FLT3

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FLT3 Inhibitors (19)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1119 Cabozantinib (XL184, BMS-907351) Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively.
  • Cancer Discov, 2014, 4(7):816-27
  • Nat Commun, 2014, 5:3116
  • Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0274
S2194 R406 R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 1.
  • Immunity, 2014, 40(3):389-99
  • Nat Cell Biol, 2015, 17(1):57-67
  • Mol Syst Biol, 2015, 11(1):789
S1526 Quizartinib (AC220) Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM in MV4-11 and RS4;11 cells, respectively, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Phase 3.
  • Nat Commun, 2014, 5:3672
  • Blood, 2014, 123(18):2826-37
  • Blood, 2014, 123(5):734-42
S1018 Dovitinib (TKI-258, CHIR-258) Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.
  • Cancer Res, 2013, 73(16):5195-205
  • Haematologica, 2011, 96(6):922-6
  • Expert Opin Inv Drugs, 2014, 23(4):469-87
S1244 Amuvatinib (MP-470) Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Phase 2.
  • Nat Genet, 2012, 44(8):852-60
  • Cancer Res, 2014, 74(20):5878-90
  • Oncogene, 2014, 33(10):1316-24
S1043 Tandutinib (MLN518) Tandutinib (MLN518, CT53518) is a potent FLT3 antagonist with IC50 of 0.22 μM, also inhibits PDGFR and c-Kit, 15 to 20-fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR and KDR. Phase 2.
  • Mol Syst Biol, 2015, 11(1):789
  • Cancer Lett, 2016, 377(2):149-57
  • Br J Cancer, 2012, 107(10):1702-13
S2692 TG101209 TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.
  • Leukemia, 2014, 28(7):1519-28
  • Cancer Lett, 2013, 341(2):224-30
  • ACS Chem Biol, 2014, 9(5):1160-71
S7576 UNC-2025 UNC-2025 is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
S7533 AMG 925 AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively.
S7003 AZD2932 AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
S7765 Dovitinib (TKI258) Lactate Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
  • Genome Biol, 2014, 15(8):428
S7545 G-749 G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases.
S7119 Go6976 Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
  • Cell Signal, 2016, 28(9):1422-31
S8023 TCS 359 TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM.
S8057 Pacritinib (SB1518) Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.
S2158 KW-2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.
S1181 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
  • Cancer Res, 2013, 73(20):6310-22
  • PLoS One, 2014, 9(7):e102741
  • Vet Comp Oncol, 2013, 10.1111/vco.12046
S2769 Dovitinib (TKI-258) Dilactic Acid Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
  • Cancer Lett, 2016, 380(1):163-173
  • Expert Opin Inv Drugs, 2014, 23(4):469-87
  • Br J Cancer, 2011, 104(1):75-82
S2018 ENMD-2076 L-(+)-Tartaric acid ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1119 Cabozantinib (XL184, BMS-907351) <1 mg/mL 100 mg/mL <1 mg/mL
S2194 R406 <1 mg/mL 126 mg/mL 8 mg/mL
S1526 Quizartinib (AC220) <0.3 mg/mL 33.2 mg/mL <0.5 mg/mL
S1018 Dovitinib (TKI-258, CHIR-258) <1 mg/mL 30 mg/mL <1 mg/mL
S1244 Amuvatinib (MP-470) <1 mg/mL 32 mg/mL <1 mg/mL
S1043 Tandutinib (MLN518) <1 mg/mL 5 mg/mL 6 mg/mL
S2692 TG101209 <1 mg/mL 102 mg/mL <1 mg/mL
S7576 UNC-2025 100 mg/mL 25 mg/mL 8 mg/mL
S7533 AMG 925 <1 mg/mL 0.01 mg/mL <1 mg/mL
S7003 AZD2932 <1 mg/mL 89 mg/mL 5 mg/mL
S7765 Dovitinib (TKI258) Lactate 66 mg/mL 100 mg/mL 1 mg/mL
S7545 G-749 <1 mg/mL 24 mg/mL <1 mg/mL
S7119 Go6976 <1 mg/mL 18 mg/mL <1 mg/mL
S8023 TCS 359 <1 mg/mL 15 mg/mL <1 mg/mL
S8057 Pacritinib (SB1518) <1 mg/mL 11 mg/mL <1 mg/mL
S2158 KW-2449 <1 mg/mL 67 mg/mL 67 mg/mL
S1181 ENMD-2076 1 mg/mL 105 mg/mL <1 mg/mL
S2769 Dovitinib (TKI-258) Dilactic Acid 70 mg/mL 90 mg/mL <1 mg/mL
S2018 ENMD-2076 L-(+)-Tartaric acid <1 mg/mL 100 mg/mL <1 mg/mL
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