM增强子的招募。值得注意的是,AIM-100抑制了Ack1介导的ATM表达,并减缓了放射线抗性CRPC肿瘤的增长[2]。AIM-100不仅抑制了Ack1的激活,还能抑制pTyr267-AR的磷酸化、AR与PSA、NKX3.1以及TMPRSS2启动子的结合,并抑制AR的转录活性[3]。

溶解度

DMSO:60 mg/mL (161.54 mM);Ethanol:30 mg/mL (80.77 mM)

参考文献

1.Mahajan K, et al. Ack1 tyrosine kinase activation correlates with pancreatic cancer progression. Am J Pathol. 2012 Apr;180(4):1386-93.
2.Mahajan K, et al. Ack1-mediated androgen receptor phosphorylation modulates radiation resistance in castration-resistant prostate cancer. J Biol Chem. 2012 Jun 22;287(26):22112-22.
3.Mahajan K, et al. Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity. Prostate. 2010 Sep 1;70(12):1274-85.

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