CSF1R-IN-2 是一种口服具有活力的、有效的 Src，MET 和 c-Fms 抑制剂，它们的 IC50 值分别为 0.12 nM，0.14 nM 和 0.76 nM。

CSF1R-IN-2 is an oral-active SRC, MET and c-FMS inhibitor (IC50s: 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively).

The suppression of MET autophosphorylation as well as the downstream STAT3 caused by CSF1R-IN-2, ERK and AKT phosphorylation at IC50 values of around 1-3 nM in SNU-5 and MKN-45 cell lines.

In mice, CSF1R-IN-2 (p.o., BID, 13 days) treatment results in an 85% tumor regression, and no bodyweight loss is observed after 21 days of treatment. In SCID/Beige mice. CSF1R-IN-2 (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 mice, CSF1R-IN-2 inhibits MET activity in MKN-45 tumors following oral administration.

2271119-26-5

C20H20FN7O2

409.42

DMSO:25 mg/mL (61.06 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years