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.

IGFIIR aptamer sodium is an IGFIIR-specific aptamer that can be potentially used as a targeting ligand for the treatment and diagnosis of liver fibrosis.

MRC-G-001 is a Genipin derivative with an IC50 of 117 μM against A549 cancer cells. MRC-G-001 inhibits the phosphorylation of EGFR, JAK1, and STAT3, and modulates epithelial-mesenchymal transition (EMT)-related protein expression, thereby attenuating cell migration and invasion. MRC-G-001 induces cell cycle arrest and cell apoptosis. MRC-G-001 can be used for the study of cancers such as non-small-cell lung cancer.

Cibrigirsen is an antisense oligonucleotide targeted to the insulin-like growth factor I receptor(IGF-1R).

Cibrigirsen sodium is an antisense oligonucleotide targeted to the insulin-like growth factor I receptor(IGF-1R).

CD117/c-Kit aptamer sodium is a single-strand DNA aptamer specific for the biomarker CD117, which is highly expressed on acute myeloid leukemia (AML) cells.

ALN-3133 sodium is a siRNA that targets VEGF, and it is one of the siRNAs in ALN-VSP.ALN-VSP is a lipid nanoparticle formulation containing two siRNAs for kinesin spindle protein (KSP) and VEGF with potential antitumor activity.

AGN-745 is a chemically modified siRNA targeted to VEGFR-1. It is used for the study of Macular degeneration.

AGN-745 sodium is a chemically modified siRNA targeted to VEGFR-1. It is used for the study of Macular degeneration.

BIEGi-1 is a potent and selective binary inhibitor of EGFR that effectively blocks EGFR-catalyzed nucleotide exchange and disrupts the EGFR–Rheb interaction. It robustly inhibits both EGFR kinase activity and mTORC1 signaling in EGFR-mutant cancer cells. This compound exhibits significant anti-proliferative effects with an IC50 of 17 nM for PC9 and 20 nM for HCC827.

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.