tumor xenograft model

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

Osimertinib mesylate (AZD-9291 mesylate) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib mesylate has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

RLY-2608 is a small molecule inhibitor, a selective allosteric PI3Kα inhibitor with high selectivity for PIK3CA mutations. This compound effectively inhibits tumor growth in PIK3CA-mutant xenograft models and is primarily used for research on PIK3CA-driven cancers.

M3258 is an immunoproteasome subunit LMP7 (β5i) inhibitor, with an IC50 of 3.6 nM for LMP7 and 3.4 nM at the cellular level. In a multiple myeloma xenograft model, M3258 exhibits significant antitumor activity. In multiple myeloma cells, M3258 significantly and persistently inhibits LMP7 activity and ubiquitinated protein turnover in tumor tissues, further inducing apoptosis.

GW 583340 dihydrochloride is a potent and orally available dual EGFR/ErbB2 (epidermal growth factor receptor/tyrosine kinase) inhibitor and is capable of reversing ABCG2- and ABCB1-mediated resistance.GW 583340 dihydrochloride selectively inhibits the growth of human tumor cells overexpressing EGFR and ErbB2, selectively inhibits the growth of human tumor cells overexpressing EGFR and ErbB2, and inhibits 80% of tumor growth in a mouse xenograft model, with potential anticancer activity.

YPC-22026 has potential anticancer activity, inducing tumor regression in a mouse xenograft model while inhibiting ZNF143-regulated genes.

FA16 is a selective, metabolically stable ferroptosis inducer with an IC50 value of 1.26 μM.FA16 is a derivative of 2-(trifluoromethyl)benzimidazole.FA16 inhibits the cystine/glutamate inverse transporter protein (system Xc-)-mediated exchange of intracellular glutamate for extracellular cystine.FA16 significantly inhibited tumor growth in a HepG2 xenograft tumor model. HepG2 xenograft tumor model significantly inhibited tumor growth.

CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.

JI130 is able to impair the ability of Hes1 to repress transcription. JI130 treatment significantly reduced tumor volume in a murine pancreatic tumor xenograft model.

OPN-9652 is a potent and orally active covalent TEAD inhibitor, with a half-maximal inhibitory concentration (IC50) of 0.005 µM against TEAD in MSTO-211H cells, and it targets the central palmitate-binding pocket of TEAD. OPN-9652 can significantly reduce the activity of TEAD-dependent reporter genes and downregulate the expression levels of TEAD target genes (CTGF and CYR61). Notably, OPN-9652 can reverse the resistance of SOX10 knockout (SOX10 KO) resistant cells to the combination of BRAF inhibitor (BRAFi) and MAPK inhibitor (MAPKi), restoring their sensitivity to the drugs. In the xenograft mouse model of BRAF-mutant A375 cells, OPN-9652 can effectively delay the development of tumor drug resistance; specifically, this effect is manifested by a significant delay in the onset of tumor drug resistance after the combination of BRAFi and MEK inhibitor (MEKi) starting from the minimal residual disease (MRD) stage. At present, OPN-9652 can be used as a research tool for scientific research related to melanoma.

LY2457546 is a highly potent, orally bioavailable multi-target anti-angiogenic tyrosine kinase inhibitor. It shows strong inhibitory activity against multiple targets including VEGFR2, PDGFRβ, FLT-3, Tie-2, and Eph family receptors, and is applied in cancer research such as leukemia.

FJ9 is an effective Wnt/β-catenin antagonist (Ki = 29 μM) that downregulates canonical Wnt signaling, inhibits HSC (hepatic stellate cell) activation, and reduces MeCP2 protein levels. FJ9 also disrupts the protein-protein interaction between Frz7 and the DVL PDZ domain, induces apoptosis in human cancer cell lines, and inhibits tumor growth in a mouse xenograft model.

Cirsiliol is a 5-lipoxygenase (5-LOX) inhibitor and low affinity benzodiazepine receptor ligand.Cirsiliol inhibits cell proliferation and promotes apoptosis of OS cells.Cirsiliol shows antitumor activity against OS cells in an in situ xenograft tumor model and can be used to study colon cancer.

Ganodermanontriol is a purified triterpene extracted from GL that inhibits proliferation of HCT-116 and HT-29 colon cancer cells without significantly compromising cell viability and suppresses β-catenin transcriptional activity and cyclin D1 protein levels in a dose-dependent manner. Ganodermanontriol also reduces Cdk-4 and PCNA while increasing E-cadherin and β-catenin accumulation in HT-29 cells, Ganodermanontriol markedly suppresses tumor growth in an HT-29 xenograft mouse model without adverse effects, highlighting its strong potential as a chemotherapeutic candidate for colorectal cancer research.

MYCMI-6 (NSC-354961) is a potent and selective inhibitor of endogenous MYC:MAX protein interactions,reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without severe side effects.

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks (Kis of 4 nM, 6 nM, 2 nM, and 1 nM for PI3Kα, β, δ, and γ, respectively), exhibiting anti-tumor activity in a mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K signaling as indicated by a decrease in p-Akt (Ser473).

JND4135, a type II TRK inhibitor, exhibits IC50 values targeting TRKA, TRKB, and TRKC at 2.79, 3.19, and 3.01 nM, respectively. It can overcome resistance due to TRKxDFG and other mutations in the BaF3 stable model, inhibiting the phosphorylation of TRKs WT, xDFG mutations, and their downstream signaling molecules. Additionally, JND4135 induces G0/G1 phase arrest and cell apoptosis (apoptosis) in BaF3–CD74-TRKA-G667C cells. This compound also demonstrates antitumor activity in a BaF3-CD74-TRKA-G667C mouse xenograft model by suppressing tumor growth.

CDK/HDAC-IN-4 is a highly selective dual inhibitor of cyclin-dependent kinase (CDK) and histone deacetylase (HDAC), with IC50 values of 88.4 nM and 168.9 nM, respectively. This compound exhibits antiproliferative effects in both hematologic and solid tumor cells. Additionally, CDK/HDAC-IN-4 induces apoptosis and S-phase cell cycle arrest in MV-4-11 cells. It has also demonstrated significant antitumor efficacy in an MV-4-11 xenograft model.

W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity and an IC50 of 17 nM. It exhibits antiproliferative activity, with an IC50 of 230 nM against RS411 cells, and significantly inhibits tumor growth in an RS411 tumor xenograft model. Pharmacokinetic analysis in mice shows that W4275 has a favorable oral bioavailability (F is 27.34%). W4275 holds potential for use in cancer research.

FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanisms in hepatocellular carcinoma cells. This leads to T-loop defects, inducing telomere shortening and cellular senescence. Additionally, FKB04 inhibits tumor growth in a human liver cancer xenograft mouse model (by implanting Huh-7 cells in BALB/c mice). This compound is utilized in research focused on liver cancer.

ML234 is a dual inhibitor targeting EZH2/LSD1, with IC50 values of 0.09 and 0.12 μM, respectively. It demonstrates strong antiproliferative effects on prostate cancer cell lines LNCAP, PC3, and 22RV1. Additionally, ML234 inhibits tumor growth in a 22RV1 xenograft mouse model, showing potential as a research agent in prostate cancer therapeutics.

AZ 14145845, a potent and highly selective dual Mer/Axl kinase inhibitor (pIC50 = 7 nM and 7.8 nM in pAxl and pMer, respectively), demonstrates significant efficacy in reducing tumor growth in a dose-dependent manner within the Mer and Axl kinase Ba/F3 tumor xenograft model in vivo. When combined with anti-PD1 antibodies and ionizing radiation, this compound enhances survival rates in mice bearing MC38-derived tumors. Additionally, AZ 14145845 is orally bioavailable.

Antiangiogenic agent 7 (Compound 1) induces apoptosis, elevates Reactive Oxygen Species (Reactive Oxygen Species), and inhibits the intracellular enzyme thioredoxin reductase. It exhibits anticancer activity with IC50 values ranging from 0.08 to 3.5 μM against cervical cancer cells (HeLa), prostate cancer cells (PC-3), and non-small cell lung cancer cells (A549). Additionally, Antiangiogenic agent 7 suppresses tumor growth in a mouse xenograft model.

Compound EF2 (Androgen receptor antagonist 12) is an orally active antagonist of the androgen receptor (AR) with an IC50 of 0.30 µM. It inhibits the transcriptional activity of mutant AR and the proliferation of AR-positive PCa (prostate cancer) cell lines. Additionally, Compound EF2 blocks the nuclear translocation of AR and suppresses tumor growth in the C4-2B xenograft mouse model. This compound is used for research in prostate cancer.