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AIM-100

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Chemical Structure| 873305-35-2 同义名 : -
CAS号 : 873305-35-2
货号 : A925431
分子式 : C23H21N3O2
纯度 : 99%+
分子量 : 371.432
MDL号 : MFCD22417088
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(134.61 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 AIM-100 is an Ack1 inhibitor. It inhibited EGF induced Ack1 activation on Tyr284 site at concentration of 0.8μM for 16h in serum-depleted MEFs, and suppressed EGF induced pTyr267-AR phosphorylation in serum and androgen-depleted LAPC4 cells. Treatment with 0.8μM AIM-100 for 16h inhibited pTyr267-AR binding to AREs, binding of AR to PSA, NKX3.1, and TMPRSS2 promoters in serum and androgen depleted LAPC4 cells and suppressed androgen-independent pTyr267-AR transcriptional activity and PSA gene expression[4]. AIM-100 suppressed Ack1 mediated ATM expression and mitigated the growth of radioresistant CRPC (castration-resistant prostate cancer) tumors[5]. AIM-100 promoted dramatic oligomerization, clustering and CIE (Clathrin-independent endocytosis) of human and mouse dopamine transporters (DAT), through an allosteric mechanism associated with the DAT conformational state[6].
作用机制 AIM-100 inhibits pTyr267-AR binding to AREs, binding of AR to PSA, NKX3.1, and TMPRSS2 promoters.[4]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL
参考文献

[1]Mahajan K, Challa S, et al. Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity. Prostate. 2010 Sep 1;70(12):1274-85.

[2]Mahajan K, Coppola D, 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]Sorkina T, Ma S, et al. Small molecule induced oligomerization, clustering and clathrin-independent endocytosis of the dopamine transporter. Elife. 2018 Apr 9;7. pii: e32293.

[4]Mahajan K, Challa S, Coppola D, Lawrence H, Luo Y, Gevariya H, Zhu W, Chen YA, Lawrence NJ, Mahajan NP. Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity. Prostate. 2010 Sep 1;70(12):1274-85. doi: 10.1002/pros.21163. PMID: 20623637; PMCID: PMC3953126.

[5]Mahajan K, Coppola D, Rawal B, Chen YA, Lawrence HR, Engelman RW, Lawrence NJ, Mahajan NP. Ack1-mediated androgen receptor phosphorylation modulates radiation resistance in castration-resistant prostate cancer. J Biol Chem. 2012 Jun 22;287(26):22112-22. doi: 10.1074/jbc.M112.357384. Epub 2012 May 7. PMID: 22566699; PMCID: PMC3381169.

[6]Sorkina T, Ma S, Larsen MB, Watkins SC, Sorkin A. Small molecule induced oligomerization, clustering and clathrin-independent endocytosis of the dopamine transporter. Elife. 2018 Apr 9;7:e32293. doi: 10.7554/eLife.32293. PMID: 29630493; PMCID: PMC5896956.