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.

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).

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.

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.

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

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.