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FLT

The fms-like tyrosine kinase (Fit) is a transmembrane receptor in the tyrosine kinase family. Expression of fit complementary DNA in COS cells conferred specific, high-affinity binding of vascular endothelial growth factor, also known as vascular permeability factor (VEGF-VPF).

  • Edicotinib
    T151991142363-52-7
    Edicotinib (JNJ-527) is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.
    • $64
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  • Pexidartinib
    T21151029044-16-3
    Pexidartinib (PLX-3397) is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.
    • $40
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  • Sorafenib
    T0093L284461-73-0
    Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic ferroptosis.
    • $34
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  • Tesevatinib
    TQ0166781613-23-8
    Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4).
    • $109
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  • Fedratinib
    T1995936091-26-8
    Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
    • $45
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  • Gilteritinib
    T44091254053-43-4
    Gilteritinib (ASP2215) is a potent inhibitor at the FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preClinicalal studies, gilteritinib showed strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 Clinicalal trials for acute myeloid leukemia.
    • $34
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  • Cabozantinib
    T2586849217-68-1
    Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.
    • $39
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  • Quizartinib
    T2066950769-58-1
    Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.
    • $53
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  • NCT-503
    T42131916571-90-8
    NCT-503 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH), inhibiting serine synthesis from 3-phosphoglycerate in cells.
    • $35
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  • Nintedanib
    T1777656247-17-5
    Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34/13/13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69/37/108 nM), PDGFRα, and PDGFRβ (IC50=59/65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.
    • $38
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  • JI6
    T64370856436-16-3In house
    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.
    • $163
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  • BPR1J-097 hydrochloride (1327167-19-0(free base))
    T4261
    BPR1J-097, a new-type small molecule FLT-3 inhibitor(IC50=11±7 nM), is with great anti-tumor activities in vivo.
    • $43
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  • BGB-102
    T10531807640-87-5
    BGB-102 (JNJ-26483327) is a kinase inhibitor targeting FLT3 and YES1 and an antagonist targeting EGFR and VEGFR3, which may be useful in the study of macular degeneration and diseases associated with genetic disorders and malformations.
    • $373
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  • UNC2025 2HCl (1429881-91-3(free base))
    T4419
    UNC2025 is a potent and orally bioavailable Mer/Flt3 dual inhibitor with IC50 of 0.8/0.74 nM for Mer/Flt3.
    • $51
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  • TG-46
    T20743936091-15-5In house
    TG-46 (TG46) inhibits JAK2, FLT3, RET, JAK3 and can be used to study glaucoma.
    • $195
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  • Cabozantinib hydrochloride
    T51641817759-42-4
    Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).
    • $37
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  • SB1317 hydrochloride (1204918-72-8(free base))
    T4227
    SB1317 hydrochloride (1204918-72-8(free base)) (TG-02 hydrochloride) is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
    • $45
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  • SKLB 1028
    T346561350544-93-2In house
    SKLB 1028 (Ruserontinib) is a new type of oral multikinase inhibitor of EGFR, FLT3, and Abl. SKLB 1028 shows excellent activity in FLT3-driven AML models and considerable potency in CML models containing Abl mutants.
    • $51
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  • TG-89
    T20742936091-56-4In house
    TG-89 is an inhibitor of JAK2, JAK3, RET and FLT3, and has an IC50 value of 11.2 μM against JAK2, showing anticancer activity in the treatment of ovarian and cervical cancer.
    • $56
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  • OTS447
    T629791356943-67-3In house
    OTS447 is a potent FLT3 inhibitor (IC50: 21 nM) with potential anticancer activity for cancer research .
    • $158
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  • AXL-IN-13
    T733002376928-82-2In house
    AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 value of 1.6 nM and a Kd value of 0.26 nM.AXL-IN-13 exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) and inhibits cancer cell migration and invasion.
    • $79
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  • JAK3-IN-14
    T67754454234-24-3In house
    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.
    • $226
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  • 4SC-203
    T9473895533-09-2In house
    4SC-203 is a multikinase inhibitor with potential antineoplastic activity. 4SC-203 selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs).
    • $83
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  • NVP-AEW541
    T6080475489-16-8
    NVP-AEW541 (AEW541), a potent inhibitor of IGF-1R(IC50=150 nM) and InsR(IC50=140 nM), exhibits excellent efficiency and specificity for IGF-1R in a cell-based assay.
    • $41
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  • AST 487
    T4053630124-46-8
    AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
    • $31
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  • SB1317
    T26531204918-72-8
    SB1317 (TG02) is a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3).
    • $64
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  • Sorafenib tosylate
    T0093475207-59-1
    Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
    • $37
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  • Pacritinib
    T6020937272-79-2
    Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
    • $34
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  • OSI-930
    T2624728033-96-3
    OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.
    • $47
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  • AT9283
    T3068896466-04-9
    AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
    • $39
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  • Cediranib
    T2500288383-20-0
    Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells.
    • $35
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  • Rebastinib
    T26401020172-07-9
    DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit. Rebastinib aimed at the Angiopoietin2-Tie2 pathway.
    • $40
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  • R406
    T6174841290-81-1
    R406 (R-406 besylate) is an effective Syk inhibitor (IC50: 41 nM) and shows no effects on Lyn.
    • $40
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  • Crenolanib
    T2677670220-88-9
    Crenolanib (ARO 002) is an orally bioavailable type III tyrosine kinases inhibitor of PDGFRα/β and FLT3 (IC50s: 11, 3.2, and 4 nM).
    • $53
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  • FLT3-IN-3
    T112982229050-90-0
    FLT3-IN-3 is an effective FLT3 inhibitor, and the IC50s of FLT3 WT and FLT3 D835Y are 13 and 8 nM, respectively.
    • $109
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  • Sunitinib
    T0374L557795-19-4
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activity and can be used for the treatment of kidney cancer and gastrointestinal tumors.
    • $53
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  • Brigatinib
    T36211197953-54-0
    Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor.
    • $30
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  • Amuvatinib
    T2516850879-09-3
    Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.
    • $44
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  • Sitravatinib
    T43491123837-84-2
    Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.
    • $47
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  • HM43239
    T94282294874-49-8
    HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells [1] [2] [3].
    • $64
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  • KG5
    T41003877874-85-6
    KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.
    • $48
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  • FLT3-IN-10
    T98562088735-51-5
    FLT3-IN-10 (2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl-) (compound 7c) is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3). FLT3-IN-10 shows the potential for the treatment of FLT3-mutated acute myeloid leukemia (AML).
    • $54
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  • 3-Hydroxy Midostaurin
    T12610L179237-49-1
    3-Hydroxy Midostaurin (CGP 52421), a PKC412 metabolite, inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50 values of roughly 132 nM in culture medium and 9.8 μM in plasma. Though less selective, it exhibits greater cytotoxicity compared to PKC412[1].
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  • AC710
    TQ02351351522-04-7
    AC710 is a potent PDGFR inhibitor (Kds: 0.6, 1, 1.57, 1.3, 1 nM for FLT3, KIT, CSF1R, PDGFRα and PDGFRβ).
    • $30
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  • SGI-1776
    T30781025065-69-3
    SGI-1776 (Pim-Kinase Inhibitor IX) has been used in trials studying the treatment of Prostate Cancer, Non-Hodgkins Lymphoma, and Relapsed/Refractory Leukemias.
    • $48
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  • R406 free base
    T2467841290-80-0
    R406 free base (R406 (free base)) is a potent Syk inhibitor.
    • $39
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  • CCT241736
    T44281402709-93-6
    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.
    • $55
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  • SGI-7079
    T69821239875-86-5
    SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR inhibitor resistance.
    • $41
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  • Ilorasertib
    TQ00591227939-82-3
    Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A/Aurora B/Aurora C (IC50s: 120 nM/7 nM/1 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).
    • $55
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  • Sunitinib Malate
    T0374341031-54-7
    Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
    • $37
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