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Catalog No.
Product Name
Application
Product Information
Citations
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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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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
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). -
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. -
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
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. -
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). -
FLT3 Inhibitor
Quizartinib dihydrochloride is a potent and selective second-generation type II FLT3 tyrosine kinase inhibitor. Demonstrating a Kd of 1.6 nM, it effectively inhibits autophosphorylation of both wild-type FLT3 and FLT3-ITD in MV4-11 cells, with IC50 values of 4.2 nM and 1.1 nM, respectively. This compound is also suitable for the development of PROTAC FLT3 degraders when linked to the VHL ligand, and it has been shown to induce apoptosis in target cells. -
Pan-FLT3/Pan-BTK Inhibitor
Luxeptinib is a first-in-class, non-covalent pan-FLT3 and pan-BTK inhibitor that exhibits potent oral activity. This compound effectively induces cell cycle arrest, apoptosis, or autophagy in acute myeloid leukemia cells, making it a significant tool for cancer research. Its dual-targeting mechanism positions Luxeptinib as a potential therapeutic candidate in the treatment of hematological malignancies. -
CDK2/JAK2/FLT3 Inhibitor
(E/Z)-Zotiraciclib hydrochloride is a potent inhibitor of CDK2, JAK2, and FLT3, exhibiting IC50 values of 13 nM, 73 nM, and 56 nM, respectively. This orally active compound demonstrates significant efficacy in inhibiting the proliferation of various cancer cell lines. It is a valuable tool for research into therapeutic strategies targeting cell cycle regulation and signal transduction pathways in cancer. -
CDK2/JAK2/FLT3 Inhibitor
(E/Z)-Zotiraciclib citrate is a potent inhibitor targeting CDK2, JAK2, and FLT3 kinases. This compound demonstrates significant biological activity in disrupting cell cycle progression and signaling pathways associated with cell proliferation and survival. It is utilized in cancer research applications, particularly for studies involving hematological malignancies and solid tumors where these kinases are dysregulated. -
JAK2/FLT3 Inhibitor
Pacritinib hydrochloride is a selective inhibitor targeting JAK2 and FLT3, demonstrating inhibitory potency against wild-type JAK2 (IC50=23 nM), the JAK2V617F mutant (IC50=19 nM), and FLT3 (IC50=22 nM) as well as the FLT3D835Y mutant (IC50=6 nM). This compound is primarily utilized in research related to acute myeloid leukemia (AML) and myelofibrosis (MF), making it a valuable tool for studying these hematological malignancies and the associated signaling pathways. -
JAK2/FLT3 Inhibitor
SB1578 is a selective inhibitor of JAK2 and FLT3, exhibiting IC50 values of 46 nM and 60 nM, respectively. This compound demonstrates high selectivity for other kinase targets, making it a valuable tool for research. SB1578 is particularly useful in studying non-oncological indications, such as rheumatoid arthritis, offering insights into potential therapeutic applications in inflammatory diseases. -
CDK2/JAK2/FLT3 Inhibitor
Zotiraciclib hydrochloride is a novel small molecule inhibitor targeting cyclin-dependent kinase 2 (CDK2), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase 3 (FLT3). This reagent demonstrates anti-tumor activity by downregulating the Myc oncogene through CDK9 inhibition, contributing to reduced tumor growth. Zotiraciclib hydrochloride is particularly relevant for research into cancers capable of crossing the blood-brain barrier, and elevated levels of the MCL-1 protein may indicate its potential as a prognostic marker and therapeutic target in cancer studies. -
FLT3 Inhibitor
JI6 is a potent and selective FLT3 inhibitor, exhibiting IC50 values of approximately 40 nM for FLT3-WT, 8 nM for FLT3-D835Y, and 4 nM for FLT3-D835H. Additionally, JI6 demonstrates inhibitory activity against JAK3 and c-Kit, with IC50 values of around 250 nM and 500 nM, respectively. This compound serves as a valuable tool for research applications focused on acute myeloid leukemia. -
BET/JAK2/FLT3 Inhibitor
SG3-179 is a selective inhibitor of BET bromodomain proteins, with additional activity against JAK2 and FLT3. This compound effectively reduces HOXB13 protein expression, demonstrating potential relevance in the study of multiple myeloma (MM1.S). SG3-179 is a valuable tool for research involving epigenetic regulation and signaling pathways associated with hematological malignancies. -
FLT3/FGFR Inhibitor
MAX-40279 is a dual inhibitor targeting FLT3 and FGFR kinases, exhibiting potent activity against both wild-type and FLT3 mutants, including FLT3D835Y. This compound effectively inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 is valuable for research applications in acute myelogenous leukemia (AML), particularly in studying resistance mechanisms to existing therapies. -
FLT3/FGFR Inhibitor
MAX-40279 hemiadipate is a dual inhibitor of FLT3 and FGFR kinases, exhibiting oral bioactivity. This compound effectively targets multiple FLT3 mutants, including FLT3D835Y, and has the potential to overcome resistance against existing treatments. Inhibition of NDRG1 phosphorylation at Ser330 and suppression of endothelial-to-mesenchymal transition (EndMT) further characterize its biological activity. MAX-40279 hemiadipate is a valuable tool for research into acute myelogenous leukemia (AML). -
FLT3/FGFR Inhibitor
MAX-40279 hydrochloride is a dual inhibitor targeting FLT3 and FGFR kinases. This compound demonstrates efficacy against FLT3 mutants, including FLT3D835Y, potentially overcoming resistance to existing therapies. MAX-40279 hydrochloride has been shown to inhibit NDRG1 phosphorylation at Ser330 and suppress endothelial-to-mesenchymal transition (EndMT). It is suited for research focused on acute myelogenous leukemia (AML) and related pathways. -
FLT3/FGFR Inhibitor
MAX-40279 hemifumarate is an orally active dual inhibitor of FLT3 and FGFR kinases, demonstrating efficacy against FLT3 mutant variants, including FLT3D835Y. This compound effectively inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hemifumarate is relevant for research in acute myelogenous leukemia (AML) and offers potential therapeutic insights into overcoming resistance associated with traditional FLT3 inhibitors. -
FLT3 Inhibitor
MZH29 is a potent inhibitor targeting FLT3, demonstrating significant activity against both wild-type and various mutant forms, including FLT3-ITD, FLT3-D835H/Y/V, and FLT3-K663Q. Notably, MZH29 effectively inhibits the FLT3-ITD/F691L mutation, a known drug resistance variant associated with AC220. This compound is valuable for research in the field of oncology, particularly for studies related to acute myeloid leukemia (AML). -
MER/FLT3 Inhibitor
UNC2025 hydrochloride is a potent ATP-competitive inhibitor targeting MER and FLT3, with IC50 values of 0.74 nM and 0.8 nM, respectively. It demonstrates over 45-fold selectivity for MERTK compared to Axl, exhibiting an IC50 of 122 nM and Ki of 13.3 nM. Its exceptional pharmacokinetic properties and ability to cross the blood-brain barrier make UNC2025 hydrochloride a valuable tool for investigating acute leukemia and related hematological conditions. -
CDK9/FLT3 Inhibitor
CDDD11-8 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9) and FLT3-ITD, exhibiting Ki values of 8 nM and 13 nM, respectively. This compound effectively reduces the proliferation of leukemia cell lines, particularly those associated with the FLT3-ITD mutation. CDDD11-8 serves as a valuable tool for research into targeted therapies for hematological malignancies, specifically in the study of cell cycle regulation and tyrosine kinase signaling pathways. -
FLT3 Inhibitor
FLT3-IN-17 is a potent FLT3 inhibitor, effectively targeting FLT3 mutants with an IC50 of less than 0.5 nM for the D835Y variant. Additionally, it exhibits inhibitory effects on focal adhesion kinase (FAK), with an IC50 value of 12 nM. This compound is valuable for research into cancer biology, particularly in the context of FLT3-driven malignancies and related pathways. -
FLT3/AURKA Inhibitor
BPR1K871 is a potent dual inhibitor targeting FLT3 and AURKA, with IC50 values of 19 nM and 22 nM, respectively. This compound demonstrates significant anti-cancer activity and is suitable for preclinical development in oncology research. Its selective inhibition of these kinases makes it a valuable tool for studying FLT3 and AURKA-related signaling pathways in cancer. -
FLT3 Inhibitor
3-Hydroxy Midostaurin is an effective inhibitor of FMS-like tyrosine kinase-3 (FLT3), demonstrating autophosphorylation inhibition with IC50 values of approximately 132 nM in culture medium and 9.8 μM in plasma. This compound serves as a metabolite of PKC412 and exhibits greater cytotoxicity, albeit with reduced selectivity compared to its parent compound. It is particularly relevant in research focusing on hematological malignancies and FLT3-related signaling pathways. -
FLT3 Inhibitor
FLT3-IN-6 is a potent and selective FLT3-ITD inhibitor, demonstrating an IC50 of 1.336 nM. This compound effectively inhibits the mutated form of FLT3, making it a valuable tool in the study of hematological malignancies. Its specificity allows for precise exploration of FLT3-related pathways and potential therapeutic applications in cancer research. -
Dual FLT3/CHK1 Inhibitor
FLT3/CHK1-IN-1 is a dual inhibitor targeting both FLT3 and CHK1, demonstrating significant selectivity for c-KIT over other kinases. With an IC50 value of 58.4 μM, it shows reduced affinity for the hERG channel, minimizing potential cardiac side effects. FLT3/CHK1-IN-1 has exhibited efficacy in inhibiting tumor growth in mouse xenotransplantation models with MV-4-11 cells, making it a valuable tool for cancer research and therapeutic development. -
ITD-FLT3 Inhibitor
GTP-14564 is a selective inhibitor of the internal tandem duplication (ITD) variant of the FLT3 receptor tyrosine kinase. This compound effectively suppresses ligand-dependent proliferation of Ba/F3 leukemia cells, providing a valuable tool for the investigation of FLT3-related hematological malignancies. Its specificity may facilitate studies focused on the molecular mechanisms underlying FLT3-driven oncogenesis and therapeutic responses in leukemia. -
FLT3 Inhibitor
OTS447 is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3), exhibiting an IC50 value of 21 nM. This compound is primarily utilized in research focused on hematological malignancies, particularly acute myeloid leukemia (AML), where aberrant FLT3 signaling is implicated. OTS447 serves as a valuable tool in studies investigating FLT3-related pathways and potential therapeutic strategies targeting FLT3 mutations. -
FLT3 Inhibitor
Crenolanib benzenesulfonate is a potent and selective inhibitor of FLT3, including both wild-type and mutant isoforms, as well as PDGFRα and PDGFRβ. With dissociation constants (Kd) of 0.74 nM for FLT3 and 2.1 nM/3.2 nM for PDGFRα/β, it exhibits strong biological activity. This compound is primarily utilized in research applications focused on hematological malignancies and other cancers driven by aberrant receptor tyrosine kinase signaling pathways. -
FLT3 Inhibitor
FLT3-IN-16 is a highly effective FLT3 inhibitor, exhibiting an IC50 value of 1.1 μM. This compound plays a critical role in the study of acute myeloid leukemia (AML), facilitating research into therapeutic strategies targeting FLT3 signaling pathways. FLT3-IN-16 is essential for investigating the molecular mechanisms underlying AML and evaluating the efficacy of FLT3-targeted treatments. -
FLT3 Inhibitor
FLT3-IN-10 is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3), a key regulator in hematopoiesis and a pivotal target in certain leukemias. This compound exhibits significant activity against FLT3-mutated acute myeloid leukemia (AML), making it a valuable tool for research into targeted therapies. Its application in preclinical studies can aid in the understanding of FLT3's role in oncogenesis and in evaluating potential therapeutic strategies for FLT3-driven malignancies. -
FLT3/CDK5 Inhibitor
AMG 925 (HCl) is a potent dual inhibitor targeting FLT3 and CDK5, demonstrating IC50 values of 2±1 nM and 3±1 nM, respectively. This compound exhibits selectivity for these kinases, making it a valuable tool for research into hematological malignancies and cancer progression. Its oral bioavailability further enhances its utility in preclinical studies investigating therapeutic interventions for FLT3-driven malignancies and CDK5-associated diseases. -
FLT3 Inhibitor
FLT3-IN-19 is a potent and selective inhibitor of the FLT3 receptor tyrosine kinase, exhibiting an IC50 of 0.213 nM. This compound is primarily utilized in the research of acute myeloid leukemia (AML), facilitating studies on FLT3-dependent signaling pathways and potential therapeutic interventions. Its high specificity makes it an invaluable tool for understanding the molecular mechanisms underlying FLT3-driven malignancies. -
FLT3/Haspin Inhibitor
HSK205 is a potent dual inhibitor of FLT3 and Haspin, exhibiting an IC50 of 0.187 nM for FLT3. This compound demonstrates significant antitumor activity, making it a valuable tool in cancer research. Its dual targeting provides insights into the therapeutic potential for FLT3-driven malignancies and the role of Haspin in cell cycle regulation. -
PDGFRα/FLT3 Inhibitor
PDGFRα/FLT3-ITD-IN-3 is a highly effective inhibitor of PDGFRα and FLT3, exhibiting IC50 values of 0.153 μM and 0.004 μM, respectively. This compound serves as a valuable tool in the investigation of acute myeloid leukemia and chronic eosinophilic leukemia. Its potent inhibitory activity against key receptors makes it a significant candidate for related biomedical research applications. -
FLT3-ITD Inhibitor
FLT3/ITD-IN-3 is a highly selective inhibitor targeting FLT3 internal tandem duplications (FLT3-ITD), demonstrating potent activity with IC50 values of 0.3 nM for FLT3D835Y, 0.4 nM for FLT3, and 0.9 nM for FLT3-ITD. This compound effectively inhibits FLT3 phosphorylation and exhibits significant antiproliferative effects against acute myeloid leukemia cell lines. It serves as a valuable tool in research aimed at understanding and developing therapies for FLT3-ITD associated malignancies.
