货号	规格	价格	上海	北京	珠海	重庆	武汉
S85057-5mg买3赠1	99.26%	￥408.00 S85057-5mg ￥408.00 现货（买3赠1）	4 4	-	-	-	-
S85057-10mg买3赠1	99.26%	￥520.00 S85057-10mg ￥520.00 现货（买3赠1）	5 1 5	1	-	-	-
S85057-25mg	99.26%	￥670.00 S85057-25mg ￥670.00 现货	4 4	-	-	-	-
S85057-100mg	99.26%	￥940.00 S85057-100mg ￥940.00 现货	1 1	-	-	-	-

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产品描述：

HLM006474 是一种小分子的泛 E2F 抑制剂，在A375细胞中可抑制 DNA 与 E2F4 的结合，其IC50值为29.8 µM。HLM006474 可诱导细胞增殖的减少及细胞凋亡的增加。CDK/Rb/E2F通路在肺癌中通常被破坏，因而 HLM006474 可在肺癌治疗中发挥作用

靶点：

E2F4(Cell-free assay):29.8 μM

体外研究：

Treatment of multiple cell lines with HLM006474 results in the loss of intracellular E2F4 DNA-binding activity within hours. Overnight exposure to HLM006474 results in down regulation of total E2F4 protein as well as known E2F targets. The effects of HLM006474 treatment on different cell lines varies, but includes a reduction in cell proliferation and an increase in apoptosis.HLM006474 reduces the viability of both SCLC and NSCLC lines with a biological IC50 that varies between 15 and 75 mM, but with no significant difference between the groups.

体内研究：

HLM006474 inhibits E2F4 DNA-binding and activity in vivo. In vivo HLM006474 leads to significant downregulation of E2F4 protein.Short exposure of Chx10Cre;Rbf/f;p107−/− embryos to HLM006474 has a dramatic effect on tumorigenesis. Thus, modest and temporary pharmaceutical E2f inhibition blocks retinoblastoma initiation

细胞实验：

Cell lines: 3T3 MEFS, A375, MDA-MB-231, MCF7, T47D, HFFs, MDA-MB-468, SK-BR3, 8226-s, 8226-dox40, 8226-MR20 Concentrations: 0-100 μM Incubation Time: 0-24 h Method: Human A375 melanocytes are treated for 9-hrs with the indicated concentration of HLM006474. A375 cells are treated with 40 μM HLM006474 and EMSA and Western analyses performs at the indicated time intervals.

动物实验：

Animal Models: Chx10Cre mice, Rbf/f mice, p107−/− mice Dosages: 100 mg/kg Administration: IP

参考文献：

1. Ma Y, et al. A small-molecule E2F inhibitor blocks growth in a melanoma culture model. Cancer Res. 2008 Aug 1;68(15):6292-9. 2. Kurtyka CA, et al. E2F inhibition synergizes with paclitaxel in lung cancer cell lines. PLoS One. 2014 May 15;9(5):e96357. 3. M Sangwan, et al. Established and new mouse models reveal E2f1 and Cdk2 dependency of retinoblastoma, and expose effective strategies to block tumor initiation. Oncogene. 2012 Nov 29;31(48):5019-28.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.503 ml	12.516 ml	25.032 ml
5 mM	0.501 ml	2.503 ml	5.006 ml
10 mM	0.25 ml	1.252 ml	2.503 ml
50 mM	0.05 ml	0.25 ml	0.501 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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