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

Model: C23H28N8OS
Place of Origin: Sichuan,China (Mainland)
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.

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Product Description

Payment & Shipping Terms Supply Capacity
Payment Terms:L/C, T/T, WUProduction Capacity:50KG/YEAR
Min. Order:1 GramPacking:as per request of...
Means of Transport:Ocean, Air, LandDelivery 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.

Category: Antineoplastic Drugs API

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