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TD52 {[allProObj[0].p_purity_real_show]}

货号:A1338559 Ambeed 开学季,买赠积分,赢豪礼

TD52是 Erlotinib 的衍生物,通过调节 CIP2A/PP2A/p-Akt 信号通路,诱导三阴性乳腺癌 (TNBC) 细胞凋亡,具有潜在的抗癌作用。

TD52 化学结构 CAS号:1798328-24-1
TD52 化学结构
CAS号:1798328-24-1
TD52 3D分子结构
CAS号:1798328-24-1
TD52 化学结构 CAS号:1798328-24-1
TD52 3D分子结构 CAS号:1798328-24-1
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TD52 纯度/质量文件 产品仅供科研

货号:A1338559 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 Akt Akt1 Akt2 Akt3 其他靶点 纯度
Honokiol MEK {[allProObj[0].p_purity_real_show]}
PF-04691502 ++++

P-Akt (T308), IC50: 7.5 nM

P-Akt (S473), IC50: 3.8 nM

{[allProObj[0].p_purity_real_show]}
PHT-427 +

Akt, Ki: 2.7 μM

{[allProObj[0].p_purity_real_show]}
Deguelin PI3K {[allProObj[0].p_purity_real_show]}
TIC10 isomer ERK {[allProObj[0].p_purity_real_show]}
Perifosine +

Akt, IC50: 4.7 μM

{[allProObj[0].p_purity_real_show]}
Miltefosine PI3K,PKC {[allProObj[0].p_purity_real_show]}
Triciribine +

Akt, IC50: 130 nM

{[allProObj[0].p_purity_real_show]}
Uprosertib +

Akt1, IC50: 180 nM

+

Akt2, IC50: 328 nM

++

Akt3, IC50: 38 nM

{[allProObj[0].p_purity_real_show]}
Afuresertib ++++

Akt1, Ki: 0.08 nM

++++

Akt2, Ki: 2 nM

++++

Akt3, Ki: 2.6 nM

{[allProObj[0].p_purity_real_show]}
Miransertib ++++

Akt1, IC50: 5 nM

++++

Akt2, IC50: 4.5 nM

++

Akt3, IC50: 16 nM

{[allProObj[0].p_purity_real_show]}
GSK-690693 ++++

Akt1, IC50: 2 nM

+++

Akt2, IC50: 13 nM

+++

Akt3, IC50: 9 nM

{[allProObj[0].p_purity_real_show]}
AT7867 ++

Akt1, IC50: 32 nM

++

Akt2, IC50: 17 nM

++

Akt3, IC50: 47 nM

PKA {[allProObj[0].p_purity_real_show]}
AKT inhibitor VIII ++

Akt1, IC50: 58 nM

+

Akt2, IC50: 210 nM

+

Akt3, IC50: 2119 nM

{[allProObj[0].p_purity_real_show]}
MK-2206 2HCl +++

Akt1, IC50: 8 nM

+++

Akt2, IC50: 12 nM

+

Akt3, IC50: 65 nM

{[allProObj[0].p_purity_real_show]}
Ipatasertib ++++

Akt1, IC50: 5 nM

++

Akt2, IC50: 18 nM

+++

Akt3, IC50: 8 nM

{[allProObj[0].p_purity_real_show]}
AT13148 ++

Akt1, IC50: 38 nM

+

Akt2, IC50: 402 nM

++

Akt3, IC50: 50 nM

PKA {[allProObj[0].p_purity_real_show]}
Capivasertib ++++

Akt1, IC50: 3 nM

+++

Akt2, IC50: 8 nM

+++

Akt3, IC50: 8 nM

{[allProObj[0].p_purity_real_show]}
A-674563 HCl +++

Akt1, Ki: 11 nM

PKA {[allProObj[0].p_purity_real_show]}
CCT128930 +++

Akt2, IC50: 6 nM

PKA {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

TD52 生物活性

描述 TD52, a derivative of Erlotinib, is an orally active and potent inhibitor of protein phosphatase 2A (CIP2A). It induces apoptosis in triple-negative breast cancer (TNBC) cells by modulating the CIP2A/PP2A/p-Akt signaling pathway. TD52 indirectly decreases CIP2A levels by disrupting Elk1 binding to the CIP2A promoter. Despite exhibiting lower inhibition of p-EGFR, TD52 demonstrates significant anti-cancer activity [1]. TD52 functions as a click chemistry reagent, featuring an alkyne group enabling it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing azide groups.
体内研究

TD52 (10 mg/kg/day; oral gavage; for 52 days) markedly reduces both the size and weight of MDA-MB-468 xenograft tumors [1].

体外研究

TD52 (2-10 μM; 48 hours) exhibits anti-proliferative effects and induces varying apoptotic responses in these cell lines [1].

TD52 (5 μM; 48 hours) has negligible impact on p-EGFR or EGFR expression but reduces the expression of CIP2A [1].

TD52 (2.5, 5, 7.5 μM; 48 hours) induces apoptosis in a time-dependent manner, concomitant with the downregulation of CIP2A and p-Akt [1].

TD52 (5 μM; 24 hours) markedly enhances the phosphatase activity of PP2A in TNBC cells [1].

TD52 (5 μM; 48 hours) does not exert noticeable effects on other common RTKs, including IGFR, PDGFR, and VEGFR2 [1].

TD52 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.

TD52 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.87mL

2.77mL

1.39mL

27.75mL

5.55mL

2.77mL

TD52 技术信息

CAS号1798328-24-1
分子式C24H16N4
分子量 360.411
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(291.33 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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