8-环戊基-7,8-二氢-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-7-氧代-吡啶并[2,3-D]嘧啶-6-甲腈

Cdk4/cyclin D1:3.87 nM (IC50)

CDK6/cyclinD1:9.82 nM (IC50)

ARK5:4.95 nM (IC50)

FGFR1:26 nM (IC50)

PDGFRβ:26 nM (IC50)

PI3K-δ:144 nM (IC50)

[1]. Divakar SK, et al. Dual inhibition of CDK4/Rb and PI3K/AKT/mTOR pathways by ON123300 induces synthetic lethality in mantle cell lymphomas. Leukemia. 2016 Jan;30(1):86-93.

[2]. Perumal D, et al. Dual Targeting of CDK4 and ARK5 Using a Novel Kinase Inhibitor ON123300 Exerts Potent Anticancer Activity against Multiple Myeloma. Cancer Res. 2016 Mar 1;76(5):1225-36.

[3]. Zhang X, et al. Preclinical pharmacological evaluation of a novel multiple kinase inhibitor, ON123300, in brain tumor models. Mol Cancer Ther. 2014 May;13(5):1105-16.