flt3 (d835y)

FLT3-IN-3 is an effective FLT3 inhibitor, and the IC50s of FLT3 WT and FLT3 D835Y are 13 and 8 nM, respectively.

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.

Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.

G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.

Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).

FLT3-ITD/D835Y-IN-1 (Compound 1) is an inhibitor of FLT3-ITD and BCR-ABL. It induces pro-apoptotic (apoptosis) effects by inhibiting the FLT3 and BCR-ABL pathways, along with potentially other targets. This compound is applicable in acute myeloid leukemia (AML) research.

FLT3/D835Y-IN-1 (compound 13a) is an orally active, selective inhibitor of FLT3 and FLT3/D835Y with IC50 values of 0.26 nM and 0.18 nM, respectively. It exhibits anticancer efficacy and has research value in AML (acute myeloid leukemia).

JI6 (JAK3 Inhibitor VI) is a potent, selective and orally active FLT3 inhibitor. JI6 exhibits IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits c-Kit and JAK3, with IC50s of ∼500 and ∼250 nM, respectively. JI6 has research value in acute myeloid leukemia.

JAK3-IN-14 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively.

Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

FLT3-IN-29 (Compound MY-10) is an FLT3 inhibitor with IC50 values of 6.5 nM and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants, respectively. It induces cell cycle arrest at the G0 G1 phase and effectively triggers apoptosis (Apoptosis). Additionally, FLT3-IN-29 reduces reactive oxygen species (ROS) and mitochondrial membrane potential (MMP), displaying anti-leukemic properties.

FLT3-IN-25 (compound 17) is a potent FLT3 inhibitor, demonstrating IC50 values of 1.2 nM for FLT3-WT, 1.4 nM for FLT3-D835Y, and 1.1 nM for FLT3-ITD. This compound plays a significant role in the treatment of acute myeloid leukemia (AML).

FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor targeting FLT3 and CHK1, with IC50 values of 25.63 nM for CHK1, 16.39 nM for FLT3-WT, and 22.80 nM for FLT-D835Y. It displays favorable oral pharmacokinetic properties and kinase selectivity. FLT3/CHK1-IN-2 is applicable in acute myeloid leukemia (AML) research.

FLT3D835Y/F691L-IN-1 (compd 8v) is an orally active inhibitor targeting the secondary mutations D835Y/F691L in the FLT3 tyrosine kinase domain, with IC50 values of 1.5 and 9.7 nM, respectively. This compound is applicable in research related to acute myeloid leukemia.

BPR1J-097) is a novel FLT-3 inhibitor(IC50: 11±7 nM) with promising in vivo anti-tumor activities. It also inhibits FLT-3 D835Y (IC50: 3 nM).

JH-IX-179 is a novel type I ATP competitive and highly selective FLT3 inhibitor. JH-IX-179 is much more selective for FLT3 and FLT3 mutants than for Kronani. In addition, JH-IX-179 showed little human serum protein binding and effectively inhibited autoph

BPR1J-097, a new-type small molecule FLT-3 inhibitor(IC50=11±7 nM), is with great anti-tumor activities in vivo.

CCT241736 is an orally bioavailable dual FLT3/Aurora kinase inhibitor that also inhibits clinically relevant FLT3-resistant mutants including FLT3-ITD and FLT3, CCT241736, an advanced analog of CCT137690, is a preclinical development candidate for the treatment of human malignancies, and in particular AML in adults and children.

FLT3-IN-11 (compound 30) is an orally active, potent, and selective inhibitor of FLT3 kinase that targets wild-type FLT3 (IC50: 7.22 nM) and FLT3-D835Y (IC50: 4.95 nM), demonstrating significant anti-AML effects with an IC50 value of 3.2 nM for MV4-11 cells.

FLT3-IN-12 is a selective, potent, orally active FLT3 kinase inhibitor that acts on FLT3-WT (IC50: 1.48 nM) and FLT3-D835Y (IC50: 2.87 nM). FLT3-IN-12 is more selective than c-KIT (>1000-fold). FLT3-IN-12 showed significant anti-AML effects, with an IC50 value of 0.75 nM for MV4-11 cells.

FLT3-IN-15 is an orally active and potent FLT3 inhibitor, capable of acting on FLT3 (IC50: 0.87 nM) and FLT3/D835Y (IC50: 0.32 nM).

FLT3/ITD-IN-4 (Compound 16) is a selective inhibitor of FLT3 internal tandem repeat mutations (FLT3-ITD) with an IC50 of 2.3 nM and is applicable for studying acute myeloid leukemia.

FLT3-IN-17 is an FAK inhibitor (IC50: 12 nM). FLT3-IN-17 inhibits the activity of CYPs and FLT3 mutants and has an IC50 of <0.5 nM for D835Y. FLT3-IN-17 can be used in cancer research.