|1-(3-((((2R,3S,4R,5R)-5-(4-氨基-5-溴-7H-吡咯并[2,3-d]嘧啶-7-基)-3,4-二羟基四氢呋喃-2-基)甲基)(异丙基)氨基)丙基)-3-(4-(叔丁基)苯基)脲|CsnPharm

CAS No.: 1561178-17-3

SGC0946 Catalog No. CSN17931

Synonyms: SGC0946

SGC0946 is a selective inhibitor of DOT1L methyltransferase with IC50 of 0.3 nM and can kill mixed lineage leukaemia cells.

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400-920-2911

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tech@csnpharm.cn

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述SGC0946 is a selective and optimized DOT1L inhibitor with IC50 value of 8.8nM and 2.65nM for inhibition of methylation of H3K79 in MCF10A cells and A431 cells, respectively. SGC0946 is a brominated analog of EPZ004777 with enhanced potency and increased cellular activity over EPZ004777 (IC50 values of 84nM and 264nM in MCF10A cells and A431 cells, respectively) likely due to its longer residence time on the protein. SGC0946 selectively killed human cord blood cells transformed with an MLL–AF9 fusion oncogene at concentration of both 1μM and 5μM, but not cord blood cells transformed with an unrelated oncogene, TLS-ERG. Associations of 5μM SAHA with 5μM SGC0946 were efficient to partially reverse TGF-β1 (10ng/ml) effects by decreasing expression of PD-L1, SEMA3C, and its receptor neuropilin-2 (NRP2) and by increasing epithelial markers such as E-cadherin.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human MCF10A cells	-	Function assay	-	Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level, IC50=0.0088 μM	25406853

动物研究
剂量
Mice: 4 mg/kg^[2] (i.p.), 10 mg/kg^[3] (i.p.)

给药途径
i.p.

动物研究
剂量	Mice: 4 mg/kg^[2] (i.p.), 10 mg/kg^[3] (i.p.)
给药途径	i.p.

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
- 1.6166 mL
- 8.0832 mL
- 16.1664 mL
- 5 mM
- 0.3233 mL
- 1.6166 mL
- 3.2333 mL
- 10 mM
- 0.1617 mL
- 0.8083 mL
- 1.6166 mL

技术信息

CAS号

1561178-17-3

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H40BrN7O4

运输

蓝冰

分子量

618.57

别名

SGC0946

溶解度

DMSO	135.0 mg/mL (218.2 mM)
Water	insoluble

动物实验配方

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