Telatinib
Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
Product Specifications
CAS Number
332012-40-5
Product Name Alternative
Bay 57-9352
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
C-Kit; PDGFR; VEGFR
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Telatinib.html
Concentration
10mM
Purity
99.37
Solubility
DMSO : ≥ 46 mg/mL
Smiles
O=C(C1=NC=CC(COC2=NN=C(NC3=CC=C(Cl)C=C3)C4=C2OC=C4)=C1)NC
Molecular Formula
C20H16ClN5O3
Molecular Weight
409.83
Precautions
H302, H315, H319, H335
References & Citations
[1]Steeghs N, et al. Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res. 2008 Jun 1;14 (11) :3470-6.|[2]Langenberg MH, et al. Phase I evaluation of telatinib, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, in combination with irinotecan and capecitabine in patients with advanced solid tumors. Clin Cancer Res. 2010 Apr 1;16 (7) :2187-97.|[3]Steeghs N, et al. Pharmacogenetics of telatinib, a VEGFR-2 and VEGFR-3 tyrosine kinase inhibitor, used in patients with solid tumors. Invest New Drugs. 2011 Feb;29 (1) :137-43.|[4]Sodani K, et al. Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. Biochem Pharmacol. 2014 May 1;89 (1) :52-61.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
PDGFRα; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4
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