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TD52 dihydrochloride

TD52 dihydrochloride

产品编号 T35528L
别名: TD52 dihydrochloride(1798328-24-1 Free base), TD52 2HCl

TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti-cancer activity while displaying less inhibition of p-EGFR.

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TD52 dihydrochloride Chemical Structure
TD52 dihydrochloride, CAS N/A
规格 价格/CNY 货期 数量
1 mg ¥ 298 现货
5 mg ¥ 690 现货
10 mg ¥ 1,330 现货
25 mg ¥ 2,890 现货
50 mg ¥ 4,360 现货
100 mg ¥ 6,190 现货
1 mL * 10 mM (in DMSO) ¥ 788 现货
其他形式的 TD52 dihydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: TD52 dihydrochloride (T35528L)
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参考文献
产品描述 TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti-cancer activity while displaying less inhibition of p-EGFR.
体外活性 TD52 dihydrochloride (2-10 μM; 48 hours) shows anti-proliferative ability and induces differential apoptotic effects in these cell lines. TD52 dihydrochloride (5 μM; 48 hours) has minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression. TD52 dihydrochloride (2.5, 5, 7.5 μM; 48 hours) time-dependently induces apoptosis accompanied with downregulating CIP2A and p-Akt. TD52 dihydrochloride (5 μM; 24 hours) significantly increases the phosphatase activity of PP2A in TNBC cells. TD52 dihydrochloride (5 μM; 48 hours) has no obvious effects on other common RTKs, such as IGFR, PDGFR and VEGFR2[1].
体内活性 TD52 dihydrochloride (10 mg/kg/day; oral gavage; for 52 days) significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight[1].
别名 TD52 dihydrochloride(1798328-24-1 Free base), TD52 2HCl
分子量 433.33
分子式 C24H18Cl2N4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 22.5 mg/mL (51.9 mM), Sonification and heating to 60℃ are recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3077 mL 11.5386 mL 23.0771 mL 57.6928 mL
5 mM 0.4615 mL 2.3077 mL 4.6154 mL 11.5386 mL
10 mM 0.2308 mL 1.1539 mL 2.3077 mL 5.7693 mL
20 mM 0.1154 mL 0.5769 mL 1.1539 mL 2.8846 mL
50 mM 0.0462 mL 0.2308 mL 0.4615 mL 1.1539 mL

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TargetMol Library Books参考文献

1. Chun-Yu Liu, et al. EGFR-independent Elk1/CIP2A signalling mediates apoptotic effect of an erlotinib derivative TD52 in triple-negative breast cancer cells. Eur J Cancer. 2017 Feb;72:112-123.

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗癌活性化合物库 已知活性化合物库 抗癌化合物库 经典已知活性库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

TD52 dihydrochloride Others TD52 dihydrochloride(1798328-24-1 Free base) TD 52 Dihydrochloride TD52 TD-52 TD52 Dihydrochloride TD52 2HCl TD 52 TD-52 Dihydrochloride Inhibitor inhibitor inhibit

 

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