FLT3 Inhibitor

Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC₅₀ values of 13 nM, 73 nM and 56 nM, respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma.

MAX-40279 is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 is also effective against the FLT3 mutants such as FLT3^D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 can be used for the research of acute myelogenous leukemia (AML).

SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with K_d values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively.

CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with K_i values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation.

Itacnosertib (TP-0184) is the inhibitor for FLT3, ACVR1 (ALK2, IC₅₀=8 nM) and JAK2 (IC₅₀=8540 nM). Itacnosertib exhibits anti-leukemic activity.

DLK-IN-1 (Compound 14) is an orally active, blood-brain barrier-penetrable and selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a K_i value of 3 nM. DLK-IN-1 inhibits Flt3, PAK4, STK33 and TrkA. DLK-IN-1 reduces p-c-Jun. DLK-IN-1 can be used in Alzheimer's disease research.

FLT3-IN-3 is a potent FLT3 inhibitor with IC₅₀s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.

Gilteritinib (Standard) is the analytical standard of Gilteritinib. This product is intended for research and analytical applications. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC₅₀s of 0.29 nM/0.73 nM, respectively.

Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC₅₀ value of 55 nM for human FLT3, and has antitumor activity.

FLT3-IN-17 inhibits CYPs and FLT3 mutants activity (IC₅₀s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC₅₀ value of 12 nM. FLT3 ligand-2 can be used in the research of cancers.

Cabozantinib (Standard) is the analytical standard of Cabozantinib. This product is intended for research and analytical applications. Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC₅₀ values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC₅₀=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.

Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.

PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC₅₀ of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor.

BPR1K871 is a potent and selective dual FLT3/AURKA inhibitor with IC₅₀s of 19 nM and 22 nM for FLT3 and AURKA, respectively, acts as a preclinical development candidate for anti-cancer therapy.

Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC₅₀ value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC₅₀ = 1.5 nM; MOLM-13: IC₅₀ = 1.4 nM). Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia.

Pacritinib (SB1518) citrate is a potent inhibitor of both wild-type JAK2 (IC₅₀=23 nM) and JAK2^V617F mutant (IC₅₀=19 nM). Pacritinib citrate also inhibits FLT3 (IC₅₀=22 nM) and its mutant FLT3^D835Y (IC₅₀=6 nM). Pacritinib citrate can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF).

(E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor.

JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC₅₀ of 23 nM, also effectively inhibits Flt3, with an IC₅₀ of 18 nM.

SKLB4771 is a potent and selective Flt3 inhibitor with an IC₅₀ value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue.

CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A K_d, 7.5 nM, IC₅₀, 38 nM; Aurora-B K_d, 48 nM), FLT3 kinase (K_d, 6.2 nM), and FLT3 mutants including FLT3-ITD (K_d, 38 nM) and FLT3(D835Y) (K_d, 14 nM).