Telatinib
Telatinib Basic information
- Product Name:
- Telatinib
- Synonyms:
-
- 2-Pyridinecarboxamide, 4-(((4-((4-chlorophenyl)amino)furo(2,3-D)pyridazin-7-yl)oxy)methyl)-N-methyl-
- Bay 57-9352
- Unii-18p7197Q7j
- Telatinib(BAY 57-9352)
- 4-[[[4-[(4-Chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl]oxy]methyl]-N-methyl-2-pyridinecarboxamide
- 4-((4-(4-chlorophenylamino)furo[2,3-d]pyridazin-7-yloxy)methyl)-N-methylpicolinamide
- 4-[[[4-[(4-Chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl]oxy]methyl]-N-methyl-2-pyridinecarboxamide Telatinib(BAY57-9352)
- Telatnib
- CAS:
- 332012-40-5
- MF:
- C20H16ClN5O3
- MW:
- 409.83
- Product Categories:
-
- API
- Inhibitors
- Mol File:
- 332012-40-5.mol
Telatinib Chemical Properties
- Boiling point:
- 713.6±60.0 °C(Predicted)
- Density
- 1.417
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; insoluble in EtOH; ≥20.5 mg/mL in DMSO
- form
- solid
- pka
- 14.18±0.46(Predicted)
Telatinib Usage And Synthesis
Description
Telatinib is a multi-kinase inhibitor that inhibits VEGF receptor 2 (VEGFR2), VEGFR3, PDGFRα, and c-Kit (IC50s = 6, 4, 15, and 1 nM, respectively). It also binds to the transmembrane region of the ABCG2 efflux transporter and enhances intracellular accumulation of [3H]-mitoxantrone in ABCG2-overexpressing cells. Telatinib (15 mg/kg) decreases tumor growth rate and size in an H460/MX20 mouse xenograft model.
Uses
Telatinib small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β tyrosine kinases. Telatinib is used therapeuticall y in patients with advanced solid tumors.
Uses
Telatinib small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β tyrosine kinases. Telatinib is used therapeutically in patients with advanced solid tumors.
Uses
Telatinib (BAY 57-9352) is an orally available, potent multitargeted VEGFR-2, VEGFR-3, PDGFR-β and c-Kit tyrosine kinases inhibitor with an IC50 of 19 nM for the inhibition of VEGFR-2 autophosphorylation.
target
c-Kit
References
[1]. steeghs, n., et al., hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. clin cancer res, 2008. 14(11): p. 3470-6.
[2]. strumberg, d., et al., phase i dose escalation study of telatinib (bay 57-9352) in patients with advanced solid tumours. br j cancer, 2008. 99(10): p. 1579-85.
[3]. sodani, k., et al., telatinib reverses chemotherapeutic multidrug resistance mediated by abcg2 efflux transporter in vitro and in vivo. biochem pharmacol, 2014. 89(1): p. 52-61.
[4]. eskens, f.a., et al., phase i dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-kit, in patients with advanced or metastatic solid tumors. j clin oncol, 2009. 27(25): p. 4169-76.
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