FLT3 Inhibitor

Flonoltinib maleate is a potent and orally active dual JAK2/FLT3 inhibitor with IC₅₀ values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.

Fostamatinib (disodium hexahydrate) (Standard) is the analytical standard of Fostamatinib (disodium hexahydrate). This product is intended for research and analytical applications. Fostamatinib (R788) disodium hexahydrate is the oral proagent of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).

KW-2449 (Standard) is the analytical standard of KW-2449 (HY-10339). This product is intended for research and analytical applications. KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC₅₀s of 6.6, 14, 4 and 48 nM, respectively.

BPR1J-340 is a potent FLT3 inhibitor with an IC₅₀ of ~25 nM. BPR1J-340 inhibits the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD⁺ acute myeloid leukemia (AML) cells. BPR1J-340 exhibits significant anti-tumor activities.

R406 (Standard) is the analytical standard of R406 (HY-12067). This product is intended for research and analytical applications. R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk K_inase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM).

Dovitinib (lactate) (Standard) is the analytical standard of Dovitinib (lactate). This product is intended for research and analytical applications. 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.

Fostamatinib Disodium (Standard) is the analytical standard of Fostamatinib Disodium. This product is intended for research and analytical applications. Fostamatinib Disodium (R788 Disodium) is the oral proagent of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).

MRX-2843 hydrochloride is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC₅₀s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively.

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

FLT3-IN-27 (compound 49) is a FLT3-ITD inhibitor with the IC₅₀ of 174 nM. FLT3-IN-27 inhibits cell growth and increases the number of cells in the G1 phase of the cell cycle and can be used for study of acute myeloid leukemia.

ENMD-2076 (Standard) is the analytical standard of ENMD-2076 (HY-10987A). This product is intended for research and analytical applications. ENMD-2076 is a multi-targeted K_inase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, K_dR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

FN-1501 (Standard) is the analytical standard of FN-1501 (HY-111361). This product is intended for research and analytical applications. FN-1501 is a potent inhibitor of FLT3 and CDK, with IC₅₀s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.

Gilteritinib hemifumarate (Standard) is the analytical standard of Gilteritinib hemifumarate. This product is intended for research and analytical applications. Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.

Ripretinib (Standard) is the analytical standard of Ripretinib. This product is intended for research and analytical applications. Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2). DCC-2618 exerts antineoplastic effect and induces apoptosis.

Quizartinib (AC220) (Standard) is the analytical standard of Quizartinib (HY-13001). This product is intended for research and analytical applications. Quizartinib is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer.

Tandutinib (MLN518) sulfate is a potent and selective inhibitor of the FLT3 with an IC₅₀ of 0.22 μM, and also inhibits c-Kit and PDGFR with IC₅₀s of 0.17 μM and 0.20 μM, respectively. Tandutinib sulfate can be used for acute myelogenous leukemia (AML). Tandutinib sulfate has the ability to cross the blood-brain barrier.

R406 free base (Standard) is the analytical standard of R406 (free base) (HY-11108). This product is intended for research and analytical applications. R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk K_inase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM).

Pacritinib (Standard) is the analytical standard of Pacritinib. This product is intended for research and analytical applications. Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).

ENMD-2076 Tartrate (Standard) is the analytical standard of ENMD-2076 (Tartrate) (HY-10987). This product is intended for research and analytical applications. ENMD-2076 Tartrate is a multi-targeted K_inase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, K_dR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

Mivavotinib (monohydrochloride) (Standard) is the analytical standard of Mivavotinib (monohydrochloride) (HY-100867A). This product is intended for research and analytical applications. TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).