JNJ-10198409 是相对选择性的、ATP 竞争性的、具有口服活性的血小板衍生生长因子受体酪氨酸激酶抑制剂，其IC50=2 nM。它对PDGFR-β激酶 (IC50=4.2 nM) 和PDGFR-α激酶 (IC50=45 nM) 有较好的抑制作用。它是双重机制的抗血管生成和肿瘤细胞的抗增殖剂。

JNJ- 10198409 is a relatively selective and ATP competitive PDGF-RTK inhibitor (IC50=2 nM). JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent.

JNJ-10198409 has effective antiproliferative activity in six of eight human tumor cell lines (IC50<0.033 μM). It also is a potent inhibitor of the c-Abl kinase (IC50: 22 nM) [1,2].

627518-40-5

C18H16FN3O2

325.34

JNJ-10198409;3-氟-N-(6,7-二甲氧基-2,4-二氢茚并[1,2-C〕吡唑-3-基苯基胺

DMSO:83.33 mg/mL (256.13 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years