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Catalog No.
Product Name
Application
Product Information
Citations
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RAF/VEGFR Inhibitor
RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers. -
RAF/VEGFR Inhibitor
Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM. -
FLT3 Inhibitor
Tandutinib (MLN518) inhibits the autophosphorylation of FLT3, c-KIT and PDGF receptor tyrosine kinases, thereby inhibiting cellular proliferation and inducing apoptosis. -
p38 MAPK inhibitor
Pexmetinib is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (MAPK), and Tie2/Tek receptor tyrosine kinase. -
VEGFR-2 inhibitor
Telatinib (BAY 57-9352) is an orally available, small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β tyrosine kinases. -
Tie2 kinase inhibitor
Tie2 kinase inhibitor is a potent and selective Tie2 inhibitor with IC50 of 0.25 μM. -
HER2 Inhibitor
ARRY-380 is an ErbB-2 inhibitor that selectively binds to and inhibits the phosphorylation of ErbB-2, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. -
CDK Inhibitor
PHA-848125 (Milciclib) is an orally bioavailable inhibitor of CDKs and TRKA with potential antineoplastic activity. -
EGFR, HER2 and VEGFR inhibitor
XL647 is an orally bioavailable small-molecule RTK inhibitor that binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including EGFR, HER2, ERBB2, VEGFR and EphB4. -
JAK2/FLT3 inhibitor
TG-101348 is an orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 with potential antineoplastic activity. -
FGFR3 inhibitor
VSPPLTLGQLLS is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation. -
multi-kinase inhibitor
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl. -
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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VEGFR-2 Inhibitor
VEGFR-2-IN-39 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), with an IC50 of 208.6 nM. This compound effectively inhibits the proliferation of EA.hy926 cells, a human umbilical vein endothelial cell line, in a concentration-dependent manner, exhibiting an IC50 of 38.65 µM. VEGFR-2-IN-39 has low toxicity, making it suitable for further research applications in angiogenesis and vascular biology. -
EGFR Inhibitor
Cucurbitacin IIa is a potent EGFR inhibitor with an IC50 of 1.455 nM, demonstrating effective modulation of the EGFR signaling pathway. This compound induces caspase-3-dependent apoptosis, downregulates survivin expression, and enhances autophagy, while disrupting the actin cytoskeleton and arresting the cell cycle at the G2/M phase. Additionally, Cucurbitacin IIa exhibits anti-inflammatory properties, making it a valuable tool for research into inflammation-related diseases, depression, and various cancers, including non-small cell lung cancer. -
RIPK2/ALK2 Inhibitor
OD36 hydrochloride is a potent inhibitor of receptor-interacting protein kinase 2 (RIPK2) and an effective modulator of activin receptor-like kinase 2 (ALK2), exhibiting an IC50 of 5.3 nM against RIPK2. This macrocyclic compound demonstrates strong binding affinity for the ALK2 kinase ATP pocket, with a Kd of 37 nM. OD36 hydrochloride is suitable for research applications focused on signaling pathways involving RIPK2 and ALK2, relevant in studying various diseases, including inflammation and cancer. -
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. -
RIPK2/ALK2 Inhibitor
OD36 is a selective inhibitor of RIPK2 with an IC50 of 5.3 nM, demonstrating potent binding affinity to the ATP pocket of the ALK2 kinase, with a KD of 37 nM. This macrocyclic compound exhibits specific ALK2-directed activity, making it a valuable tool for investigating the roles of these kinases in various biological pathways. Research applications include the exploration of inflammatory signaling and potential therapeutic interventions in related diseases. -
RIPK2/ALK2 Inhibitor
RIPK2-IN-1 is a selective inhibitor targeting RIPK2 and ALK2, with an IC50 of 51 nM and 5 nM, respectively. This compound demonstrates substantial efficacy in modulating RIPK2/NOD2 pathways, exhibiting an IC50 of 390 nM in cellular assays. RIPK2-IN-1 is suitable for research applications investigating pathways related to inflammation and immune response mechanisms. -
ALKBH5 Inhibitor
ALKBH5-IN-5 is a selective inhibitor of ALKBH5 with an IC50 of 0.62 μM and a Kd of 804 nM. This compound disrupts the interaction between ALKBH5 and its substrates, m6A-RNA and 6mA-DNA, leading to enhanced differentiation and apoptosis in cancer cells, as well as G2-M phase arrest. Notably, ALKBH5-IN-5 reduces the protein levels of TACC3 and MYC while increasing cleaved caspase-3 levels, demonstrating significant antiproliferative effects. Furthermore, it exhibits antitumor activity in xenograft mouse models and is relevant for research into acute myeloid leukemia. -
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). -
DDR2 Inhibitor
CIDD-8633 is a potent inhibitor of DDR2, exhibiting an IC50 value of 6.105 μM. This compound effectively inhibits cell migration, induces cell cycle arrest, and promotes apoptosis, leading to significant suppression of pancreatic ductal adenocarcinoma (PDAC) tumor growth. CIDD-8633 is valuable for research applications focused on understanding and combating pancreatic cancer, particularly in the context of PDAC. -
ALK Inhibitor
ALK-IN-26 is a selective inhibitor of the anaplastic lymphoma kinase (ALK) with an IC50 value of 7.0 μM for ALK tyrosine kinase. This compound exhibits favorable pharmacokinetic properties and demonstrates permeability across the blood-brain barrier. ALK-IN-26 has been shown to induce apoptosis, autophagy, and necrosis, making it a valuable tool in the study of glioblastoma and related malignancies. -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib is a potent multi-targeted kinase inhibitor that primarily targets c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This orally active compound demonstrates significant antitumor activity in human gastric cancer cells and xenograft models. Famitinib also induces apoptosis, making it a valuable tool for research in cancer therapeutics and signaling pathways. -
c-MET Kinase Inhibitor
Capmatinib dihydrochloride hydrate is a potent, orally bioavailable inhibitor of c-Met kinase, exhibiting an IC50 value of 0.13 nM. This selective and ATP-competitive inhibitor disrupts the phosphorylation of c-MET and its downstream signaling pathways, including ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate demonstrates substantial antitumor activity by effectively inhibiting c-MET-dependent tumor cell proliferation, migration, and promoting apoptosis. Primarily metabolized by CYP3A4 and aldehyde oxidase, this compound is instrumental in cancer research focused on targeting c-Met-associated pathways. -
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. -
ALK/FAK/ROS1 Multikinase Inhibitor
APG-2449 is an orally active inhibitor targeting BCL-2 and multikinase pathways, specifically ALK, FAK, and ROS1. It demonstrates potent antitumor activity by reducing cell viability and enhancing apoptosis in acute myeloid leukemia cells in vitro. APG-2449 effectively decreases the activation of FAK and its downstream signaling effectors. This compound is suitable for research applications in various malignancies, including mesothelioma, non-small cell lung cancer, ovarian cancer, and other hematologic and solid tumors. -
Src Inhibitor
Peruvoside is a potent Src inhibitor that also targets PI3K, JNK, STAT, and EGFR pathways. This compound induces apoptosis and autophagy, demonstrating a broad spectrum of anticancer activity in various cancers, including breast, lung, liver, and leukemia. Additionally, Peruvoside exhibits significant antiviral activity against positive-sense RNA viruses and can sensitize Gefitinib-resistant tumor cells, such as A549, PC9/gef, and H1975, to Gefitinib treatment. -
ALKBH5 Inhibitor
W23-1006 is a selective and covalent inhibitor of ALKBH5, targeting the C200 residue with an IC50 of 3.848 μM. This compound exhibits approximately 30-fold and 8-fold greater inhibitory activity against ALKBH5 compared to FTO and ALKBH3, respectively. W23-1006 is particularly valuable for research applications focusing on triple-negative breast cancer (TNBC), enabling studies on the role of ALKBH5 in tumor biology and potential therapeutic strategies. -
c-MET Kinase Inhibitor
Capmatinib dihydrochloride is a selective, ATP-competitive inhibitor of the c-MET kinase, exhibiting an IC50 of 0.13 nM. This compound effectively inhibits the phosphorylation of c-MET and its downstream effector pathways, including ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride demonstrates potent antitumor activity by suppressing c-MET-dependent tumor cell proliferation and migration, while also inducing apoptosis. The drug undergoes significant metabolism via CYP3A4 and aldehyde oxidase, making it relevant for studies involving c-MET-driven malignancies. -
EGFR Inhibitor
EGFR-IN-86 is a potent EGFR inhibitor, exhibiting an IC50 of 1.5 nM. It demonstrates significant biological activity against glioblastoma by inducing apoptosis and causing cell cycle arrest in the G2/M phase in U87 cells. This compound serves as a valuable tool for research focused on targeting EGFR in cancer therapy. -
Src/Tubulin Inhibitor
KX2-361 is an inhibitor of Src-kinase and tubulin polymerization. This compound exhibits significant anti-tumor activity and induces apoptosis in glioblastoma (GBM) cells. With good oral bioavailability and the ability to cross the blood-brain barrier in murine models, KX2-361 is a valuable tool for investigating Src-related signaling pathways and therapeutic strategies in cancer research. -
ACK1 Inhibitor
(R)-9b is a potent inhibitor of ACK1 tyrosine kinase, exhibiting an IC50 value of 56 nM. This compound selectively targets ACK1 while also exhibiting inhibitory effects on JAK2 and Tyk2 kinases. (R)-9b is valuable for research into hormone-regulated cancers, including prostate and breast cancer, providing a tool for understanding ACK1's role in cancer progression and treatment. -
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. -
ITK/JAK3 Inhibitor
Modzatinib is a selective, covalent inhibitor targeting ITK and JAK3, demonstrating IC50 values of 8 nM and 23 nM, respectively. Its potent anti-inflammatory properties make it a valuable tool for research in autoimmune and inflammatory diseases, facilitating the exploration of therapeutic interventions in these areas. Researchers can leverage modzatinib to study the mechanistic roles of ITK and JAK3 in immune responses and disease pathology. -
IRAK4/IRAK1 Inhibitor
IRAK4 modulator-2 is a selective inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) and IRAK1, exhibiting IC50 values of 0.005 μM and 0.97 μM, respectively. This compound effectively disrupts IRAK-mediated signaling pathways, including JAK-STAT and NF-κB pathways, leading to a reduction in pro-inflammatory cytokine production, such as IL-1 and TNF. IRAK4 modulator-2 demonstrates potential for use in research focusing on autoimmune and inflammatory diseases, including rheumatoid arthritis, psoriasis, and inflammatory bowel disease. -
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.
