Cat. No. Name Size Price Add Cart
KI1113Telatinib5 mg$272
Telatinib10 mg$512
Telatinib50 mg$1552
Telatinib200 mg$3952

Chemical Characteristic

Product NameTelatinib
SynonymsBAY 57-9352
CAS No.332012-40-5
Molecular Weight 409.83
FormulaC20H16ClN5O3
Chemical Name4-((4-(4-chlorophenylamino)furo[2,3-d]pyridazin-7-yloxy)methyl)-N-methylpicolinamide
Smilesc1(cc(ccn1)COc1c2c(c(nn1)Nc1ccc(cc1)Cl)cco2)C(=O)NC
Chemical Structure

Biological activities

Telatinib is an orally available, small-molecule multitargeted vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β tyrosine kinases inhibitor. The IC50 of telatinib is 6 and 4 nM against VEGFR-2 and VEGFR-3, respectively. Telatinib inhibits the growth factors recetpors platelet-derived growth factor receptor-? and c-Kit with IC50 of 15 and 1 nM, respectively.[1] Telatinib is metabolized by various cytochrome P450 (CYP) isoforms including CYP3A4/3A5, CYP2C8, CYP2C9, and CYP2C19 as well as by uridine diphosphate glucuronosyltransferase 1A4 (UGT1A4).[2] In vitro, telatinib also functions as a Ca2+ mitochondrial regulator. Telatinib binds selectively to the Hsp90 chaperone protein and inhibit its function. Telatinib reduces mitochondrial membrane potential. The Ki of 3H-telatinib is 0.274 µM against the N-terminal domain of HSP90. [3]

Protocols

In vitro Telatinib is dissolved in DMSO at 10 mM, and kept at -80 °C until use.[3]

References

[1] Steeghs N, et al. Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res. 2008, 14(11): 3470-3476.
[2] 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, 29(1): 137-143.
[3] Xie Q et al. Benzoquinone ansamycin 17AAG binds to mitochondrial voltage-dependent anion channel and inhibits cell invasion. Proc Natl Acad Sci U S A. 2011, 108(10): 4105-4110.

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