| Identification | Back Directory | [Name]
Telatinib | [CAS]
332012-40-5 | [Synonyms]
CS-361
CS-1854
Telatnib
Bay 57-9352
Unii-18p7197Q7j
Telatinib USP/EP/BP
Telatinib(BAY 57-9352)
4-((4-(4-chlorophenylamino)furo[2,3-d]pyridazin-7-yloxy)methyl)-N-methylpicolinamide
4-[[4-(4-Chloroanilino)furo[2,3-d]pyridazin-7-yl]oxymethyl]-N-methyl-pyridine-2-carboxamide
4-[[[4-[(4-Chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl]oxy]methyl]-N-methyl-2-pyridinecarboxamide
2-Pyridinecarboxamide, 4-(((4-((4-chlorophenyl)amino)furo(2,3-D)pyridazin-7-yl)oxy)methyl)-N-methyl-
4-[[[4-[(4-Chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl]oxy]methyl]-N-methyl-2-pyridinecarboxamide Telatinib(BAY57-9352) | [Molecular Formula]
C20H16ClN5O3 | [MDL Number]
MFCD18251453 | [MOL File]
332012-40-5.mol | [Molecular Weight]
409.83 |
| Chemical Properties | Back Directory | [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) | [color ]
White to light yellow | [InChI]
InChI=1S/C20H16ClN5O3/c1-22-19(27)16-10-12(6-8-23-16)11-29-20-17-15(7-9-28-17)18(25-26-20)24-14-4-2-13(21)3-5-14/h2-10H,11H2,1H3,(H,22,27)(H,24,25) | [InChIKey]
QFCXANHHBCGMAS-UHFFFAOYSA-N | [SMILES]
C1(C(NC)=O)=NC=CC(COC2=NN=C(NC3=CC=C(Cl)C=C3)C3C=COC2=3)=C1 |
| Hazard Information | Back Directory | [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).1 It also binds to the transmembrane region of the ABCG2 efflux transporter and enhances intracellular accumulation of [3H]-mitoxantrone in ABCG2-overexpressing cells.2 Telatinib (15 mg/kg) decreases tumor growth rate and size in an H460/MX20 mouse xenograft model. | [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.
| [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. | [in vivo]
Telatinib causes a significant decrease in endothelium-dependent and endothelium-independent vasodilation. VEGF inhibition by itself decreases NO synthesis, which promotes vasoconstriction, increases peripheral resistance, and therefore can induce an increase in blood pressure[1]. Telatinib (15 mg/kg) with doxorubicin (1.8 mg/kg) significantly decreases the growth rate and tumor size of ABCG2 overexpressing tumors in a xenograft nude mouse model[4]. | [target]
c-Kit | [IC 50]
VEGFR2: 6 nM (IC50); VEGFR3: 4 nM (IC50); PDGFRα: 15 nM (IC50); c-Kit: 1 nM (IC50) | [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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