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CAS No. : 2271119-26-5
MCE 国际站:Elzovantinib
产品活性:Elzovantinib (TPX-0022) 是 SRC,MET 和 c-FMS 的口服有效抑制剂, 其对 SRC,MET 和c-FMS 的 IC50 值分别为 0.12 nM,0.14 nM 和 0.76 nM。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:Src | c-Met/HGFR | c-Fms
In Vitro: Elzovantinib (TPX-0022) causes the suppression of MET autophosphorylation as well as the downstream STAT3, ERK and AKT phosphorylation at IC50 values of around 1-3 nM in SNU-5 and MKN-45 cell lines.
In Vivo: Elzovantinib (TPX-0022; p.o., BID, 13 days) treatment results in an 85% tumor regression and no body weight loss is observed after 21 days treatment in mice.
Elzovantinib (p.o., BID, 10 days) demonstrates the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively in SCID/Beige mice.
Elzovantinib inhibits MET activity in MKN-45 tumors following oral administration in mice.
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