| Identification | Back Directory | [Name]
(E)-N'-(4-(diethylamino)-2-hydroxybenzylidene)nicotinohydrazide | [CAS]
1375060-02-8 | [Synonyms]
SCFSkp2-IN-2
(E)-N'-(4-(diethylamino)-2-hydroxybenzylidene)nicotinohydrazide
3-Pyridinecarboxylic acid, (2E)-2-[[4-(diethylamino)-2-hydroxyphenyl]methylene]hydrazide | [Molecular Formula]
C17H20N4O2 | [MOL File]
1375060-02-8.mol | [Molecular Weight]
312.37 |
| Hazard Information | Back Directory | [Uses]
SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities[1]. | [in vivo]
SCFSkp2-IN-2 (Compound AAA-237) (15 or 45?mg/kg; i.p.; daily for 14 days) shows antitumor activity in lung cancer A549 xenograft mice model[1]. | Animal Model: | A549 xenograft model[1] | | Dosage: | 15 or 45?mg/kg | | Administration: | Intraperitoneal administration, daily for 14 days | | Result: | Significantly reduced tumor volume and weight. The tumor growth inhibition of the low dose and high dose was 55% and 64%, respectively. No obvious weight loss or abnormal behavior was observed. Reduced the expression of Ki67 in tumor tissue. Reduced the expression of Skp2 and Bcl-2 and increased the expression of p27, the cleaving of caspase 3, caspase 9, PARP and Bax. |
| [References]
[1] Liu J, et al. Anti-tumor effects of Skp2 inhibitor AAA-237 on NSCLC by arresting cell cycle at G0/G1 phase and inducing senescence. Pharmacol Res. 2022 Jul;181:106259. DOI:10.1016/j.phrs.2022.106259 |
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PHARMEKS Ltd.
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+7 (495) 702-9648 |
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www.pharmeks.com |
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