Pro-Dasatinib (compound 2j), an amino acid analog of Dasatinib, is a potent Src/Abl kinase inhibitor. Pro-Dasatinib has antiproliferative activity against K652 leukemia cancer cells with an IC50 of 0.21 nM.

CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia.

cis-NVP-ADW742 (cis-ADW742) is a cis isomer of NVP-ADW742. NVP-ADW742 is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.

SKS-927 is a Src kinase inhibitor, with an IC50 value of 3.9 nM. SKS-927 inhibits the proliferation of Src-transformed rat fibroblasta, with an IC50 value of 73 nM. SKS-927 exhibits an IC50 value of 720 nM against EGFR. SKS-927 can be used for the study of cancer and osteoporosis.

Eratrectinib (Example 1) is a Trk inhibitor. Eratrectinib can be studied in research for tropomyosin receptor kinase-related diseases and cancers.

BMS-577098 is an orally active and ATP-competitive insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 0.016 μM. BMS-577098 shows anti-tumor effect.

Tuspetinib (HM43239) dihydrochloride is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib dihydrochloride inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib dihydrochloride inhibits the proliferation and induces the apoptosis of leukemic cells.

CGP-59326 (TRX-13) is a highly potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. CGP-59326 blocks the EGFR signaling pathwa, demonstrating highly selective inhibition of EGFR-dependent tumor cells. CGP-59326 is promising for research of cancers.

ODS-2004436 is a small molecule radiotracer that uses positron emission tomography (PET) imaging to measure the activity of the epidermal growth factor receptor (EGFR) in tumors. ODS-2004436 labeled with the radioactive isotope fluorine-18 shows significantly higher uptake in the xenograft models of lung cancer with EGFR mutations compared to the wild-type models, and could be used to distinguish the mutation status. ODS-2004436 can be used to identify EGFR-positive tumors and predict their response to certain reagent treatments, especially for non-small cell lung cancer (NSCLC).

N-Acetyl-O-phosphono-Tyr-Glu dipentylamide (Ac-Tyr-Glu-N(n-C5H11)2), a dipeptide, is a pp60c-src SH2 domain inhibitor. N-Acetyl-O-phosphono-Tyr-Glu dipentylamide can be used for cancer research.

MolPort-002-705-878 is a highly selective FMS-like tyrosine kinase 3 (FLT3) inhibitor with a binding affinity of −11.33 kcal/mol. MolPort-002-705-878 inhibits the proliferation of FLT3-mutated acute myeloid leukemia (AML) cells. MolPort-002-705-878 is promising for research of FLT3-mutated AML.

INCB126503 is an orally activeM, selective FGFR2/3 Inhibitor with IC50 values of 70 nM (FGFR1), 2.1 nM (FGFR2), 1.2 nM (FGFR3), 0.92 nM (FGFR3-V555L), 0.85 nM (FGFR3-V555M) and 64 nM (FGFR4). INCB126503 suppresses FGFR signaling in vivo without causing hyperphosphatemia and shows antitumor efficacy in xenograft models harboring FGFR3 genetic alterations.

Type II TRK inhibitor 3 (Compound 18d) is a Type II TRK inhibitor with IC50 values of 0.82, 1.82, and 0.12 nM for TRKAWT/G595R/G667C, respectively. Type II TRK inhibitor 3 exhibits antitumor activity.

AGW-11 is a potent dual inhibitor of EGFR (IC50 = 556 nM) and VEGFR2 (IC50 = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer.

Enozertinib (ORIC-114) hemihydrate is the inhibitor for EGFR that exhibits antineoplastic activity.

PF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active site cysteines in the ATP-binding pocket. PF-06658607 can be used to detect "off "-targets for covalent kinase inhibitors in cancer cells. The alkyne moiety allows for azide-based detection probe via copper-catalyzed click chemistry.

ISM7594 is an orally active FGFR2/3 inhibitor. ISM7594 shows broad-spectrum antiproliferative potency in FGFR2- or FGFR3-altered cancer cell panels, including FGFR2/3 amplification, fusion, and mutation (BaF3-TEL-FGFR2-V564F (IC50 = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC50 = 2 nM)) types. ISM7594 inhibits tumor growth in a dose-dependent manner. ISM7594 can be used for the study of advanced solid tumors with FGFR2/3 aberrations.

BMS-279700 is an orally active Src-family kinase p56Lck inhibitor. BMS-279700 can block the production of proinflammatory cytokines (IL-2 and TNFα). BMS-279700 can inhibit T cell proliferation. BMS-279700 can be used for the researches of inflammation and immunology.

TCB-32 (Compound I-1) is a FGFR1 agonist with an EC50 of 0.88  μM. TCB-32 significantly increases cell proliferation through activating FGFR1 signaling pathway as bFGF and its downstream ERK 1/2 with excellent thermal stability. TCB-32 can replace bFGF in serum-free cell culture media. TCB-32 can be used for tissue repair and wound healing related diseases like psoriasis and eczema research.

(Rac)-Ibrutinib alkyne (Compound 8) is a Btk inhibitor with an IC50 of 0.72 nM. (Rac)-Ibrutinib alkyne can effectively inhibit functions related to the B-cell receptor signaling pathway, with an IC50 of 9 nM for inhibiting Ca flux in Ramos cells. (Rac)-Ibrutinib alkyne can be used in the research of diseases such as rheumatoid arthritis.

Umedaptanib pegol is an anti-fibroblast growth factor-2 (FGF2) aptamer. It is used for the study of neovascular age-related macular degeneration (nAMD).

Umedaptanib pegol sodium is an anti-fibroblast growth factor-2 (FGF2) aptamer. It is used for the study of neovascular age-related macular degeneration (nAMD).

Pegpleranib is a pegylated DNA aptamer that selectively binds to PDGF-BB and PDGF-AB homodimers and heterodimers, interrupting the interaction with their associated tyrosine kinase receptors.

Pegpleranib sodium is a pegylated DNA aptamer that selectively binds to PDGF-BB and PDGF-AB homodimers and heterodimers, interrupting the interaction with their associated tyrosine kinase receptors.

N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.

KRCT-6j is a potent and selective TYRO3 inhibitor, 300-fold selectivity for TYRO3 over both AXL and MerTK.KRCT-6j selectively inhibited the proliferation of TYRO3-overexpressing Ba/F3 cells, also suppressed csEV-stimulated cell migration of LNCaP-SL cells in a concentration-dependent manner.KRCT-6j diminished csEV-induced membrane localization of F-actin, reversed the increased expression and nuclear localization of YAP stimulated by csEVs.KRCT-6j significantly inhibited tumor growth in xenografts implanted with GR-H1993 cells when combined with gefitinib.

AC3573 (AC-3573) is a potent, specific small molecule inhibitor of HER3.AC3573 abrogates HER2–HER3 signalling in cells and is more specific for HER3, inhibits NRG (heregulin)-induced HER3 phosphorylation with IC50 of 10 uM, abrogates the formation of the active HER2-HER3 heterodimer, inhibits oncogenic downstream signalling in SK-BR-3 breast cancer cells.

Lenvatinib N-Oxide (Lenvatinib impurity 10) is the impurity of Lenvatinib. DCG04 is a multivalent ligand for the mannose-6-phosphate receptor. DCG-04 is an activity-based probe for cysteine cathepsins, and can be used for labelling numerous cysteine cathepsins in cell and tissue lysates.

(Z)-SU14813 is an analog of SU14813. CAY10568 is physically smaller and less hydrophobic than the QX-314. CAY10568 can be used in studies of inflammation and pain perception.

VMD-928 is an orally active, allosteric, irreversible and selective tropomyosin receptor kinase A (TrkA) inhibitor. VMD-928 blocks the downstream signaling pathways triggered by the binding of nerve growth factor (NGF) to TrkA, thereby inhibiting cell proliferation, invasion, and promoting cancer cell death. VMD-928 is promising for research of various cancers, including prostate cancer, thymic carcinoma, mesothelioma, squamous cell carcinoma of the head and neck, squamous cell carcinoma of the lung, ovarian cancer, hepatocellular carcinoma.