среда, 14 марта 2012 г.

Telatinib

Telatinib (BAY 57-9352)

Telatinib (BAY 57-9352) is an new orally available, multitargeted tyrosine kinases inhibitor (VEGFR-2, VEGFR-3, PDGFR-β and c-Kit) with an IC50 of 19 nanomol for the inhibition of VEGFR-2 autophosphorylation. 
Telatinib (BAY 57-9352, CP 127374; NSC 330507; KOS 953; Tanespimycin) also inhibits VEGF-dependent proliferation of human umbilical vein endothelial cells (HUVECs) with an IC50 of 26 nM and PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM. Telatinib demonstrates anticancer activity in various tumor models. Formation of the N-glucuronides of telatinib is identified as the major biotransformation pathway in man.


Телатиниб - новый оральный мультикиназный ингибитор (VEGFR-2, VEGFR-3, PDGFR-β and c-Kit) с IC50 равной 19 наномолям для ингибирования VEGFR-2 автофосфорилирования.

Synonyms:     BAY 57-9352, CP 127374; NSC 330507; KOS 953; Tanespimycin
Molecular Weight:     409.83
Formula:        C20H16ClN5O3
Solubility:         DMSO ≥ 83mg/mL     Water <1mg/mL     Ethanol ≥1mg/mL
CAS No.:         332012-40-5





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