TD52 是 Erlotinib (HY-50896) 衍生物，一种具有口服活性的强效癌性蛋白磷酸酶 2A (CIP2A) 抑制剂。TD52 通过调节 CIP2A/PP2A/p-Akt 信号通路介导三阴性乳腺癌 (TNBC) 细胞的凋亡作用。TD52 通过干扰 Elk1 与 CIP2A 启动子的结合间接减少 CIP2A。TD52 具有小的 p-EGFR 抑制作用并具有抗癌活性。

TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity.

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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.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

TD52 (10 mg/kg/day; oral gavage; for 52 days) significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight.
has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 100 mg/mL (277.46 mM; Need ultrasonic)配制储备液