Tozasertib CAS 639089-54-6 Cyclopropane carboxylic acid VX-680 Tozasertib Free Base

Payment Terms: T/T,L/C,WU
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Basic Info.
  • Brand: MOSINTER 
  • Molecular Formula: C23H28N8OS 
  • Molecular Weight: 464.59 
  • Content: ≥99% 
  • Specification: CP/USP/EP 
  • Appearance: White to off-white solid powder 
  • Structure: 1 H-NMR and MS spectrum of the sample correspond to the data reported in the literature 
  • Solubility: DMSO 90 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL 
  • Shipping condition: Ambient temperature 
  • Self life: At least 5 years if properly stored. 
  • Model No.: C23H28N8OS 
  • Place of Origin: Sichuan  
  • Min.Order: 1 Gram
  • Means of Transport: Ocean, Air, Land
Supply Capacity
  • Production Capacity: 50KG/YEAR
  • Packing:as per request of clients
  • Delivery Date: within 7 days

Tozasertib ( CAS: 639089-54-6)

 

Item

Index

Molecular Formula

C23H28N8OS

Molecular Weight

464.59

Specification

CP/USP/EP

Content

≥99%

Tozasertib, also known as VX-680, MK0457 or VE465,  is a synthetic, small-molecule Aurora kinase inhibitor with potential antitumor activity. Tozasertib binds to and inhibits Aurora kinases (AKs), thereby inducing apoptosis in tumor cells in which AKs are overexpressed. AKs, a family of serine-threonine kinases, are essential for mitotic progression, spindle formation, centrosome maturation, chromosomal segregation, and cytokinesis.


Details

Although its multi-kinase profile, VX-680 induces similar cytotoxicity with IC50 of approximately 300 nM and exhibits an AUR B-like inhibitory phenotype of G2/M arrest, endoreduplication and apoptosis in BaF3 cells transfected with ABL or FLT-3 (mutant and wild type) kinases. VX-680 prevents the CAL-62 proliferation in a time-dependent manner. VX-680 treatment for 14 days significantly decreases the number and size of colonies by approximately 70% in the 8305C and 90% in the CAL-62, 8505C and BHT-101. Treatment of the different ATC cells with VX-680 inhibits proliferation with the IC50 between 25 and 150 ?nM. The VX-680 significantly impairs the ability of the different cell lines to form colonies in soft agar. Analysis of caspase-3 activity indicates that VX-680 induces apoptosis in the different cell lines. CAL-62 cells exposed for 12? hours to VX-680 showed an accumulation of cells with ≥4N DNA content. Time-lapse analysis demonstrates that VX-680-treated CAL-62 cells exit metaphase without dividing. Moreover, histone H3 phosphorylation is abrogated following VX-680 treatment.VX-680 has significant inhibitory activity against BCR-Abl bearing the T315I mutation in patient-derived samples.


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MOSINTER GROUP LIMITED
Guangbo Center Office 2001, YinXianDaDao 1357, Ningbo, Zhejiang, China (Mainland) / 315100
Fax: +86-574-89212215
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