ChemicalBook > CAS DataBase List > Telatinib
Telatinib
Telatinib
- CAS No.332012-40-5
- Chemical Name:Telatinib
- CBNumber:CB51179861
- Molecular Formula:C20H16ClN5O3
- Formula Weight:409.83
- MOL File:332012-40-5.mol
Telatinib Property
- 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
- FDA UNII 18P7197Q7J
Safety
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H302-H315-H319-H335
- Precautionary statements P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501
Telatinib Chemical Properties,Usage,Production
- 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 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.
-
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.
Telatinib Preparation Products And Raw materials
Raw materials
Preparation Products
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332012-40-5, TelatinibRelated Search:
- Inhibitors
- API
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- 合成有机化合物配体
- 原料药
- 医药原料
- 抑制剂
- 小分子抑制剂,天然产物
- 蛋白酪氨酸激酶
- BAY-2880376
- 替拉替尼,10 MM DMSO 溶液
- 4-(((4-((4-氯苯基)氨基)呋喃并[2,3-D]哒嗪-7-基)氧基)甲基)-N-甲基吡啶-2-甲酰胺
- TELATINIB,抑制剂
- BAY 57-9352|||替拉替尼
- 4-(((4-((4-氯苯基)氨基)呋喃并[2,3-D]哒嗪-7-基)氧基)甲基)-N-甲基吡啶酰胺
- 332012-40-5
- naproxen sodium + caffeine
- Telatinib, 10 mM in DMSO
- Telatinib USP/EP/BP
- CS-1854
- CS-361
- 4-[[4-(4-Chloroanilino)furo[2,3-d]pyridazin-7-yl]oxymethyl]-N-methyl-pyridine-2-carboxamide
- Telatnib
- 4-[[[4-[(4-Chlorophenyl)amino]furo[2,3-d]pyridazin-7-yl]oxy]methyl]-N-methyl-2-pyridinecarboxamide Telatinib(BAY57-9352)
- 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(BAY 57-9352)
- Unii-18p7197Q7j
- Bay 57-9352
- 2-Pyridinecarboxamide, 4-(((4-((4-chlorophenyl)amino)furo(2,3-D)pyridazin-7-yl)oxy)methyl)-N-methyl-