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| CAS号: | 1423715-09-6 |
| 英文名称: | SP2509 |
| 英文同义词: | SP2509;HCI-2509;(E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide;(E)-N'-(1-(5-chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide SP2509 |
| 中文名称: | N/A |
| 中文同义词: | |
| CBNumber: | CB22734796 |
| 分子式: | C19H20ClN3O5S |
| 分子量: | 0 |
| MOL File: | Mol file |
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N/A 性质、用途与生产工艺 |
生物活性
SP2509是一种选择性histone demethylase LSD1抑制剂，IC50为 13 nM，对MAO-A，MAO-B，乳酸脱氢酶和葡萄糖氧化酶没有活性。
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体外研究
In AML cells, SP2509 inhibits the association of LSD1 with CoREST, increases promoter-specific H3K4Me3 and induces p53, p21 and C/EBPα. SP2509 also significantly inhibits the colony growth and induces apoptosis of OCI-AML3. In addition, SP2509 induces differentiation of cultured and primary AML cells, and exerts synergistic lethal activity when used in combination with panobinostat.
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体内研究
In mice bearing OCI-AML3 xenografts, SP2509 (25 mg/kg i.p.) significantly improved the survival of the mice, while co-treatment with SP2509 and panobinostat exerts superior in vivo activity.
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| N/A 生产厂家 全球有 14家供应商
N/A国内生产厂家
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