CSF1R-IN-2 (compound 5) 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。
货号:ajcx38640
CAS:2271119-26-5
分子式:C20H20FN7O2
分子量：409.42
溶解度:DMSO : 25 mg/mL (61.06 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively[1].

CSF1R-IN-2 (compound 5) 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[1].

CSF1R-IN-2 (compound 5: 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[1].CSF1R-IN-2 (compound 5: 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[1].CSF1R-IN-2 (compound 5) inhibits MET activity in MKN-45 tumors following oral administration in mice[1].

[1]. WO 2019023417 A1.