PTC-209

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PTC-209  纯度: 99.85%

PTC-209 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 不可逆转地损害结直肠癌起始细胞 (CICs)。PTC-209 显示有效的抗骨髓瘤活性并损害肿瘤微环境。

PTC-209

PTC-209 Chemical Structure

CAS No. : 315704-66-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1125 In-stock
5 mg ￥1023 In-stock
10 mg ￥1500 In-stock
50 mg ￥4900 In-stock
100 mg ￥8400 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 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].

上海金畔生物科技有限公司 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[1].

上海金畔生物科技有限公司 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

495.19

Formula

C17H13Br2N5OS
CAS 号

315704-66-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 32 mg/mL (64.62 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0194 mL 10.0971 mL 20.1943 mL
5 mM 0.4039 mL 2.0194 mL 4.0389 mL
10 mM 0.2019 mL 1.0097 mL 2.0194 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (5.05 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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]. Sulaiman S, et al. PTC-209 Anti-Cancer Effects Involved the Inhibition of STAT3 Phosphorylation. Front Pharmacol. 2019;10:1199. Published 2019 Oct 21.

    [3]. Chen D, et al. Targeting BMI1+ Cancer Stem Cells Overcomes Chemoresistance and Inhibits Metastases in Squamous Cell Carcinoma. Cell Stem Cell. 2017 May 4;20(5):621-634.e6.

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