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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).

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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TargetMol | Inhibitor Hot
Ripretinib
T84821442472-39-0
Ripretinib (DCC-2618) is an orally bioavailable inhibitor of (KIT) and (PDGFRA).
  • $73
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TargetMol | Inhibitor Hot
gilteritinib
T44091254053-43-4
Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.
  • $34
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TargetMol | Inhibitor Hot
Fostamatinib
T6115901119-35-5
Fostamatinib (R788)(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.
  • $36
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Sorafenib
T0093L284461-73-0
Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets 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. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.
  • $34
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Pexidartinib
T21151029044-16-3
Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.
  • $40
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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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Fostamatinib Disodium
T26051025687-58-4
Fostamatinib Disodium (R788 Disodium) is an orally available Syk kinase inhibitor with potential anti-inflammatory and immunomodulatory activities.
  • $39
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UNC2025
T70071429881-91-3
UNC2025 (mrx-6313)(IC50 of 0.74 nM and 0.8 nM) is a potent and orally bioavailable dual MER FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3.
  • $33
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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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TargetMol | Inhibitor Hot
Merestinib
T34551206799-15-6
Merestinib (LY2801653) is an orally available, small molecule inhibitor of the proto-oncogene c-Met (Ki: 2 nM) with potential antineoplastic activity. Merestinib electively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing the constitutively activated c-Met protein.
  • $45
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GSK-1070916
T6129942918-07-2
GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B C with IC50 of 3.5 nM 6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.
  • $41
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NCT-503
T42131916571-90-8
NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=2.5 µM) with no activity against other dehydrogenases. NCT-503 has antitumor activity and inhibits the growth of PHGDH-dependent tumors.
  • $35
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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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MRX-2843
T161441429882-07-4
MRX-2843 (UNC2371) is a potent and orally active inhibitor of MERTK and FLT3(IC50s of 1.3 nM and 0.64 nM, respectively).
  • $59
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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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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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Brigatinib
T36211197953-54-0
Brigatinib (AP-26113) is a highly potent and selective inhibitor of ALK.
  • $30
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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). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.
  • $30
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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.
  • $35
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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].
  • $61
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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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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.
  • $189
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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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