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Altiratinib

Catalog No.
B5832
c-MET/TIE-2/VEGFR inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$120.00
In stock
10mg
$150.00
In stock
25mg
$250.00
In stock
50mg
$450.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Altiratinib (DCC-2701) is a potent inhibitor of c-MET/TIE-2/VEGFR with IC50 values of 2.7, 8.0 and 9.2 nM, respectively [1].

Hepatocyte growth factor receptor (c-MET) is a tyrosine kinase receptor for hepatocyte growth factor and is essential for wound healing and embryonic development. TEK tyrosine kinase (TIE-2) is a receptor for angiopoietin-1 (ANG-1) and is important for endothelial cell-smooth muscle cell communication. VEGFR is a tyrosine kinase receptor for vascular endothelial growth factor that involved in both vasculogenesis and angiogenesis.

Altiratinib (DCC-2701) is a potent c-MET/TIE-2/VEGFR inhibitor. Altiratinib potently inhibited MET kinase and activating oncogenic MET mutations and also inhibited TRKA, TRKB and TRKC kinases with IC50 values of 0.85, 4.6, and 0.83 nM, respectively. In EBC-1 NSCLC and MKN-45 gastric cancer cell lines overexpressing MET, altiratinib inhibited MET phosphorylation with IC50 values of 0.85 and 2.2 nM, respectively. In VEGF-stimulated HUVECs, altiratinib inhibited VEGFR2 phosphorylation with IC50 value of 4.7 nM. In HUVECs and EA.hy926 cells, altiratinib inhibited TIE2 phosphorylation stimulated by ANG-1 with IC50 values of 1.0 and 2.6 nM, respectively [1].

In the MET-amplified MKN-45 xenograft model, altiratinib (30 mg/kg) inhibited MET phosphorylation by >95% for the 24-hour period [1]. In nude mouse xenografted SKOV3 cells, DCC-2701 (10 or 20 mg/kg for 28 days) significantly reduced tumor burden by 53% and 52%, respectively [2].

References:
[1].  Smith BD, Kaufman MD, Leary CB, et al. Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2. Mol Cancer Ther, 2015.
[2].  Kwon Y, Smith BD, Zhou Y, et al. Effective inhibition of c-MET-mediated signaling, growth and migration of ovarian cancer cells is influenced by the ovarian tissue microenvironment. Oncogene, 2015, 34(2): 144-153.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt510.46
Cas No.1345847-93-9
FormulaC26H21F3N4O4
Solubility≥21.55mg/mL in DMSO
Chemical NameN-(4-((2-(cyclopropanecarboxamido)pyridin-4-yl)oxy)-2,5-difluorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
SDFDownload SDF
Canonical SMILESFC1=CC=C(NC(C2(C(NC3=C(F)C=C(OC4=CC(NC(C5CC5)=O)=NC=C4)C(F)=C3)=O)CC2)=O)C=C1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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