anti-tumour

Ifebemtinib (BI-853520) is an orally active and potent inhibitor of adhesion plaque kinase (FAK) (IC50=1 nM) with anti-tumour activity that inhibits globule formation and in situ tumour growth in malignant pleural mesotheliomas, and may be useful for the study of breast and ovarian cancer.

Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.

Glutathione arsenoxide hydrochloride (Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)) is a potentially active anti-cancer molecule and inhibitor of tumour metabolism. glutathione arsenoxide hydrochloride targets the mitochondrial inner membrane adenine nucleotidyl transferase (ANT), which inhibits cell proliferation and promotes apoptosis. Glutathione arsenoxide hydrochloride can be used to recognize cell surface proteins such as protein disulfide isomerases.

NM-3 is an orally available anti-angiogenic inhibitor with anti-tumour activity.NM-3 is used as a radiation modulator in vitro and in vivo.NM-3 inhibits vascular endothelial growth factor (VEGF), thereby inhibiting the proliferation of endothelial cells. This inhibits the proliferation of endothelial cells. NM-3 is associated with a mechanism of apoptosis induction by reactive oxygen species.

Esculetin (Cichorigenin) is a coumarin derivative from various natural plant products with various biological and pharmaceutical properties including anti-edema, anti-inflammatory and anti-tumour effects. It inhibits lipoxygenases (LOs).

(-)-α-Terpineol has antitumour, anti-inflammatory, and antimicrobial activities, it inhibits the growth of tumour cells through a mechanism that involves inhibition of the NF-kappaB pathway

Talmetacin has anti-inflammatory and analgesic and anti-tumour activity and can be used to study cardiovascular disease.

(S)-OSMI 3 (Ent-OSMI-3) has anti-inflammatory and anti-tumour activity and can be used to study diabetes and neurodegenerative diseases.

Erbulozole (R 55104) is a potent synthetic microtubule inhibitor with anti-invasive, anti-tumor, and radiosensitizing activities that induces Wernicke's encephalopathy-like neurotoxicity.

Poloxin-2 is a potent and selective Plk1 PBD inhibitor with anti-tumour activity that reduces the protein level of Plk1 in HeLa cells.

Tafetinib (SIM-010603) is a novel potent and orally available tyrosine kinase inhibitor with anti-angiogenic and anti-tumour activity.

TNKS-2-IN-2 is a novel and potent TNKS2 selective inhibitor (IC50: 22 nM) with potential anti-tumour activity for studying colon cancer, lung cancer, and breast cancer.

Dihydromollugin is a naphthol ester found in Rubia cordifolia that may have anti-tumour, virus-inhibiting and other activities.

DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with anti-tumor activity, which also inhibits EGFR and HER2, and is useful for studying pancreatic cancer.

BMS-960 is an S1P agonist with potential anti-tumour activity for cancer research.

ALK ROS1 inhibitor 2e HCL possesses anti-apoptotic, anti-proliferative and anti-tumour activities.

Ensituximab (NEO-102) is a quasi-selective IgG1 monoclonal antibody against the MUC5AC variant with anti-tumour activity that inhibits colorectal and pancreatic cancer.

A-176120 is a potent farnesyl pyrophosphate (FPP) analogues, it selectively inhibits farnesyltransferase. It has anti-angiogenic potential and may reduce H-ras NIH3T3 tumour growth.

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5 nM for TRKA, 0.7 nM for TRKB, and 2.6 nM for TRKC. The compound demonstrates good selectivity within the kinase group and exhibits significant anti-tumor efficacy in vivo.

IMT1B (LDC203974) is an orally administered, specific noncompetitive allosteric inhibitor of mitochondrial RNA polymerase (POLRMT), effectively suppressing mitochondrial DNA (mtDNA) expression and conferring anti-tumor properties.

RX-3117 (fluorocyclopentenylcytosine) is a novel a cytidine analog. RX-3117 displays anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.

Mavacoxib is a selective inhibitor of cyclooxygenase-2 (COX-2) ,with Anti-Tumour activity.

9-Methoxycanthin-6-one has anti-tumour activity, exhibits cytotoxic activity towards KB, LU-1, LNCaP, HL-60 cancer cells and other human cancer cell lines with IC50 values around 1-4 μg mL.

PAK4-IN-1 is a selective, potent, orally active PAK4 inhibitor that is stable under both acidic and neutral conditions.PAK4-IN-1 exhibits good anti-tumour effects in vivo.

EGFR/HER2-IN-5 is an irreversible, orally active dual inhibitor of EGFR activity (IC50: 0.6 nM). EGFR/HER2-IN-4 shows potent EGFR kinase inhibitory activity against L858R and T790M mutations. EGFR/HER2-IN-4 exhibits significant anti-tumour effects in vivo and can be used to study lung cancer.

Anticancer agent 49 (compound 69) is a broad-spectrum anticancer agent with anti-proliferative activity. Anticancer agent 48 inhibits microtubule protein aggregation and has in vivo antitumour activity, with potential for studies on solid tumours and haematological tumours.

A2AAR HDAC-IN-2 is a potent dual A2AAR HDAC inhibitor with good affinity for A2AAR (Ki: 10.3 nM) and effective HDAC1 inhibition (IC50: 18.5 nM). A2AAR HDAC-IN-2 is applicable in anti-tumour studies.

TGFβRI-IN-6 is a potent TGFβRI inhibitor with an IC50 value of 0.55 nM.TGFβRI-IN-6 has the potential to enhance anti-tumour immunity.

(Rac)-Tanomastat ((Rac)-BAY 12-9566) is a racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally active zinc carboxy-containing inhibitor of non-peptide biphenyl matrix metalloproteinases (MMPs) and inhibits MMP-2 (Ki: 11 nM), MMP-3 (Ki: 143 nM), MMP-9 (Ki: 301 nM), and MMP-13 (Ki: 1470 nM). In several experimental tumor models, Tanomastat exhibits anti-invasive and anti-metastatic effects.

TH-6 is a potent inhibitor of HDAC, acting on HDAC1 (IC50: 0.115 μM), HDAC2 (IC50: 0.135 μM), HDAC3 (IC50: 0.242 μM), HDAC6 (IC50: 0.138 μM), HDAC8 (IC50: 2.120 μM). TH-6 inhibits cell migration and invasion and exhibits anti-tumour effects.

Antiproliferative agent-4 showed good anti-proliferative effects on some cancer cells. antiproliferative agent-4 inhibited tumour growth in nude mice and showed low toxicity. antiproliferative agent-4 reduced the mitochondrial membrane potential of EC109 cells and increased Antiproliferative agent-4 reduced the mitochondrial membrane potential of EC109 cells and increased the apoptosis rate and ROS level.

Regorafenib (BAY 73-4506) mesylate is an orally active multi-target receptor tyrosine kinase inhibitor, inhibiting VEGFR1 2 3 (IC50=13 4.2 46 nM), PDGFRβ (IC50: 22 nM), Kit (IC50: 7 nM), RET (IC50: 1.5 nM), and Raf-1 (IC50: 2.5 nM), with potent anti-tumor and anti-angiogenic effects.

CDK8-IN-13 is a CDK8 inhibitor (IC50: 51.9 nM) with potent, selective and oral activity. CDK8-IN-13 induces apoptosis and reduces the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 exhibits anti-tumour activity.

Tubulin polymerization-IN-9, a potent inhibitor of tubulin (IC50: 1.82 μM), arrests the cell cycle of K562 cells in the G2 M phase, induces apoptosis and mitochondrial depolarization, and exhibits strong anti-vascular and anti-tumor effects.

HDAC-IN-31 is a selective, potent, orally active HDAC inhibitor that acts on HDAC1 (IC50: 84.90 nM), HDAC2 (IC50: 168.0 nM), HDAC3 (IC50: 442.7 nM), HDAC8 (IC50>10000 nM). HDAC-IN-31 has good anti-tumour effects. HDAC-IN-31 has shown potential research value in diffuse large B-cell lymphoma.

Quinovic acid shows some anti-tumour activities, quinovic acid glycosides have a potent inhibitory effect on the growth of human bladder cancer cell lines by inducing apoptosis through modulation of NF-κB.

Echitamine chloride possesses anti-tumour activity in-vitro and in-vivo.

BTK-IN-15 is a novel, orally active Bruton's tyrosine kinase (BTK) inhibitor that inhibits BTK (IC50: 0.7 nM). BTK-IN-15 induces apoptosis in cancer cells and has good kinase selectivity and anti-tumour activity.

c-Met-IN-12 is a selective, orally active type II c-Met kinase inhibitor (IC50: 10.6 nM). c-Met-IN-12 is a high inhibitor of AXL, Mer and TYRO3 kinases (>80% inhibition at 1 μM). c-Met-IN-12 can be used as a scaffold to further enhance kinase selectivity. c-Met-IN-12 exhibits anti-tumour activity.

CSF1R-IN-3 is an orally effective CSF-1R inhibitor with an IC50 value of 2.1 nM. CSF1R-IN-3 has anti-proliferative activity against colorectal cancer cells. CSF1R-IN-3 exhibits anti-tumour effects and immune enhancing effects by inhibiting the migration of macrophages and inducing the reprogramming of M2-type macrophages to M1-type macrophages, thus exhibited activity against colorectal cancer cells.

PDGFR-IN-1 (compound 7m) is an orally active PDGFR (platelet-derived growth factor receptor) inhibitor that targets PDGFRα (IC50: 2.4 nM) and PDGFRβ (IC50: 0.9 nM), exhibiting strong anti-tumor effects and low toxicity, making it suitable for osteosarcoma studies.

ABN401 is a potent, selective, ATP-competitive inhibitor of c-MET (IC50: 10 nM). ABN401 exhibits cytotoxicity against MET-loving cancer cells. c-MET phosphorylation in tumour tissues is inhibited by ABN401. ABN401 can be used in anti-cancer studies.

Antitumor agent-37 exhibits potent anti-proliferative and anti-metastatic effects. antitumor agent-37 induces severe DNA damage, leading to high expression of γ-H2AX and p53. antitumor agent-37 induces apoptosis by exploiting the mitochondrial apoptosis pathway Bcl-2/Bax/caspase3. Antitumor agent-37 inhibits PD-L1 expression, increases CD3+ and CD8+ T-infiltrating cells in tumour tissue and significantly improves the immune response.

pan-HER-IN-2 (Compound C6) is an orally active, reversible, broad-spectrum HER inhibitor that targets EGFR (IC50: 0.72 nM), HER4 (IC50: 2.0 nM), EGFRT790M (IC50: 8.2 nM), and L858R (IC50: 75.1 nM). pan-HER-IN-2 induces apoptosis and possesses anti-tumor effects.

VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent inhibitor of VEGFR-2 with an IC50 of 0.037 μM and demonstrates anti-tumor effects.

KRAS G12C inhibitor 44 is a potent, orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 exhibits anti-proliferative effects in MIA PaCA-2 (IC50: 0.016 μM), H358 cells (IC50: 0.028 μM). inhibitor 44 has anti-tumour activity in vivo.

CT1-3 is a potent anti-cancer agent. CT1-3 regulates the JNK/Bcl-2/Bax/XIAP pathway, which induces mitochondria-mediated apoptosis. CT1-3 regulates the E-cadherin/Snail axis to inhibit epithelial mesenchymal transition (EMT) potentials in human cancer cells (HCCs) and suppresses tumourigenesis. CT1-3 has anti-tumour effects in mouse models and does not show significant hepatotoxicity or nephrotoxicity.

Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, selective, orally active, ATP-competitive inhibitor of colony-stimulating factor 1 (CSF1R or M-CSFR) (IC50: 20 nM) and c-Kit (IC50: 10 nM), with 10-100 times greater selectivity for these targets compared to FLT3 (IC50: 160 nM), KDR (VEGFR2) (IC50: 350 nM), and LCK (IC50: 860 nM). Pexidartinib hydrochloride induces apoptosis and exhibits anti-tumor effects.