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TD52
- Soluble in DMSO
- MF: C24H16N4
- MW: 360.41
Description
TD52 is an erlotinib-derived modulator of the CIP2A–PP2A–AKT pathway. By downregulating the oncoprotein CIP2A, it reactivates the PP2A tumor suppressor and reduces phosphorylated AKT, triggering apoptosis. In hepatocellular carcinoma (HCC) models (HA22T, Hep3B, PLC5, SK-Hep1), TD52 exhibits potent antiproliferative effects (IC50: 0.8–1.2 µM), outperforming erlotinib (Axon 1128). This mechanism—driving tumor inhibition via CIP2A knockdown, AKT dephosphorylation, and PP2A restoration—is effective both in vivo and in triple-negative breast cancer (TNBC) cells. Consequently, TD52 is a valuable tool for studying pharmacological PP2A restoration rather than direct enzyme inhibition.
Key Features
- Modulates the CIP2A–PP2A–AKT pathway
- IC50: 0.8–1.2 µM in hepatocellular carcinoma cell lines
- Downregulates CIP2A and phosphorylated AKT
- Reactivates PP2A tumor-suppressor activity
- Induces apoptosis and inhibits tumor growth in preclinical models
Applications
- CIP2A biology and PP2A reactivation
- AKT survival-signaling research
- Hepatocellular carcinoma models
- Triple-negative breast cancer studies
- Apoptosis and oncogenic phosphatase regulation
More Information
| Parent CAS No. | 1798328-24-1 |
|---|---|
| Chemical Name | N2,N3-Bis(3-ethynylphenyl)quinoxaline-2,3-diamine |
| SMILES | C1C=C2N=C(NC3C=CC=C(C#C)C=3)C(NC3C=C(C#C)C=CC=3)=NC2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C24H16N4/c1-3-17-9-7-11-19(15-17)25-23-24(26-20-12-8-10-18(4-2)16-20)28-22-14-6-5-13-21(22)27-23/h1-2,5-16H,(H,25,27)(H,26,28) |
| InChiKey | SCUPZFSEJFWQIS-UHFFFAOYSA-N |
| CID | 118656842 |
| Short Description | CIP2A inhibitor |
References
- HC Yu et al. Erlotinib derivative inhibits hepatocellular carcinoma by targeting CIP2A to reactivate protein phosphatase 2A. Cell Death Dis. 2014 Jul 31;5:e1359.
- CY 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.
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