Drug intelligence / Profile preview

Ki11502

Development stage
Preclinical
Lead developer
Kyowa Kirin
Modality
Small Molecules
Administration
Oral
01

Overview

**Ki11502** is a novel multitargeted **small molecule** receptor tyrosine kinase inhibitor selective for platelet-derived growth factor receptor alpha and beta (PDGFRα/β). It also shows inhibitory activity against several other kinases, including FMS-like tyrosine kinase 3 (FLT3), KIT (c-KIT), KDR (VEGFR2), and non-receptor tyrosine kinase SRC. Ki11502 induces growth arrest, G0/G1 cell cycle arrest, and apoptosis in hematologic malignancies (such as eosinophilic leukemia and acute myeloid leukemia) with abnormal RTK signaling, including those resistant to imatinib. It disrupts downstream signaling by lowering phosphorylation of key proteins such as Akt, ERK, and STAT5, downregulates antiapoptotic Bcl-2 family members, and is effective even against certain imatinib-resistant mutations (PDGFRαT674I, KITT670I mutants). It has shown marked antiproliferative effects in vitro and in xenograft leukemia models without notable adverse effects[1][2][3][7][9].

Other names
Ki11502Ki-11502Ki 11502
02

Targets

FLT3 (Fms related receptor tyrosine kinase 3)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)

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