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MERTK/FLT3 Inhibitor
MRX-2843 hydrochloride is an orally active, ATP-competitive inhibitor targeting MERTK and FLT3 tyrosine kinases. It demonstrates potent enzymatic inhibitory activity with IC50 values of 1.3 nM for MERTK and 0.64 nM for FLT3. This compound is ideal for research applications investigating cancer therapies and related signaling pathways involving these kinases. -
FLT3 Inhibitor
AAE871 is a potent type I FLT3 inhibitor, exhibiting an IC50 value of 0.034 µM. It demonstrates significant biological activity in inhibiting FLT3 signaling, making it a valuable tool for investigating acute myeloid leukemia (AML) and related hematological malignancies. AAE871 is useful in preclinical studies aimed at understanding FLT3-mediated pathways and their role in cancer progression. -
FLT3 Inhibitor
FLT3-IN-38 is a selective FLT3 inhibitor that targets the FLT3 receptor tyrosine kinase, which is implicated in hematologic malignancies. This compound also exhibits off-target effects by inhibiting serine/threonine kinase haspin, a critical regulator of mitotic signaling. FLT3-IN-38 is suitable for cancer research applications, particularly in studies focused on the treatment of FLT3-mutated leukemias. -
FLT3 Inhibitor
FLT3-IN-14 is a potent inhibitor of the FLT3 receptor, exhibiting IC50 values of 5.6 nM for wild-type FLT3 and 1.4 nM for the FLT3-ITD mutant. This compound effectively reduces the phosphorylation of FLT3 at Y591, leading to cell cycle arrest in the G1 phase and subsequent induction of apoptosis. In preclinical studies, FLT3-IN-14 has demonstrated significant efficacy in reducing tumor growth within MV4-11 xenograft mouse models, highlighting its potential for therapeutic applications in FLT3-related malignancies. -
JAK2/Bcr-Abl/FLT3 Inhibitor
LS-104 is a non-ATP-competitive inhibitor targeting JAK2, Bcr-Abl, and FLT3. It effectively induces apoptosis in JAK2V617F-positive cells while inhibiting JAK2 autophosphorylation and downstream signaling pathways. Additionally, LS-104 demonstrates significant cytotoxic effects and inhibits the proliferation of FLT3-expressing leukemic cells. This hydroxystyryl-acrylonitrile compound holds potential for research into myeloproliferative disorders and refractory or relapsed hematologic malignancies. -
FLT3 Inhibitor
AFG206 is a first-generation ATP-competitive "type II" inhibitor of FLT3. This compound effectively inhibits cell proliferation with an IC50 of approximately 0.1 µM by inducing apoptosis in FLT3-ITD-Ba/F3 and D835Y-Ba/F3 cell lines. AFG206 holds significant promise for research applications related to acute myeloid leukemia. -
FLT3 Inhibitor
BPR1J-340 is a potent inhibitor of FLT3, exhibiting an IC50 of approximately 25 nM. It effectively inhibits the phosphorylation of FLT3 and STAT5, inducing apoptosis in FLT3-ITD positive acute myeloid leukemia (AML) cells. This compound demonstrates considerable anti-tumor activities, making it a valuable tool for research in cancer biology and therapeutic strategies targeting FLT3 dysregulation. -
FLT3 Inhibitor
Tandutinib sulfate is a selective inhibitor of FLT3, exerting its effects with an IC50 of 0.22 μM. It also targets c-Kit and PDGFR, with IC50 values of 0.17 μM and 0.20 μM, respectively. This compound is particularly relevant for research in acute myelogenous leukemia (AML) and is noted for its capacity to cross the blood-brain barrier, expanding its potential applications in hematological malignancies and central nervous system studies. -
FLT3 Inhibitors
FLT3-IN-32 is a highly selective, orally bioavailable inhibitor of the FLT3 receptor tyrosine kinase. It effectively targets FLT3-activating mutations, promoting apoptosis in malignant cells. In vivo studies demonstrate significant anti-tumor efficacy in MV4-11 xenograft models within NOD/SCID mice, leading to notable extensions in survival. FLT3-IN-32 is valuable for research applications focused on acute myeloid leukemia. -
FLT3 Inhibitor
HSB401 is an orally active FLT3 inhibitor with IC50 values of 28, 5, 72, and 51 nM for FLT3-WT, FLT3-D835Y, FLT3-ITD-F691L, and FLT3-ITD, respectively. It effectively downregulates FLT3 signaling, leading to cell cycle arrest and apoptosis in sensitive cells. Notably, HSB401 spares c-KIT inhibition, minimizing the risk of myelosuppression. This compound has demonstrated significant tumor growth suppression in the MV4-11 xenograft mouse model and is valuable for research in acute myeloid leukemia. -
FLT3 Inhibitor
SILA-123 is a potent FLT3 inhibitor, demonstrating IC50 values of 2.1 nM for FLT3-WT and 1.0 nM for FLT3-ITD. This compound effectively inhibits FLT3 phosphorylation and disrupts downstream signaling pathways, resulting in apoptosis through cell cycle arrest in the G0/G1 phase. SILA-123 is particularly valuable in research related to acute myeloid leukemia. -
FLT3 Inhibitor
JH-IX-179 is a potent FLT3 inhibitor with an IC50 of 4 nM for FLT3-ITD and 10 nM for FLT3-D835Y variants. This compound effectively induces cell cycle arrest in the G1 phase and promotes apoptosis in cells expressing the FLT3-ITD mutation. JH-IX-179 is primarily utilized in research focused on acute myeloid leukemia (AML), providing valuable insights into therapeutic strategies targeting FLT3 signaling pathways. -
FLT3/HDAC Inhibitor
HDAC-IN-63 is a dual inhibitor targeting both FLT3 and HDAC, with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1. It demonstrates potent inhibition of MV4-11 cell proliferation, with an IC50 of 92 nM, and effectively induces apoptosis while arresting the cell cycle in MV4-11 cells. This compound serves as a valuable research tool for the study of acute myeloid leukemia (AML) and the exploration of novel therapeutic strategies. -
FLT3 Inhibitor
FLT3-IN-31 is a potent inhibitor of FLT3, exhibiting IC50 values of 0.16 nM for the wild-type FLT3 receptor and 2.4 nM for the FLT3-D835Y mutant. It demonstrates significant antiproliferative activity by decreasing the protein expression of phosphorylated FLT3, STAT5, and ERK. Additionally, FLT3-IN-31 induces apoptosis and triggers cell cycle arrest at the G1 phase, making it a valuable tool for research in targeted cancer therapies and leukemia treatment. -
FLT3/HDAC Inhibitor
FLT3/HDAC-IN-3 is a dual inhibitor targeting FLT3 and HDAC, with a potent inhibitory effect on FLT3 (IC50 = 14 nM) and HDAC isoforms, including HDAC1 (IC50 = 27 nM) and HDAC6 (IC50 = 20 nM). This compound demonstrates selective inhibition, exhibiting reduced activity against HDAC8 and no activity toward HDAC4. FLT3/HDAC-IN-3 has shown anti-proliferative effects across various hematological malignancy cell lines and demonstrates efficacy in the Jeko-1 xenograft model without significant toxicity. It is suitable for research focused on hematological malignancies and the role of dual inhibition in therapeutic strategies. -
FLT3/JAK2 Inhibitor
JAK2/FLT3-IN-3 is a potent dual inhibitor of FLT3 and JAK2, exhibiting IC50 values of 2.01 nM for JAK2, 0.51 nM for FLT3, and 104.40 nM for JAK3. This compound induces apoptosis in cancer cells and demonstrates significant antitumor activity. Its ability to inhibit both FLT3 and JAK2 pathways makes it a valuable tool for research related to hematological malignancies and targeted cancer therapies. -
FLT3 Inhibitor
Tuspetinib dihydrochloride is a selective FLT3 inhibitor that demonstrates potent inhibitory activity with IC50 values of 1.1 nM for FLT3 WT, 1.8 nM for FLT3 ITD, and 1.0 nM for FLT3 D835Y kinases. As a reversible type I inhibitor, it effectively modulates downstream signaling pathways, including p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib dihydrochloride is utilized in research for its ability to inhibit proliferation and induce apoptosis in leukemic cells, making it significant for studies on hematological malignancies. -
FLT3/MNK2 Inhibitor
K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2, demonstrating IC50 values of 680 nM and 406 nM, respectively. This compound effectively inhibits the growth of acute myeloid leukemia (AML) cell lines, MOLM-13 and MV-4-11, with IC50 values of 10.5 µM and 10.4 µM. Additionally, K783-0308 promotes apoptosis and induces cell cycle arrest in the G0/G1 phase, making it a valuable tool for research into AML and related pathways. -
FLT3-ITD Inhibitor
FLT3-ITD-IN-3 is a potent inhibitor of FLT3-ITD (FLT3 internal tandem duplication), primarily targeting the FLT3 signaling pathway. This compound effectively disrupts FLT3 signal transduction, leading to G0/G1 cell cycle arrest and the induction of apoptosis in malignant cells. FLT3-ITD-IN-3 is valuable for research applications focused on acute myeloid leukemia (AML) and related hematological disorders. -
FLT3 Inhibitor
FLT3-IN-33 is a potent FLT3 inhibitor with an IC50 value of 7.82 nM, demonstrating significant anti-cancer activities, particularly against acute myeloid leukemia (AML) cell lines such as MV4-11 and MOLM-13. This compound effectively induces apoptosis in cancer cells and inhibits the phosphorylation of FLT3 signaling pathways. FLT3-IN-33 is suitable for research applications targeting AML and other malignancies, providing valuable insights into therapeutic strategies and cellular responses. -
RTK inhibitor
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively. -
Syk Inhibitor
R406 is an orally available spleen tyrosine kinase inhibitor with an IC50 of 41 nM. -
FLT3 Inhibitor
Tandutinib (MLN518) inhibits the autophosphorylation of FLT3, c-KIT and PDGF receptor tyrosine kinases, thereby inhibiting cellular proliferation and inducing apoptosis. -
JAK2/FLT3 inhibitor
TG-101348 is an orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 with potential antineoplastic activity. -
multi-targeted kinase inhibitor
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively. -
pan-PIM/FLT3 inhibitor
SEL24-B489 is a potent, type I, orally active dual inhibitor of PIM kinases and FLT3-ITD. It exhibits high affinity for PIM family members, with Kd values of 2 nM for PIM1, 2 nM for PIM2, and 3 nM for PIM3, making it a promising candidate for targeted cancer therapy. -
IRAK4/FLT3 inhibitor
Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation. -
FLT3 inhibitor
5'-Fluoroindirubinoxime (5'-FIO, compound 13), an Indirubin derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
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FLT3 Inhibitor
AKN-028 is a potent inhibitor of FMS-like receptor tyrosine kinase 3 (FLT3), demonstrating an IC50 value of 6 nM and effectively inhibiting FLT3 autophosphorylation. This orally active compound elicits a dose-dependent cytotoxic effect, with a mean IC50 of 1 μM. AKN-028 promotes apoptosis through the activation of caspase 3, making it particularly relevant for research on acute myeloid leukemia (AML) and related hematological malignancies. -
FLT3 Inhibitor
AKN-028 TFA is a potent and orally active inhibitor of FMS-like receptor tyrosine kinase 3 (FLT3), exhibiting an IC50 value of 6 nM. This compound effectively inhibits FLT3 autophosphorylation and elicits a dose-dependent cytotoxic response with a mean IC50 of 1 μM. Additionally, AKN-028 TFA induces apoptosis through the activation of caspase 3. It is a valuable tool for research in acute myeloid leukemia (AML). -
JAK2/FLT3 Inhibitor
Flonoltinib sulfate is a potent, orally active dual inhibitor targeting JAK2 and FLT3. It demonstrates significant biological activity with IC50 values of 0.7 nM for JAK2 and 4 nM for FLT3, along with activity against JAK1 and JAK3 at 26 nM and 39 nM, respectively. This compound is primarily utilized in cancer research, particularly in the study of hematological malignancies influenced by aberrant JAK2 and FLT3 signaling pathways. -
FLT3 Inhibitor
Tuspetinib hydrate is a selective FLT3 inhibitor that demonstrates IC50 values of 1.1 nM, 1.8 nM, and 1.0 nM against FLT3 wild-type, FLT3 internal tandem duplication (ITD), and FLT3 D835Y kinases, respectively. As a reversible type I inhibitor, Tuspetinib hydrate effectively modulates key signaling pathways, including p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. This compound exhibits potent anti-leukemic activity by inhibiting cell proliferation and inducing apoptosis in leukemic cells, making it a valuable tool for research in leukemia and related hematological malignancies. -
FLT3 Inhibitor
HI042 is a selective inhibitor of FMS-like Tyrosine Kinase 3 (FLT3), demonstrating potent activity with IC50 values of 0.62 μM in MOLM-13, 0.33 μM in MV4-11, and 0.89 μM in OCI-AML3 cell lines. This compound effectively reduces the viability of FLT3-internal tandem duplication (FLT3-ITD) mutation-positive cells, induces apoptosis, disrupts cell cycle progression, and diminishes clonogenic potential. HI042 serves as a valuable reagent in the research of acute myeloid leukemia (AML). -
Menin-KMT2A inhibitor
Bleximenib (JNJ-75276617) is an orally active and highly selective menin–KMT2A (MLL) interaction inhibitor, with IC50 values of 0.1 nM in humans, 0.045 nM in mice, and ≤0.066 nM in dogs. It effectively inhibits the proliferation of tumor cells and induces apoptosis and differentiation, particularly in malignancies driven by KMT2A rearrangements. Bleximenib is a promising therapeutic candidate for the study and treatment of leukemia and other menin-dependent cancers. -
Menin-KMT2A inhibitor
Bleximenib (JNJ-75276617) oxalate is an orally active and highly selective inhibitor of the menin–KMT2A (MLL) interaction, with IC50 values of 0.1 nM in humans, 0.045 nM in mice, and ≤0.066 nM in dogs. It effectively inhibits tumor cell proliferation and induces apoptosis and differentiation, particularly in cancers driven by KMT2A rearrangements. Bleximenib oxalate is a promising candidate for research in leukemia and other menin–KMT2A-dependent malignancies. -
JAK2/FLT3 inhibitor
Flonoltinib is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM for JAK2, 4 nM for FLT3, 26 nM for JAK1, and 39 nM for JAK3. It exhibits strong anti-cancer activity and is a promising candidate for the treatment of hematologic malignancies and other JAK/FLT3-driven cancers. -
FLT3/CHK2 inhibitor
Lasmotinib (PHI-101) is a dual inhibitor of FLT3 and CHK2 with potent activity against FLT3 single activating mutations (ITD or TKD), as well as double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. It synergizes with Venetoclax or Azacytidine to enhance anti-leukemic effects and also demonstrates anticancer activity in ovarian and breast cancer models. -
FLT3 Inhibitor
FLT3-IN-32 hydrochloride is a potent and orally bioavailable inhibitor of FLT3, demonstrating IC50 values of 0.29 nM, 0.77 nM, and 2.07 nM against the FLT3-ITD, FLT3-D835Y, and FLT3-N676K mutations, respectively. This compound effectively reduces FLT3 phosphorylation and inhibits downstream signaling pathways such as STAT5, MAPK, and AKT, ultimately leading to apoptosis in FLT3-mutated Ba/F3 cells. Additionally, FLT3-IN-32 hydrochloride exhibits significant anti-tumor efficacy in the MV4-11 xenograft model, making it a valuable tool for investigations into acute myeloid leukemia (AML). -
FLT3 Inhibitor
FLT3-IN-34 is a selective FLT3 inhibitor, exhibiting an IC50 value of 1.4 nM. It effectively blocks FLT3 phosphorylation and disrupts downstream signaling pathways involving AKT and ERK1/2. FLT3-IN-34 induces a concentration-dependent G0/G1 phase arrest and promotes mild apoptosis in FLT3-ITD-positive MV4-11 cells, demonstrating potent anti-proliferative effects with IC50 values of 14.95 nM and 18.5 nM against MV4-11 and MOLM-13 cell lines, respectively. This compound is suitable for investigating FLT3-positive acute myeloid leukemia (AML) and understanding FLT3-related signaling mechanisms. -
FLT3-ITD Inhibitor
Clifutinib is a selective inhibitor of the FLT3-ITD mutation, exhibiting an IC50 of 15.1 nM. This compound demonstrates potent antiproliferative effects against FLT3-ITD acute myeloid leukemia (AML) cell lines, with IC50 values of 1.5 nM and 1.4 nM for MV-4-11 and MOLM-13, respectively. Clifutinib disrupts FLT3-ITD kinase activity, subsequently inhibiting downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways, leading to apoptosis in FLT3-ITD-positive AML cells. Additionally, it shows significant antitumor efficacy in mouse models bearing MV-4-11 or MOLM-13 xenografts, making it a valuable tool for investigating relapsed/refractory FLT3-ITD-positive AML. -
FLT3 Inhibitor
Dovitinib lactate hydrate is a multi-targeted tyrosine kinase inhibitor primarily targeting FLT3. It exhibits potent inhibitory activity with IC50 values of 1 nM for FLT3, making it a valuable tool for research in hematological malignancies. In addition to FLT3, it also inhibits c-Kit, FGFR1/3, VEGFR1/2/3, and PDGFRα/β, facilitating studies focused on various signaling pathways and cancer therapeutics. -
FLT3 Inhibitor
CHMFL-FLT3-122 is a selective FLT3 kinase inhibitor with an IC50 of 40 nM. It demonstrates significant selectivity for FLT3 over BTK and c-KIT, exhibiting IC50 values of 421 nM and 559 nM, respectively. This compound effectively induces apoptosis through cell cycle arrest in the G0/G1 phase, making it a valuable tool for research in hematological malignancies and targeted cancer therapies. -
FLT3 Inhibitor
Tandutinib hydrochloride is a potent and selective inhibitor of FLT3, with an IC50 of 0.22 μM. This compound also exhibits inhibitory activity against c-Kit and PDGFR, with IC50 values of 0.17 μM and 0.20 μM, respectively. Its primary applications include research in acute myelogenous leukemia (AML). Additionally, Tandutinib hydrochloride demonstrates the ability to cross the blood-brain barrier, making it a valuable tool in studying central nervous system involvement in malignancies. -
JAK2/FLT3 Inhibitor
Flonoltinib TFA is a potent and orally bioavailable inhibitor that targets both JAK2 and FLT3, exhibiting IC50 values of 0.7 nM and 4 nM, respectively, alongside 26 nM and 39 nM for JAK1 and JAK3. This compound possesses significant anti-cancer activity, making it a valuable tool for research in oncology and therapeutic development against malignancies driven by these pathways. Its dual inhibition profile highlights its potential in addressing cancers associated with aberrant JAK2 and FLT3 signaling. -
EGFR/FLT3/Abl Inhibitor
Ruserontinib is an orally active multikinase inhibitor targeting EGFR, FLT3, and Abl. With an IC50 of 55 nM for human FLT3, it demonstrates significant antitumor activity. This compound is primarily utilized in cancer research, particularly for studying the effects of inhibiting key kinases involved in tumor progression and survival. -
FLT3 Inhibitor
FLT3-IN-40 is a type I ATP-competitive inhibitor of FLT3, demonstrating an IC50 of 16.26 nM. This compound effectively reduces FLT3 autophosphorylation and downregulates ERK phosphorylation, thereby exhibiting significant antiproliferative activity, influencing cell cycle regulation, and promoting apoptosis. FLT3-IN-40 is particularly valuable for research applications focused on acute myeloid leukemia.

