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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

Available Sizes

Curated Selection

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