Telatinib (BAY 57-9352)

Telatinib (BAY 57-9352)

参考价：¥1298
供货周期： 一周
品牌：
规格： 2mg
货号： K1303
CAS号： 332012-40-5
上海高创化学科技有限公司
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SKU:K1303   M. Wt:409.83  
Formula:C20H16ClN5O3   Solubility:No  
Purity:>99%   Storage:2 years at -20 degrees centigrade  
CAS No.:332012-40-5   Synonyms:N/A  
Chemical NameN/A
Biological Activity
Description Telatinib (BAY 57-9352)
Targets VEGFR2 VEGFR3 c-Kit PDGFR-beta  
IC50 6 nM 4 nM 1 nM 15 nM  
In vitro Telatinib (BAY 57-9352), a small molecule angiogenesis inhibitor, can potently inhibit VEGFR2, VEGFR3, c-Kit and PDGFRbeta with IC50 of 6 nM, 4 nM, 1 nM and 15 nM. Telatinib (BAY 57-9352) impairs vascular function, induces rarefaction, and causes hypertension. Telatinib can inhibit the autophosphorylation of VEGFR2 autophosphorylation with an IC50 of 19 nM, and telatinib also suppresses VEGF-dependent proliferation of human umbilical vein endothelial cells with an IC50 of 26 nM.
In vivo The maximum-tolerated dose was not reached up to a dose of 1500 mg BID continuous dosing. Telatinib was rapidly absorbed with median t(max) of 3 hours or less.Telatinib is safe and well tolerated up to a dose of 1500 mg BID continuous dosing. Telatinib (450 mg b.i.d.) combined with bevacizumab (1 mg/kg bi-weekly) shows antitumor activity, but accumulating constitutional toxicity impedes long-term treatment of patients.
Clinical Trials N/A
Features N/A

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