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Catalog No.
Product Name
Application
Product Information
Citations
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EGFR inhibitor
Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. -
EGFR Inhibitor
Gefitinib hydrochloride is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR. -
Lck Inhibitor
TC-S 7003 is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM. -
Lck inhibitor
Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively . -
ALK inhibitor
LDK378 dihydrochloride is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. -
MET inhibitor
LY2801653 dihydrochloride is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM). -
VEGFR/PDGFRβ/KIT inhibitor
N-desethyl sunitinib is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively). -
FGFR Inhibitor
NVP-BGJ398 phosphate is a novel selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively; >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes. -
c-Met Inhibitor
PF-04217903 methanesulfonate is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant). -
Tyrosine kinase inhibitor
Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. -
VEGFR Inhibitor
SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3). -
VEGFR2/Src kinase inhibitor
TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively. -
VEGFr2 inhibitor
TG 100801 is the prodrug of TG 100572, TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM or VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.
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c-Kit/VEGFR2/PDGFRβ inhibitor
Toceranib phosphate is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ. -
Tyrosine kinase inhibitor
Tyrosine-kinase inhibitor is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades. -
VEGFR/EGFR inhibitor
Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM. -
EGFR inhibitor
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. -
EGFR inhibitor
AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR). It binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. -
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.
