antitumour

Camonsertib (RP-3500) is a selective, orally active ATR kinase inhibitor (ATRi) with an IC50: 1.00 nM in biochemical assays and exhibits potent antitumour effects. Camonsertib is 30 times more selective for ATR than mTOR (IC50: 120 nM) and is a more active inhibitor of ATM, DNA-PK and PI3Kα kinases. PK and PI3Kα kinases.

Trastuzumab deruxtecan (T-DXd) is an antibody-activated molecule coupling (ADC) with anticancer and antitumour activity.Trastuzumab deruxtecan has been shown to have an ameliorative effect in HER2-positive breast and gastric cancers.

4-Methoxycoumarine has antitumour effects.

BMS-906024 (Osugacestat) is an orally available and selective inhibitor of γ-secretase, a small molecule Notch inhibitor.BMS-906024 has broad-spectrum antitumour activity against a variety of human cancer xenografts.BMS-906024 prevents the activation of all four Notch receptors, and is active against Notch1, -2, -3 and -4 receptors. BMS-906024 prevents the activation of all four Notch receptors, with IC50s of 1.6, 0.7, 3.4 and 2.9 nM for Notch1, -2, -3 and -4 receptors, respectively.

CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

Clanfenur belongs to a new group of substituted benzoylphenylureas. The drug shows both in vitro and in vivo antitumour activity.

Ainsliadimer A, a sesquiterpene lactone dimer from Ainsliaea macrocephala, has antitumour activity and induces cell death in various cancer cells.

HFY-4A HCL is a novel HDAC inhibitor.HFY-4A HCL has antitumour activity and has shown antiproliferative activity in breast cancer cells.

ARTD10/PARP10-IN-1 is a potent PARP inhibitor of the mono-ADP ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly ADP-ribose polymerase-1 (ARTD1/PARP1), with potential anticancer and antitumour activity for the study of prostate and breast cancers.

Alethine (β-Alethine) is a small molecule compound with antitumour activity and is used to treat tumours and infections. The alethine-induced up-regulation of TNFα increases the cytotoxicity of T cells.

Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.

P22074 is a USP7 inhibitor. It is not an active antagonist like its halogenated related compounds. p22074 has antitumour activity.

Triumbelletin is a tricoumarin rhamnopyranoside obtained from Wikstroemia indica with antitumour activity for the study of tumours.

EGFR-IN-3 is an EGFR inhibitor with potential antitumour activity.EGFR-IN-3 inhibits EGFRwt-TK and induces apoptosis (cell death), which can cause cells to block in the G2/M phase.

FC-116 is a potent Tubulin inhibitor with antitumour activity and inhibits tumour growth in mice. FC-116 induces apoptosis in colorectal cancer (CRC) cells and promotes protein degradation.

Euxanthone (1,7-Dihydroxyxanthone), an xanthone derivative extracted from the roots of Polygala tenuifolia Willd, has antitumour, neuroprotective and vasorelaxant activities, and attenuates Aβ1-42-induced oxidative stress and apoptosis by inducing autophagy.SB-674042 is used for the treatment of depression.SB-674042 is used for the treatment of depression.SB-674043 is used for the treatment of depression.SB-674044 is used for the treatment of depression.SB-674045 is used for the treatment of depression. 2A (BU-1) cell differentiation.

β-catenin modulator IIa-661 is a small molecule inhibitor of the Wnt pathway with antitumour activity.

IDH2R140Q-IN-2 is an orally active and potent IDH2R140Q inhibitor with an IC50 of 29 nM.IDH2R140Q-IN-2 possesses potential antitumour activity, reducing D2HG production in TF-1 cell lines carrying the IDH2R140Q mutation (IC50 of 10 nM) and inhibiting tumour tissue D2HG levels.IDH2R140Q-IN-2 is suitable for the study of acute myeloid leukaemia (AML).

DUN73423 (RET-IN-21) is a potent tyrosine kinase (RET) inhibitor with antitumour activity for the study of cancer.

INCB3619 is a selective and potent inhibitor of ADAM with antitumour effects, inhibiting ADAM10, ADAM17, MMP12 and MMP15.

OTUB1/USP8-IN-1 HCL is a potent dual inhibitor of OTUB1 and USP8 with potential antitumour activity, inhibiting both OTUB1 and USP8. OTUB1/USP8-IN-1 may be used in the study of leukaemia.

(R)-BI-2852 can be used as (R)-5-isoindolin-1-one is used as an inhibitor of the RAS family of proteins and as a compound for the treatment and prevention of tumours. (R)-BI-2852 has Antiproliferative and antitumour agent activity.

CTP Synthetase-IN-1 is an orally active and potent cytidine 5'-triphosphate synthetase (CTPS) inhibitor with potential antitumour activity, shows anti-inflammatory activity in animal models of inflammation, inhibits human CTPS1 and human CTPS2, and can be used in studies of arthritis and rheumatoid arthritis.

Vamotinib (PF-114) is an orally active and specific tyrosine kinase inhibitor with antiproliferative and antitumour activity.Vamotinib inhibits the phosphorylation of BCR/ABL and BCR/ABL-T315I, which promotes apoptosis. Vamotinib is used to study drug-resistant Philadelphia chromosome-positive (Ph+) leukaemia and Alzheimer's disease.

HFY-4A is a novel HDAC inhibitor.HFY-4A has antitumour activity and has shown antiproliferative activity in breast cancer cells.

AC265347 is a potent calcium-sensitive receptor (CaSR) agonist and ago-PAM orthosteric modulator with antitumour activity that inhibits neuroblastoma tumour growth by inducing differentiation.AC265347 can be used to study neuroblastoma.

GPX4-IN-5 is a small molecule covalent GPX4 inhibitor (IC50: 0.12 μM) with antitumour activity.GPX4-IN-5 induces ferroptosis and can be used for the prevention and treatment of triple-negative breast cancer (TNBC).

XPW1 is a new potent and selective CDK9 inhibitor with antitumour activity that transcriptionally inhibits the DNA repair process in ccRCC cells.XPW1 can be used to study clear cell renal cell carcinoma.

Cyclo(D-Leu-L-Pro) shows antitumour and antifungal activities.

Pericosine A is a fungal metabolite that has been found inP. byssoidesand has anticancer activity.1It inhibits the growth of a variety of cancer cells, including breast, colon, lung, ovary, stomach, and prostate cell lines (GI50s = 0.05-24.55 μM) and increases survival in a P388 mouse xenograft model when administered at a dose of 25 mg/kg. Pericosine A inhibits EGFR by 40 to 70% when used at a concentration of 100 μg/ml. It also reacts with organosulfur compounds in skunk spray to form stable thioethers as odorless products.2 1.Yamada, T., Iritani, M., Ohishi, H., et al.Pericosines, antitumour metabolites from the sea hare-derived fungus Periconia byssoides. Structures and biological activitiesOrg. Biomol. Chem.5(24)3979-3986(2007) 2.Du, L., Munteanu, C., King, J.B., et al.An electrophilic natural product provides a safe and robust odor neutralization approach to counteract malodorous organosulfur metabolites encountered in skunk sprayJ. Nat. Prod.82(7)1989-1999(2019)

GPX4-IN-6 is a small molecule covalent GPX4 inhibitor (IC50: 0.12 μM) with antitumour activity.GPX4-IN-6 induces ferroptosis and is used for the treatment= and prevention of triple negative breast cancer (TNBC).

Obovatol has antioxidant, neuroprotective, antiinflammatory, antithrombotic and antitumour effects, it is a potent NF-κB inhibitors for Alzheimer's disease treatment.

Hypophyllanthin and phyllanthin have antitumour effects against Ehrlich Ascites Carcinoma in mice.

MI-773 is a potent inhibitor of the MDM2-p53 protein interaction (PPI) with a high affinity for MDM2 and a Kd value of 8.2 nM. MI-773 exhibits antitumour effects.

N6F11 is a novel, selective and potent inducer of ferroptosis with anticancer and antitumour activity that promotes GPX4 degradation by binding to TRIM25 in cancer cells.N6F11 can be used to study pancreatic cancer.

MS023 dihydrochloride (MS023 2HCl) is a selective, cytosolic and highly potent inhibitor of human type I protein arginine methyltransferases (PRMTs) with antitumour activity, inhibits PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, and increases the proliferative capacity of isolated cultured MuSC. It can be used to study breast cancer.

Antitumor agent-55 (compound 5q) is a potent antitumour agent that effectively inhibits PC3 (IC50: 0.91 μM). antitumor agent-55 blocks the G1/S phase of the PC3 cell cycle, induces apoptosis, inhibits cell migration and prevents the formation of PC3.

Sparstolonin B, a selective TLR2 and TLR4 antagonist, is an isocoumarin compound isolated from the tubers of Sparganium stoloniferum and Scirpus yagara with anti-HIV, anticancer, antitumour and anti-inflammatory activities, inhibits selective Toll-like receptors, inhibits free fatty acids It inhibits selective Toll-like receptors, inhibits free fatty acid palmitate-induced chondrocyte inflammation and attenuates post-traumatic arthritis in obese mice, and inhibits lipopolysaccharide-induced inflammation in 3T3-L1 adipocytes, which can be used for validation and mammary carcinoma studies.

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. anticancer agent 48 has potential for solid tumour and haematological tumour studies. anticancer agent 49 is a broad-spectrum anticancer agent with anti-proliferative activity.

(R)-Bicalutamide is the R-type enantiomer of Bicalutamide, an androgen receptor (AR) antagonist that exhibits antitumour effects. (R)-Bicalutamide is widely used in prostate cancer research.

MRT-2359 is a potent and orally available GSPT1 reducer with antitumour activity.MRT-2359 inhibits the growth of drug-resistant non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) cells.MRT-2359 exhibits preferential activity in MYC-driven cell lines.

MYF-03-176 is an orally active anticancer agent. MYF-03-176 exhibits strong antitumour effects in the MPM mouse xenograft tumour model following oral administration.

KB SRC 4 is a selective and potent c-Src inhibitor with antitumour activity that inhibits the growth of cancer cells.

cis-Moschamine exerts antitumour effects on HeLa, MCF7 and A431 cells.

2-Hydroxyanthraquinone is an anthraquinone that has been found inSpermacoce latifoliaand has antibacterial and estrogenic activities.1,2It is active againstB. subtilisandB. cereus(MICs = 1.9 and 62.5 μg/ml, respectively).12-Hydroxyanthraquinone (19 μM) induces estrogen receptor α (ERα) activation in a yeast two-hybrid assay.2 1.Luo, Y., Shen, H.-Y., Shen, Q.-X., et al.A new anthraquinone and a new naphthoquinone from the whole plant of Spermacoce latifoliJ. Asian Nat. Prod. Res.19(9)869-876(2017) 2.Kurihara, R., Shiraishi, F., Tanaka, N., et al.Presence and estrogenicity of anthracene derivatives in coastal Japanese watersEnviron. Toxicol. Chem.24(8)1984-1993(2005)

Topoisomerase II inhibitor 4 (compound E17) is a potent inhibitor of topoisomerase II. Topoisomerase II inhibitor 4 has antitumour effects, blocking the cell cycle in the G2/M phase, inhibiting the proliferation of cancer cells and exhibiting cytotoxicity. It inhibits the proliferation of cancer cells and exhibits cytotoxicity.

5-Hydroxyuridine (OHUrd) is a purine nucleoside analogue with potential antitumour activity, showing cytotoxicity against human colon adenocarcinoma cell lines.

GPX-100 (13-deoxydoxorubicin) is an analogue of the anthracycline antitumour antibiotic doxorubicin. GPX-100 inserts into DNA and interacts with topoisomerase II to inhibit DNA replication and repair as well as RNA and protein synthesis.

Bropirimine (U-54461) (U-54461) is a biological response modifier that is thought to act through the induction of lymphokines.