InChI key
SCUPZFSEJFWQIS-UHFFFAOYSA-N
SMILES string
C#CC1=CC=CC(NC2=NC3=CC=CC=C3N=C2NC4=CC=CC(C#C)=C4)=C1
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
TD52, an erlotinib analog, is a putative inhibitor of CIP2A that 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.
putative inhibitor of CIP2A that exhibits potent antitumor efficacy on HCC and TNBC cells.
存储类别
11 - Combustible Solids
wgk
WGK 3
Chun-Yu Liu et al.
European journal of cancer (Oxford, England : 1990), 72, 112-123 (2016-12-28)
Cancerous inhibitor of protein phosphatase 2A (CIP2A) has emerged as a therapeutic determinant mediating the anti-cancer effects of several new agents. We investigated the efficacy and mechanism of TD52, an erlotinib derivative with minimal p-EGFR inhibition but significant CIP2A downregulation
H-C Yu et al.
Cell death & disease, 5, e1359-e1359 (2014-08-01)
Protein phosphatase 2A (PP2A) is a tumor suppressor, which is functionally defective in various cancers. Previously, we found that PP2A activity determined the anticancer effect of bortezomib and erlotinib in hepatocellular carcinoma (HCC) cells. Here, we tested a novel erlotinib
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