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| | 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 | | EINECS: | | | 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 (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. | | 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. | | 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. |
| | Telatinib Preparation Products And Raw materials |
| Raw materials | Furo[2,3-d]pyridazin-7-amine, 4-chloro-N-(4-chlorophenyl)--->Furo[2,3-d]pyridazine, 4,7-dichloro-->4-(hydroxymethyl)-N-methylpicolinamide-->FURAN-2,3-DICARBOXYLIC ACID-->(2-METHYLAMINOCARBONYL-4-PYRIDYL)METHANOL-->2-METHYLCARBAMOYLISONICOTINIC ACID ETHYL ESTER-->Furo[2,3-d]pyridazin-4-amine, 7-chloro-N-(4-chlorophenyl)-
-->5,6-dihydrofuro[3,2-d]pyridazine-4,7-dione-->2,3-furandicarboxylic acid dimethyl ester-->3-Furoic acid-->N-Methylformamide-->Ethyl isonicotinate |
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