Angiogenesi

Brivanib Alaninate (BMS-582664) is an alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic effect.

BIBF 1202 is a VEGFR2 kinase inhibitor (IC50 = 62 nM).

Naquotinib mesylate (ASP8273 (mesylate)) is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR

Canertinib dihydrochloride (PD-183805 dihydrochloride) is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and

BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR. It has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

<p>Applications 5-[(4-Hydroxyphenyl)methylene]-2,4-thiazolidinedione is a 5-Benzylidene-2,4-thiazolidenedione derivative designed as inhibitors of angiogenesis targeting VEGFR-2. Also, it is an intermediate used in the synthesis of MSDC 0602 (M755420), which is an analogue of thiazolidinediones, exhibits low affinity for binding and activation of peroxisome proliferator-activated receptor γ (PPARγ). Thiazolidinediones are effective insulin-sensitizing drugs for treating various metabolic and inflammatory diseases.<br>References Bhanushali, U., et al.: Bioorg. Chem., 67, 139-147 (2016); Chen, Z., et al.: J. Biol. Chem. 287, 23537 (2012); Fukunaga, T., et al.: J. Bone Miner. Res., 30, 508 (2015)<br></p>

Fidasimtamab, a recombinant human IgG1 bispecific antibody, targets both HER2 and PD-1, bridging T cells and tumor cells to modulate immune responses.

Anbenitamab (KN-026) is a bispecific HER2 antibody for metastatic breast cancer research, blocking HER2 pathways and mediating ADCC.

Fepixnebart is a humanized IgG4κ antibody that targets TGF-alpha (TGFA).

Solrikitug,Anti-CRLF2 humanized IgG1κ monoclonal antibody.

Tarcocimab (OG1953) is a humanized IgG1 monoclonal antibody targeting VEGFA, researched for RVO and wet AMD.

Zalutumumab is a high-affinity fully human monoclonal antibody ,the extracellular domain of the EGFR squamous cell carcinoma of the head and neck (SCCHN).

<p>Vanucizumab is a bispecific humanised monoclonal antibody that simultaneously inhibits the receptor interactions of VEGF-A and Angiopoietin-2 (Ang-2)</p>

Dilpacimab (ABT165) is a dual-variable antibody that targets DLL4 and VEGF pathways, showing potential in cancer research by blocking angiogenesis and Notch.

Ivonescimab (AK112) is a PD-1/VEGF bispecific antibody with cancer immunotherapy and anti-angiogenic effects, NSCLC).

Runimotamab, an IgG1-κ humanized chimeric antibody, targets CD3E and HER2 [1].

EGFRT790M/L858R-IN-8 (compound 9) is a potent inhibitor of EGFR, specifically targeting the EGFRT790M/L858R mutations with an IC50 of 56.8 μM. This compound does not show significant antiproliferative effects on cancer cell lines A549, A431, and NHI-H1975.

Anti-Mouse VEGFR-2 Antibody (DC101) is a rat-derived monoclonal antibody against mouse VEGFR2/KDR/Flk-1, serving as a mouse analogue of ramucirumab.

<p>Becotatug (JMT-101) is an IgG1 antibody that targets EGFR and can be conjugated to Afatinib and Osimertinib, functioning as a synthetic antibody-drug conjugate</p>

Zanidatamab (ZW25) is a bispecific, humanized monoclonal antibody that targets two distinct epitopes (ECD2 and ECD4) of the HER2 receptor, exhibiting anti-tumor

Elgemtumab (LJM716) is a fully humanised monoclonal antibody targeting HER3/ERBB3, acting as an antagonist to block HER3/Akt phosphorylation antitumour.

Bafisontamab (EMB-01) is a bispecific antibody that targets EGFR and cMET, displaying antitumor activity [1].

Tovetumab (MEDI-575) is an anti-PDGFRα mAb inhibiting its signaling, in trials for glioblastoma and NSCLC.

<p>Depatuxizumab is a humanised monoclonal antibody targeting EGFR with blood-brain barrier (BBB) permeability, inhibit tumor growth,GBM,SCCHN.</p>

Faricimab,Bispecific antibody targeting Ang-2/VEGF-A. Prevents retinal I/R injury. Improves vision in w-AMD, DME, RVO.

Ponezumab (PF-04360365), a humanized IgG2 antibody, lowers Aβ in the CNS & boosts mice memory. Used in Alzheimer's research.

Izalontamab (SI-B001) is a bispecific EGFR/HER3 monoclonal antibody that binds to both EGFR×EGFR homodimers and EGFR×HER3 heterodimers.

<p>Serclutamab, a humanized chimeric monoclonal antibody of the IgG1-κ isotype, selectively targets the epidermal growth factor receptor (EGFR).</p>

Futuximab is a chimeric monoclonal antibody targeting EGFR, commonly used in combination with zatuximab to form Sym004.

<p>Imgatuzumab (RG 7160) is a humanized anti-EGFR monoclonal antibody and immunomodulator for cancer research.</p>

Ibrutinib D5 is a deuterium-labeled Ibrutinib. Ibrutinib is an irreversible Btk inhibitor.

Dasatinib D8 is deuterium-labeled dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

Apatinib-d8 is a deuterated compound of Apatinib. Apatinib has a CAS number of 811803-05-1. Apatinib is an orally bioavailable and specific VEGFR2 inhibitor (IC50: 1 nM). In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.

(3S,4S)-Tofacitinib, a less active enantiomer of tofacitinib, is a Janus kinases inhibitor.

ALK5-IN-79 (compound 57), an ALK inhibitor, exhibits anticancer activity by inhibiting the TGF-β1/SMAD signaling pathway. It effectively reduces the production of extracellular matrix (ECM) and collagen deposition. Moreover, ALK5-IN-79 demonstrates satisfactory pharmacokinetic (PK) properties and favorable in vivo tolerance.

EGFR-IN-109 (compound 4), an EGFR inhibitor, displays IC 50 values of 25.8 nM for EGFR WT and 182.3 nM for EGFR T790M. This compound halts the growth of cancer cells at the G2/M phase and triggers both early and late apoptosis. It is applicable in cancer research [1].

ZM39923 is a JAK3 inhibitor (pIC50: 7.1). ZM39923 also effectively inhibits tissue transglutaminase (IC50: 10 nM).

HVH-2930 is an inhibitor of Heat Shock Protein 90 (HSP90). It suppresses the cell viability of BT474 (Trastuzumab sensitive) and JIMT-1 (Trastuzumab resistant) by downregulating HSP90 client proteins such as HER2, p-HER2, AKT, p-AKT, cyclin D1, and survivin, with IC50 values of 6.86 μM and 4.42 μM, respectively. Additionally, HVH-2930 demonstrates antitumor efficacy in a mouse model and exhibits favorable pharmacokinetic properties in vivo.

AD1058 is a selective ATR inhibitor that crosses the blood-brain barrier with in vivo anticancer activity, used in the study of brain and CNS metastasis.

MAPK-IN-2 (compound 3h) is an efficacious MAPK inhibitor with antineoplastic properties that significantly hinders proliferation across various cancer cell

Icotinib (Conmana) is an orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity.

<p>Erlotinib: reversible inhibitor binding to ATP site of epidermal growth factor receptor.</p>

ZM323881 hydrochloride (ZM 323881 HCl) is a potent and selective VEGFR2 inhibitor.

GZD856 formic inhibits PDGFRα/β (IC50: 68.6, 136.6 nM) & Bcr-Abl (IC50: 19.9, 15.4 nM), with antitumor properties.

Dovitinib dilactic acid: multitarget RTK inhibitor for FLT3/c-Kit (IC50=1-2 nM), FGFR1/3, VEGFR1-4 (IC50=8-13 nM), less effective on InsR, EGFR. Phase 4.

<p>IGF-1Rmodulator 1 (Example 5) is an IGF-1R modulator featuring an EC50 of 0.29 μM (FGFR1), 0.25 μM (IGF1R), 0.34 μM (TrkA), and 0.39 μM (TrkB). This compound is useful in research on diseases characterized by impaired signaling of neurotrophic and/or other trophic factors, such as Alzheimer's disease.</p>

EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutations, specifically targeting the tumor environment and inducing apoptosis in cancer cells. This compound effectively inhibits the proliferation of H1975, PC-9, and mutant EGFR cells including BaF3-EGFRL858R/T790M/C797S and BaF3–C797S/Del19/T790M, with IC50 values of 13 nM, 19 nM, 1.2 nM, and 1.3 nM respectively. Additionally, EGFR-IN-117 demonstrates anti-tumor activity in mouse models.

<p>Applications LB 42708 is a selective nonpeptidic Farnesyltransferase (FTase) inhibitor.LB42708 suppresses tumor growth and tumor angiogenesis in both xenograft tumor models of Ras-mutated HCT116 cells and its wild-type Caco-2 cells, indicating its potential application in the treatment of both Ras-mutated and wild type tumors.<br>References Kim, C., et. al.: Mol. Pharmacol., 78, 142 (2010)<br></p>

<p>Applications 2-Chloro-N-[4-(1-cyanocyclopentyl)phenyl]-3-pyridinecarboxamide is an intermediate Apatinib 25-N-Oxide (A726160), a metabolite of the antiangiogenic agent and selective VEGFR2 inhibitor Apatinib (A726150).<br></p>