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Telatinib

Telatinib Structure
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
Hazard and Precautionary Statements (GHS)
  • 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
Global(129)Suppliers
  • Supplier:
    Capot Chemical Co.,Ltd.
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    Alchem Pharmtech,Inc.
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    TargetMol Chemicals Inc.
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    Career Henan Chemica Co
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Telatinib Spectrum
332012-40-5, TelatinibRelated Search:
  • Inhibitors
  • API
  • 药靶配体
  • 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-