TD52
TD52 Basic information
- Product Name:
- TD52
- Synonyms:
-
- TD52
- 2,3-Quinoxalinediamine, N2,N3-bis(3-ethynylphenyl)-
- TD52 >=98% (HPLC)
- breast,triple-negative,TD52,inhibit,HCC-1937,orally,Erlotinib,TD 52,CIP2A,Protein kinase B,p-Akt,p-EGFR,Apoptosis,PKB,Elk1,PP2A,Inhibitor,TD-52,cancer,Phosphatase,TNBC,Akt
- N2,N3-Bis(3-ethynylphenyl)quinoxaline-2,3-diamine
- TD52【SML2145】
- CAS:
- 1798328-24-1
- MF:
- C24H16N4
- MW:
- 360.41
- Mol File:
- 1798328-24-1.mol
TD52 Chemical Properties
- Boiling point:
- 530.0±50.0 °C(Predicted)
- Density
- 1.29±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 5 mg/ml; DMSO: 5 mg/ml
- form
- A solid
- pka
- 2.45±0.59(Predicted)
- color
- White to yellow
TD52 Usage And Synthesis
Uses
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]. TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Biological Activity
TD52, an erlotinib analog, is a putative inhibitor of CIP2A th at exhibits potent antitumor efficacy on HCC and TNBC cells. TD52 induces apoptosis through downregulation of CIP2A (Cancerous inhibitor of protein phosphatase 2A) in HCC, NSCLC and TNBC cells. Apparently TD52 indirectly downregulates CIP2A transcripts through interrupting the binding of Elk1 to CIP2A promoter. TD52 is a weak inhibitor of EGFR tyrosine kinase.
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
[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. DOI:10.1016/j.ejca.2016.11.012
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