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Elzovantinib

CAS No. : 2271119-26-5

MCE 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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