FLT3 Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
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 RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. This compound inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.	Int J Biol Macromol, 2025, 292:139119 Cell, 2021, 184(2):334-351.e20 Sci Adv, 2021, 7(4)eabd7851
S6662	AST-487 (NVP-AST487)	AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM.	Cancer Cell, 2022, S1535-6108(22)00312-9 Int J Mol Sci, 2022, 23(18)10819 Nat Commun, 2020, 21;11(1):1924
S8023	TCS 359	TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM.	Nat Commun, 2021, 12(1):2148 Blood, 2016, 127(23):2890-90
E2387	FLT3-IN-2	FLT3-IN-2 is a FLT3 inhibitor with IC50 of ＜ 1 μM.	Pathogens, 2022, 12(1)53
S8899	FF-10101	FF-10101 is a novel irreversible FLT3 inhibitor with ic50 of 0.20 nM and 0.16 nM for FLT3 (WT) and FLT3(D835Y), respectively.	Front Oncol, 2021, 11:686765
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.	Front Pharmacol, 2021, 12:730241
S1099	SKLB4771 (FLT3-IN-1)	SKLB4771 (FLT3-IN-1) is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with an IC50 of 10 nM.	Front Pharmacol, 2022, 13:899775
S7533	AMG 925	AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively.	Molecules, 2020, 8;25(9) pii: E2220
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.
E1437	PHI-101	PHI-101 is an orally active, potent third-generation inhibitor of FLT3 that overcomes resistance to multiple drug-resistant mutations. It has potential for research in relapsed or refractory acute myeloid leukemia (AML).
S0550	5'-Fluoroindirubinoxime	5'-Fluoroindirubinoxime (5’-FIO, compound 13), an indirubin derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
S9275	Isoguanosine	Isoguanosine (Crotonoside) inhibits FLT3 and HDAC3/6 for the treatment of AML. This compound is a naturally occurring active isomer of guanosine that is found in the seeds of Croton tiglium.
S7640^New	Lestaurtinib	Lestaurtinib (CEP-701, KT-5555) is a derivative of the indolocarbazole K252 and a staurosporine analog. It is an orally active inhibitor of receptor protein tyrosine kinases (RPTKs), which inhibits FLT3 and Trk, with an IC50 of 3 nM and < 25 nM, respectively. It also inhibits JAK2 with an IC50 of 0.9 nM.
S5986	FLT3-IN-3	FLT3-IN-3 is a potent inhibitor of FLT3 with IC50 values of 13 nM and 8 nM for FLT3 WT and FLT3 D835Y, respectively. This compound effectively suppresses the proliferation of FLT3-ITD-positive MV4-11 and MOLM-13 cell lines at low nanomolar concentrations.
S9892	HM43239	HM43239 is a novel potent small molecule FLT3 inhibitor that selectively inhibits not only FLT3 wild type, ITD mutants or TKD mutations, but also FLT3 ITD/TKD double mutations. IC50s' of this compound against FLT3 WT, FLT3 ITD and FLT3 D835Y kinases are 1.1 nM, 1.8 nM and 1.0 nM, respectively.
S1040	Sorafenib Tosylate (BAY 43-9006)	Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.	Int J Oncol, 2025, 67(3)72 Nature, 2024, 629(8013):927-936 Cell Mol Life Sci, 2024, 81(1):238
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. Quizartinib (AC220) induces apoptosis of tumor cells. Phase 3.	Signal Transduct Target Ther, 2025, 10(1):222 Leukemia, 2025, 39(9):2152-2162 EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2
S1048	Tozasertib (VX-680)	Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with K_i_app of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by this compound with both Ki of 30 nM. It induces apoptosis and autophagy, and is in Phase 2.	Cell Rep Med, 2025, S2666-3791(25)00102-8 Biochim Biophys Acta Mol Cell Res, 2025, 1872(7):120001 Cell Death Dis, 2024, 15(1):56
S2194	R406	R406(R406 besylate) 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. R406 induces apoptosis. Phase 1.	J Allergy Clin Immunol, 2025, 155(2):569-582 Int J Biol Sci, 2025, 21(12):5287-5304 Front Immunol, 2025, 16:1636917
S7083	Ceritinib	Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. This compound also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.	Signal Transduct Target Ther, 2025, 10(1):124 Leukemia, 2025, 10.1038/s41375-025-02682-8 Cell Mol Life Sci, 2025, 82(1):314
S4001	Cabozantinib malate	Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-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. This compound induces apoptosis.	Sci Rep, 2025, 15(1):35889 bioRxiv, 2025, 2025.08.15.670608 Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
S1533	R406 (free base)	R406 (free base) is a potent Syk inhibitor with IC50 of 41 nM in a cell-free assay, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. This compound triggers apoptosis. Phase 1.	Autophagy, 2025, 1-17. EMBO Rep, 2025, 10.1038/s44319-025-00444-2 J Transl Med, 2024, 22(1):283
S2736	Fedratinib (TG101348)	Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.	Leukemia, 2025, 39(7):1678-1691 Front Immunol, 2025, 16:1514618 Cancer Immunol Immunother, 2025, 74(3):79
S1111	Foretinib	Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.	J Microbiol, 2025, 63(2):e2409001 Int J Mol Sci, 2023, 24(1)757 Biol Open, 2023, 12(8)bio059994
S8032	PRT062607 (P505-15) HCl	PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.	Sci Adv, 2025, 11(31):eadu4270 Sci Rep, 2024, 14(1):7739 J Exp Med, 2023, 220(9)e20230054
S8229	Brigatinib	Brigatinib is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.	Leukemia, 2025, 10.1038/s41375-025-02682-8 Cell Death Dis, 2025, 16(1):194 Toxicol Appl Pharmacol, 2025, 498:117310
S2198	SGI-1776 free base	SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. SGI-1776 induces apoptosis and autophagy.	Cell Death Dis, 2024, 15(9):644 Mar Drugs, 2024, 22(10)444 Mol Cancer, 2023, 22(1):64
S7119	Go6976	Go6976 (PD406976) 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.	FASEB J, 2025, 39(12):e70768 bioRxiv, 2025, 2025.02.02.636139 Int J Biol Sci, 2024, 20(10):3956-3971
S1003	Linifanib (ABT-869)	Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). This compound induces autophagy and apoptosis, and is in Phase 3.	Biomed Pharmacother, 2024, 180:117533 Cell Death Discov, 2023, 9(1):57 Cancer Cell, 2022, S1535-6108(22)00312-9
S8057	Pacritinib	Pacritinib 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.	Front Pharmacol, 2025, 16:1549183 Toxicol In Vitro, 2025, S0887-2333(25)00050-5 Sci Adv, 2025, 11(36):eadu2796
S1244	Amuvatinib (MP-470)	Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. It suppresses c-MET and c-RET, and is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2.	Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2220 Hematol Oncol, 2025, 43(5):e70131 bioRxiv, 2024, 2023.11.21.568071
S2692	TG101209	TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET (c-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.	Signal Transduct Target Ther, 2025, 10(1):131 Phytomedicine, 2023, 117:154918 EBioMedicine, 2022, 78:103963
S7014	Merestinib (LY2801653)	Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. This compound also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.	Mol Oncol, 2025, 19(8):2366-2387 NPJ Breast Cancer, 2024, 10(1):65 Cancers (Basel), 2024, 16(12)2253
S7576	UNC2025 HCl	UNC2025 HCl 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.	Immunity, 2023, 56(8):1778-1793.e10 Cell Rep, 2022, 38(13):110600 Cancers (Basel), 2021, 13(23)6072
S8442	TAK-659 Hydrochloride	TAK-659 Hydrochloride is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.	Exp Ther Med, 2025, 29(6):110 Int J Mol Sci, 2024, 25(18)9914 Int J Mol Sci, 2022, 23(23)14706
S0278	SU5614	SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. This compound reduces cell proliferation and induces apoptosis.	Am J Pathol, 2024, S0002-9440(24)00326-2 Adv Sci (Weinh), 2021, e2101848 Front Cell Dev Biol, 2021, 9:797047
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.	Cancer Res, 2020, canres.1992.2020 Molecules, 2020, 8;25(9) pii: E2220 Development, 2016, 143(23):4394-4404
S9779	Emavusertib (CA-4948)	Emavusertib (CA-4948) is a potent and orally bioavailable inhibitor of interleukin-1 receptor-associated kinase 4/FMS-like Tyrosine Kinase 3 (IRAK4/FLT3) with anti-tumor activity.	Arthritis Rheumatol, 2021, 10.1002/art.42043
S7002	Zotiraciclib	Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency.
E4598	MEN1703(SEL24,SEL24-B489)	MEN1703 (SEL24, SEL24-B489) is a potent, type I, orally active, dual inhibitor of PIM and FLT3-ITD, that exhibits Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively. This Pim/flt3 kinase inhibitor exhibits its broad therapeutic potential in treatment of acute myeloid leukemia.
S6839	MRX-2843	MRX-2843 (UNC2371) is an orally active dual inhibitor of tyrosine kinases MERTK and FLT3 with IC50 of 1.3 nM and 0.64 nM, respectively.
E4720^New	Flonoltinib	Flonoltinib (JAK2/FLT3-IN-1) is a potent and selective dual inhibitor of JAK2 and FLT3, with IC50 of of 0.8, 1.4, and 15 nM against JAK2, JAK2^V617F, and FLT3, respectively, in in vitro kinase assays. It also inhibits cell proliferation and induces G2/M cell cycle arrest and apoptosis in Hemophagocytic Lymphohistiocytosis (HLH) patients' CD8+T cells, CTLL2 cells, and RAW 264.7 cells.
S6060	HPK1-IN-2	HPK1-IN-2 is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1, a serine/threonine Ste20-related protein kinase), Lck and Flt3 with IC50 of <0.05 μM, IC50 of <0.5 μM and IC50 of <0.05 μM, respectively. This compound exhibits antitumor activity.
E2658	FN-1501	FN-1501 is a potent inhibitor of Fms-like receptor tyrosine kinase 3 (FLT3) and cyclin-dependent kinase (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.