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PTC-209

现货
Catalog No.
B3179
Bmi-1抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,800.00
现货
2mg
¥ 890.00
现货
5mg
¥ 1,000.00
现货
10mg
¥ 1,600.00
现货
50mg
¥ 4,700.00
现货

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Background

PTC-209 is a small-molecule inhibitor of BMI-1 with IC50 value of 0.5 µM [1].

PTC-209 is screened out by using gene expression modulation by small molecules (GEMS) technology. It can lower BMI-1 transcript levels. PTC-209 is demonstrated to inhibit not only the UTR-mediated expression but also endogenous BMI-1 expression in HCT116 cell line. For HEK293 and HT1080 cell lines, PTC-209 doesn’t show any inhibition of the growth, suggesting that PTC-209 has no cytotoxicity. And for tumor cells or stem cells, such as U937, HT1080 and human hematopoietic stem cells, PTC-209 can inhibit the proliferation of them. As BMI-1 plays its role through the PRC1 complex, PTC-209 reduces the ability of PRC1 selectively. It is also reported that PTC-209 suppresses the growth of colorectal tumor cells through irreversible growth inhibition of CICs [1].

References:
[1] Kreso A, van Galen P, Pedley NM, Lima-Fernandes E, Frelin C, Davis T, Cao L, Baiazitov R, Du W, Sydorenko N, Moon YC, Gibson L, Wang Y, Leung C, Iscove NN, Arrowsmith CH, Szentgyorgyi E, Gallinger S, Dick JE, O'Brien CA. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt495.19
Cas No.315704-66-6
FormulaC17H13Br2N5OS
Solubility≥24.75mg/mL in DMSO
Chemical NameN-(2,6-dibromo-4-methoxyphenyl)-4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-1,3-thiazol-2-amine
SDFDownload SDF
Canonical SMILESCC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验: [1]

细胞系

人结肠直肠HCT116和人纤维肉瘤HT1080肿瘤细胞

制备方法

溶解度有限,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

37℃

实验结果

在人结肠直肠HCT116和人纤维肉瘤HT1080肿瘤细胞中,PTC-209不仅以剂量依赖性方式抑制UTR介导的报道基因表达,而且抑制内源性BMI-1表达,IC50大约为0.5 μM。0.1和10 μM之间的PTC-209以剂量依赖性方式降低BMI-1蛋白水平,同时减少细胞生长。

动物实验: [1]

动物模型

原代人结肠癌异种移植物裸鼠

给药剂量

60 mg/kg,每天一次,皮下给药

实验结果

在移植样品01细胞的小鼠中,初始给药后9天,PTC-209治疗组的肿瘤体积显著减少,用PTC-209继续治疗动物额外一周不影响小鼠的整体健康,并且肿瘤的大小没有增加。同样地,对于给予样品03细胞的小鼠,在PTC-209治疗后9天,与对照肿瘤相比,药物处理的肿瘤体积显著减小。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

1. Kreso A, van Galen P, Pedley NM et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.

生物活性

描述 PTC-209是BMI-1的小分子抑制剂,IC50值为0.5 ?M。
靶点 BMI-1          
IC50 0.5 ?M          

质量控制