CSF1R-IN-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CSF1R-IN-2 是一种口服活性的 SRC、MET 和 c-FMS 抑制剂（SRC、MET 和 c-FMS 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).

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.

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. Animal Model:Mice bearing LU2503 tumors patient derived xenograft (PDX) NSCLC model.Dosage:15 mg/kg.Administration:PO, BID (twice daily) for 13 days.Result:Resulted in an 85% tumor regression and no body weight loss was observed after 21 days treatment.Animal Model:SCID/Beige mice bearing Ba/F3 ETV6-CSF1R tumors with average tumor size of ~180 mm3.Dosage:5 and 15 mg/kg.Administration:PO, BID (twice daily) for 10 days.Result:Demonstrated the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively.

——

Tyrosine Kinase

Src

c-FMS|MET|SRC

——

——

2271119-26-5

409.42

C20H20FN7O2

>98% (HPLC)

DMSO:25 mg/mL (61.06 mM; Need ultrasonic)

N#CC1=C2CN(CC)C(C=C3)=NC(N3N=C4N)=C4C(NC[C@H](C)OC2=CC=C1F)=O

——

(-20℃)

With Ice Pack

≥ 2 years