TD52
产品名称:TD52
产品描述:
产品描述 | TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. |
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 | In female NCr athymic nude mice, TD52 (10 mg/kg/day; oral gavage) significantly inhibited MDA-MB-468 xenograft tumour size and tumour weight and decreased the protein expressions of CIP2A and p-Akt in the three MDA-MB-468 xenograft tumours.[1]. |
分子量 | 360.41 |
分子式 | C24H16N4 |
CAS No. | 1798328-24-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 95 mg/mL (263.59 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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