化合物TD52 T35528

Product Introduction
Bioactivity


英文名: TD52

描述: TD52 是 PP2A (CIP2A) 癌性抑制剂的口服活性抑制剂。 TD52 是厄洛替尼衍生物，通过干扰 Elk1 与 CIP2A 启动子的结合间接降低了 CIP2A。

体外活性: TD52 (5 μM; 24 hours) significantly increases the phosphatase activity of PP2A in TNBC cells. TD52 (5 μM; 48 hours) has no obvious effects on other common RTKs, such as IGFR, PDGFR and VEGFR2. TD52 (2-10 μM; 48 hours) shows anti-proliferative ability and induces differential apoptotic effects in these cell lines. TD52 (5 μM; 48 hours) has minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression. TD52 (2.5, 5, 7.5 μM; 48 hours) time-dependently induces apoptosis accompanied with downregulating CIP2A and p-Akt[1].

体内活性: 在雌性NCr裸鼠中，TD52（每天10 mg/kg；口腔灌注）显著抑制了MDA-MB-468异种移植瘤的大小和重量，并降低了三个MDA-MB-468异种移植肿瘤中CIP2A和p-Akt的蛋白表达。[1]。

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

溶解度: DMSO : 95 mg/mL (263.59 mM)


关键字: breast | triple-negative | inhibit | HCC-1937 | orally | Erlotinib | CIP2A | Protein kinase B | p-Akt | p-EGFR | Apoptosis | TD52 | TD 52 | PKB | Elk1 | PP2A | TD-52 | Inhibitor | cancer | Phosphatase | TNBC | Akt

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途