ChemicalBook > CAS DataBase List > TD52

TD52

Product Name: TD52
CAS No.: 1798328-24-1
Chemical Name: TD52
Synonyms: TD52;TD52【SML2145】;TD52 >=98% (HPLC);N2,N3-Bis(3-ethynylphenyl)quinoxaline-2,3-diamine;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
CBNumber: CB23364118
Molecular Formula: C24H16N4
Formula Weight: 360.41
MOL File: 1798328-24-1.mol

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TD52 Property

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

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Hazard and Precautionary Statements (GHS)

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TD52 Chemical Properties,Usage,Production

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

TD52 Preparation Products And Raw materials

Raw materials

Preparation Products

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TD52 Suppliers

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1798328-24-1, TD52Related Search:

ZM 39923 HCl RGB-286638 (free base) GSK2141795 SR9009 Fexaramine BAM15 (3aR,6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxamide TG4-155 PH 797804 NVP-TAE684

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】

1798328-24-1