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 selective mutant PI3Kα inhibitor that inhibits tumor growth in a PIK3CA mutant xenograft model.

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.

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.

DSPE-PEG(2000)-biotin is a biotinylated and PEGylated form of 1,2-distearoyl-sn-glycerol-3-phosphoethanolamine. This compound is extensively used in both in vitro and in vivo for the delivery of small molecule liposomes, as well as for fluorescently labeling nanoparticle lipid carriers (NLCs). Additionally, DSPE-PEG(2000)-biotin is employed to form micelles and serves as a precursor for immobilizing liposomes, utilized in biolayer interferometry binding experiments. Liposomes containing DSPE-PEG(2000)-biotin, encapsulating doxorubicin and quercetin, exhibit cytotoxicity against MCF-7/adr multidrug-resistant breast cancer cells in vitro and slow tumor growth in the MCF-7/adr mouse xenograft model. Fluorescent labeling of NLCs containing DSPE-PEG(2000)-biotin has been successfully achieved using avidin conjugated with FITC-labeled biotin.

PTX80 is an antagonist of p62, with an IC50 value of 31.18 nM. It has been shown to reduce tumor volume in a HCT116 colorectal cancer mouse xenograft model.

(R)-SR-C-107 is an orally active inhibitor developed based on ENL (containing YEAST domain protein), designed to target acute myeloid leukemia (AML). The inhibitor has an IC50 of 40 nM and a KD of 144 nM for ENL. In a xenograft mouse model of AML, (R)-SR-C-107 demonstrated in vivo efficacy, achieving a tumor regression rate of 45% at a dosage of 200 mg/kg (PO; QD).

WRN inhibitor 14 (compound S35) is an orally administered WRN inhibitor with anticancer properties. It effectively suppresses tumor growth in the SW48 xenograft model in BALB/c nude mice.