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FLT3
Isoform-selective Products
- All (54)
- FLT3 Inhibitors (54)
- New FLT3 Products
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S1018 | Dovitinib (TKI-258) | Dovitinib (TKI-258, CHIR258) is a multitargeted RTK inhibitor, primarily targeting class III RTKs (FLT3/c-Kit) with IC50 values of 1 nM/2 nM. It is also potent against class IV (FGFR1/3) and class V (VEGFR1-4) RTKs, exhibiting IC50 values of 8–13 nM, while showing lower potency toward InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R, and HER2 in cell-free assays. Phase 4. |
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| S7754 | Gilteritinib (ASP2215) | Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM). | ||
| S7765 | Dovitinib (TKI258) Lactate monohydrate | Dovitinib (TKI258) Lactate monohydrate 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. |
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| S1043 | Tandutinib (MLN518) | Tandutinib (MLN518, CT53518, NSC726292) is a potent FLT3 antagonist with IC50 of 0.22 μM. This compound also inhibits PDGFR and c-Kit, with 15 to 20-fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR and KDR. It was studied in Phase 2. |
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| 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. |
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| 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. |
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| S9662 | UNC2025 | UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. This compound also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively. | ||
| 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. | ||
| S8023 | TCS 359 | TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7533 | AMG 925 | AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively. | ||
| 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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| E2387 | FLT3-IN-2 | FLT3-IN-2 is a FLT3 inhibitor with IC50 of ＜ 1 μM. | ||
| 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. | ||
| S7640New | 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. |
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| S1460 | SP600125 | SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. This compound is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A，FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. It inhibits autophagy and activates apoptosis. |
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| S7397 | Sorafenib (BAY 43-9006) | Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib 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 induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
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| S1040 | Sorafenib tosylate | 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. This compound 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. It induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
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| 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. |
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| S1048 | Tozasertib (VX-680) | Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| S7818 | Pexidartinib (PLX3397) | Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. This compound induces apoptosis and necrosis with antitumor activity. Phase 3. |
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| S2730 | Crenolanib | Crenolanib is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. This compound helps to induce mitophagy. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| E4720New | 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, JAK2V617F, 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. | ||
| S1018 | Dovitinib (TKI-258) | Dovitinib (TKI-258, CHIR258) is a multitargeted RTK inhibitor, primarily targeting class III RTKs (FLT3/c-Kit) with IC50 values of 1 nM/2 nM. It is also potent against class IV (FGFR1/3) and class V (VEGFR1-4) RTKs, exhibiting IC50 values of 8–13 nM, while showing lower potency toward InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R, and HER2 in cell-free assays. Phase 4. |
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| S7754 | Gilteritinib (ASP2215) | Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM). | ||
| S7765 | Dovitinib (TKI258) Lactate monohydrate | Dovitinib (TKI258) Lactate monohydrate 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. |
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| S1043 | Tandutinib (MLN518) | Tandutinib (MLN518, CT53518, NSC726292) is a potent FLT3 antagonist with IC50 of 0.22 μM. This compound also inhibits PDGFR and c-Kit, with 15 to 20-fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR and KDR. It was studied in Phase 2. |
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| 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. |
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| 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. |
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| S9662 | UNC2025 | UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. This compound also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively. | ||
| 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. | ||
| S8023 | TCS 359 | TCS 359 is a potent FLT3 inhibitor with IC50 of 42 nM. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S7533 | AMG 925 | AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively. | ||
| 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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| E2387 | FLT3-IN-2 | FLT3-IN-2 is a FLT3 inhibitor with IC50 of ＜ 1 μM. | ||
| 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. | ||
| S7640New | 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. |
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| S1460 | SP600125 | SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. This compound is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A，FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. It inhibits autophagy and activates apoptosis. |
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| S7397 | Sorafenib (BAY 43-9006) | Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib 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 induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
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| S1040 | Sorafenib tosylate | 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. This compound 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. It induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
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| 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. |
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| S1048 | Tozasertib (VX-680) | Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| S7818 | Pexidartinib (PLX3397) | Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. This compound induces apoptosis and necrosis with antitumor activity. Phase 3. |
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| S2730 | Crenolanib | Crenolanib is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src. This compound helps to induce mitophagy. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| E4720New | 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, JAK2V617F, 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. | ||
| S7640New | 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. | ||
| E4720New | 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, JAK2V617F, 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. |
Signaling Pathway Map
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