1798328-24-1
1798328-24-1 structure
- Name: TD52
- Chemical Name: TD52
- CAS Number: 1798328-24-1
- Molecular Formula: C24H16N4
- Molecular Weight: 360.41
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2021-09-05 21:20:51
- Modify Date: 2024-01-12 12:58:39
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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[1].
| Name | TD52 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
Akt |
| In Vitro | TD52 (2-10 μM; 48 hours) shows anti-proliferative ability and induces differential apoptotic effects in these cell lines[1]. TD52 (5 μM; 48 hours) has minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression[1]. TD52 (2.5, 5, 7.5 μM; 48 hours) time-dependently induces apoptosis accompanied with downregulating CIP2A and p-Akt[1]. TD52 (5 μM; 24 hours) significantly increases the phosphatase activity of PP2A in TNBC cells[1]. TD52 (5 μM; 48 hours) has no obvious effects on other common RTKs, such as IGFR, PDGFR and VEGFR2[1]. Apoptosis Analysis[1] Cell Line: Three TNBC cell lines including HCC-1937, MDA-MB-231 and MDA-MB-468 cells Concentration: 2, 4, 6, 8, 10 μM Incubation Time: 48 hours Result: Showed anti-proliferative ability and induced differential apoptotic effects in these cell lines. Western Blot Analysis[1] Cell Line: MDA-MB-231 cell Concentration: 5 μM Incubation Time: 48 hours Result: Had minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression. |
| In Vivo | TD52 (10 mg/kg/day; oral gavage; for 52 days) significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight[1]. Animal Model: Female NCr athymic nude mice (5-7 weeks of age)[1] Dosage: 10 mg/kg Administration: Oral gavage; daily; for 52 days Result: Significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight. Decreased the protein expressions of CIP2A and p-Akt in the three MDA-MB-468 xenograft tumours. |
| References |
| Molecular Formula | C24H16N4 |
|---|---|
| Molecular Weight | 360.41 |
| Storage condition | -20°C |