| Identification | Back Directory | [Name]
TD52 | [CAS]
1798328-24-1 | [Synonyms]
TD52
TD52 >=98% (HPLC)
2,3-Quinoxalinediamine, N2,N3-bis(3-ethynylphenyl)-
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 | [Molecular Formula]
C24H16N4 | [MDL Number]
MFCD31697737 | [MOL File]
1798328-24-1.mol | [Molecular Weight]
360.41 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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]
TD52an erlotinib analogis 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 HCCNSCLC 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.
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| [storage]
Store at -20°C | [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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| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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