| Name | TD52 |
| Description | 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. |
| In vitro | 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]. |
| In vivo | 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 95 mg/mL (263.59 mM), Sonication is recommended.
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| Keywords | triple-negative | TNBC | TD-52 | TD52 | TD 52 | Protein kinase B | PP2A | PKB | Phosphatase | p-EGFR | p-Akt | orally | Inhibitor | inhibit | HCC-1937 | Erlotinib | Elk1 | CIP2A | cancer | breast | Apoptosis | Akt |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Ethyl linoleate | Formamide | Dimethyl phthalate | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Glycolysis Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Hematonosis Compound Library | Anti-Prostate Cancer Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | Neuronal Differentiation Compound Library |
United States
