Crenolanib
PDGFR and FLT3 inhibitor / Crenolanib is a potent inhibitor of PDGFR (Kd for α = 2.1 nM; ß = 3.2 nM) and FLT3 (Kd = 0.74 nM).1 Crenolanib is a type I inhibitor binding only to the active kinase conformation. It showed potent activity against imatinib-resistant PDGFRα mutations D842I, D842V, D842Y, DI842-843M, and deletion I8432 as well as FLT3/ITD and FLT3/D835 mutants3. Crenolanib acted synergistically with FLT3-CAR T-cells in a FLT3-ITD+ AML murine xenograft model.4
Biochemicals & reagents
670220-88-9
CP-868,596
1) Lewis et al. (2009) Phase I study of the safety, tolerability, and pharmacokinetics of oral CP-868,596, a highly specific platelet-derived growth factor receptor tyrosine kinase inhibitor in patients with advanced cancers; J. Clin. Oncol. 27 5262 2) Smith et al. (2014) Crenolanib is a selective type I pan-FLT3 inhibitor; Proc. Natl. Acad. Sci. USA 111 5319 3) Heinrich et al. (2012) Crenolanib Inhibits Drug-Resistant PDGFRA D842V Mutation Associated with Imatinib-Resistant Gastrointestinal Stromal Tumors; Clin. Cancer Res. 18 4375 4) Jetani et al. (2018) CAR T-cells targeting FLT3 have potent activity against FLT-ITD+ AML and act synergistically with the FLT3-inhibitor crenolanib; Leukemia 32 1168
-20°C
TARGET: Kinase -- DISEASE AREA: Cancer