PTC-209 hydrobromide

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PTC-209 hydrobromide 

PTC-209 hydrobromide 是一种特定的 BMI-1 抑制剂，在 HEK293T 细胞系中的 IC50 为 0.5 μM。PTC-209 hydrobromide 不可逆转地损害结直肠癌起始细胞 (CICs)。PTC-209 hydrobromide 显示有效的抗骨髓瘤活性并损害肿瘤微环境。

PTC-209 hydrobromide

PTC-209 hydrobromide Chemical Structure

CAS No. : 1217022-63-3

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PTC-209 hydrobromide 的其他形式现货产品:

PTC-209

生物活性

PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment[1][2].

IC50 & Target

IC50: 0.5 μM (BMI-1, in HT1080 tumor cells)[1]
体外研究
(In Vitro)

PTC-209 (0.01-10 µM; 24-72 hours) induces a concentration- and time-dependent decrease in the cellular viability of all cell lines tested[2].
PTC-209 (1-2.5 μM) inhibits STAT3 phosphorylation in A549 lung cancer cells and MDA-MB-231 breast cancer cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Lung (LNM35, A549 cells), breast (MDA-MB-231 and T47D cells), and colon (HT-29, HCT-116, and HCT8/S11 cells)
Concentration: 0.01-10 µM
Incubation Time: 24, 48, and 72 hour
Result: Induced a concentration- and time-dependent decrease in the cellular viability of all cell lines tested.

体内研究
(In Vivo)

PTC-209 (60 mg/kg body weight; subcutaneously; once a day for 11 days) significantly reduces tumor volume[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (male, aged 8-10 weeks, HCT1116 cell-derived tumor)[1]
Dosage: 60 mg/kg body weight
Administration: Subcutaneously; once a day for 11 days
Result: Significantly reduced tumor volume.

分子量

576.10

Formula

C17H14Br3N5OS
CAS 号

1217022-63-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Kreso A, et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.

    [2]. Christian Mayr, et al. The BMI1 inhibitor PTC-209 is a potential compound to halt cellular growth in biliary tract cancer cells. Oncotarget. 2016 Jan 5; 7(1): 745-758.

    [3]. Shahi MH, et al. BMI1 is expressed in canine osteosarcoma and contributes to cell growth and chemotherapy resistance. PLoS One. 2015 Jun 25;10(6):e0131006.

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