G-749

G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants with IC50s of 0.4/0.6/3.5/7.5 nM for Wt Flt3/D835Y/MV4-11/Molm-14 respectively.IC50 value: 0.4/0.6/3.5/7.5 nM(Wt Flt3/D835Y/MV4-11/Molm-14) [1]Target: Flt3 inhibitorG-749 showed potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays. G-749 retained its inhibitory potency in various drug-resistance milieus such as patient plasma, FLT3 ligand surge, and stromal protection. Furthermore, it displayed potent antileukemic activity in bone marrow blasts from AML patients regardless of FLT3 mutation status, including those with little or only minor responses to AC220 or PKC412. Oral administration of G-749 yielded complete tumor regression and increased life span in animal models.

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3

Research Areas >> Cancer

[1]. Lee HK, et al. G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood. 2014 Apr 3;123(14):2209-19.

Gilteritinib | Quizartinib (AC220) | Pacritinib | Linifanib (ABT-869) | LY2784544 | DCC-2036 (Rebastinib) | Dovitinib (TKI-258, CHIR-258) | SB1317 | mrx-6313 | CHIR-124 | KW-2449 | ENMD-2076 | AST 487 | Tandutinib (MLN518) | TG101209