|6,7-二甲氧基-N-(2-甲基-4-苯氧基苯基)喹唑啉-4-胺盐酸盐|CsnPharm

CAS No.: 2002381-31-7

6,7-二甲氧基-N-(2-甲基-4-苯氧基苯基)喹唑啉-4-胺盐酸盐 Catalog No. CSN18997

Synonyms: APS-2-79 (hydrochloride);APS-2-79 HCl

APS-2-79 HCl is a KSR (Kinase suppressor of Ras)-dependent MAPK modulator which can stabilize KSR inactive state with an IC50 value of 120 nM, resulting in inhibition of oncogenic Ras signaling, antagonizing the Ras–MAPK pathway.

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技术信息

生物活性

描述The RAS/RAF/MEK/ERK and PI3K/AKT/mTOR signaling pathways have been identified as promising therapeutic targets for cancer therapy. Over-activation of these pathways and their components including gene mutations has been considered as one of the major causes of melanoma. Mitogen-activated protein kinase (MEK) is a downstream kinase of RAS pathway found in two different forms MEK1/2^[2]. APS-2-79 hydrochloride behaves as a kinase suppressor of Ras (KSR)-dependent antagonist of RAF-mediated MEK phosphorylation. APS-2-79 binds directly to KSR2 within the KSR2-MEK1 complex with an IC₅₀ of 120 ± 23 nM for KSR2^[3]. APS-2-79 (1 μM) shifts the cell viability dose response to Trametinib in Ras-mutant cell lines HCT-116 and A549, but not BRAF mutant cell lines SK-MEL-239 and A375. Although the cellular effects of APS-2-79 alone are modest, combination analysis over full concentration matrices reveal that kinase suppressor of Ras (KSR)-inactive state (KSRi) synergizes with Trametinib, and other MEK inhibitors, specifically in KRAS mutant cell lines. APS-3-77, and additional control compounds, do not demonstrate Ras-mutant-specific synergy, supporting the hypothesis that the enhanced activity of Trametinib when combined with APS-2-79 depends on co-modulation of KSR^[3].
参考文献

[1] Dhawan NS, Scopton AP, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1;537(7618):112-116.
[2] Mahapatra DK, Asati V, Bharti SK. MEK inhibitors in oncology: a patent review (2015-Present). Expert Opin Ther Pat. 2017 Aug;27(8):887-906. doi: 10.1080/13543776.2017.1339688. Epub 2017 Jun 19. PMID: 28594589.
[3] Dhawan NS, Scopton AP, Dar AC. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1;537(7618):112-116. doi: 10.1038/nature19327. Epub 2016 Aug 24. PMID: 27556948; PMCID: PMC5161575.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3591 mL
- 11.7955 mL
- 23.5909 mL
- 5 mM
- 0.4718 mL
- 2.3591 mL
- 4.7182 mL
- 10 mM
- 0.2359 mL
- 1.1795 mL
- 2.3591 mL

技术信息

CAS号

2002381-31-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H22ClN3O3

运输

蓝冰

分子量

423.89

别名

APS-2-79 (hydrochloride);APS-2-79 HCl

溶解度

DMSO	70.0 mg/mL (165.1 mM)
Water	insoluble

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6,7-二甲氧基-N-(2-甲基-4-苯氧基苯基)喹唑啉-4-胺 盐酸盐 Catalog No. CSN18997

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确认信息

6,7-二甲氧基-N-(2-甲基-4-苯氧基苯基)喹唑啉-4-胺盐酸盐 Catalog No. CSN18997