|3-(3-氨基丙氧基)-N-(2-((3-((4-4-氯-2-羟基苯基)氨基甲酰基)萘-2-基)氧基)乙基)-2-萘甲酰胺盐酸盐|CsnPharm

CAS No.: 1433286-70-4

666-15 Catalog No. CSN24157

Synonyms: Compound 3i

666-15 is a potent and cell-permeable inhibitor of cAMP-response element binding protein (CREB) with efficacious anti-cancer activity both in vitro and in vivo.

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技术信息

生物活性

描述cAMP-response element binding protein (CREB) is a nuclear transcription factor that has been implicated in the pathogenesis and maintenance of various types of human cancers. Identification of small molecule inhibitors of CREB-mediated gene transcription has been pursued as a novel strategy for developing cancer therapeutics^[1].666-15 is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM). 666-15 also potently inhibited cancer cell growth without harming normal cells^[2].In anin vivo MDA-MB-468 xenograft model, 666-15 completely suppressed the tumor growth without overt toxicity. 666-15 was found to be readily bioavailable to achieve pharmacologically relevant concentrations for CREB inhibition. The mice treated with 666-15 showed no evidence of changes in body weight, complete blood count, blood chemistry profile, cardiac contractility and tissue histologies from liver, kidney, and heart^[3].Inhibition of CREB's transcriptional activity with 666-15 dramatically enhanced apoptosis in PC12 cells by downregulating B-cell lymphoma 2 (Bcl-2)^[4]. 666-15 compound could effectively reverse the anti-inflammatory effect of CBL in primary mouse microglia cells and anti-ischemic brain injury of cerebrolysin in rats subjected to transient middle cerebral artery occlusion(tMAO)^[5].After 666-15 or SR-18292 treatment, such protective effect of PEG-IGF-1 can be attenuated, and the mice suffered from the re-deterioration of behavioral and mitochondrial abnormalities in hippocampus^[6].
参考文献

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
- 1.6115 mL
- 8.0577 mL
- 16.1155 mL
- 5 mM
- 0.3223 mL
- 1.6115 mL
- 3.2231 mL
- 10 mM
- 0.1612 mL
- 0.8058 mL
- 1.6115 mL

技术信息

CAS号

1433286-70-4

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H31Cl2N3O5

运输

蓝冰

分子量

620.52

别名

Compound 3i

溶解度

DMSO	100.0 mg/mL (161.2 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (4.8 mM)

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