sarcoma

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

Seclidemstat (SP-2577) is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.

Laminin β2 (Engelbreth-Holm-Swarm murine sarcoma basement membrane) is a crucial structural component in animal tissues, forming part of the framework that supports tissue architecture. It interacts with type IV collagen through entactin and basement membrane proteoglycans and associates with cell membranes via integrin receptors, dystroglycan complexes, and Lutheran blood group glycoproteins. Additionally, it contains functional domains that facilitate collagen binding, cell adhesion, heparin interactions, and promote neurite outgrowth.

Osteosarcoma-IN-D14 is an inhibitor of migration and invasion of osteosarcoma cells mediated by p53, regulating EMT-related genes.

Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma/follicular lymphoma.

Silver chloride can be used as a buffer in electrodes or spectroscopic analysis. Silver chloride exhibits inhibitory activity against various bacteria and demonstrates antitumour activity against Ewing sarcoma when formulated as nanoparticles (AgCl-NPs).

BK60106 is a selective inhibitor of the transmembrane protein CD99, which causes cell death in Ewing Sarcoma cells by directly binding to the extracellular structural domain of CD99.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

Dacarbazine citrate is an alkylating agent used to treat cancers of the lymphatic system and malignant melanoma (a type of skin cancer) in patients with certain conditions: islet cell carcinoma (part of the pancreas) Soft tissue sarcoma (cancer of muscles

TK216 is a potent inhibitor of E26 transformation-specific (ETS) with anticancer activity.

Trabectedin (Ecteinascidin 743) has potent antitumor activity and the potential for soft tissue sarcoma and ovarian cancer research. Trabectedin inhibits cell growth of MX-1, MCF7 and MCF7 DXR cells with IC50 values of 0.1 nM, 1.5 nM and 3.7 nM, respectively.

SXT1596 is a novel SS18-SSX/TLE1 interaction inhibitor. SXT1596 reduces cell viability and reactivates EGR1 expression in synovial sarcoma.

NSC635437 acts as an inhibitor of the EWS-FLI1 oncoprotein in Ewing's sarcoma.

Olomorasibum is an inhibitor of Kirsten rat sarcoma viral oncogene homolog (KRAS) and belongs to the category of antitumor compounds.

Sosimerasib is an inhibitor of the kirsten rat sarcoma viral oncogene homolog (KRAS) and exhibits antitumor activity.

EB-TCIP (BAK-04-212) is a bivalent molecule composed of AP1867 and BI-3812. It facilitates the reversible formation of a ternary complex between FKBPF36V and BCL6BTB, thereby recruiting FKBP12F36V-tagged EWS/FLI1 to DNA sites bound by the transcriptional regulator BCL6, rapidly inducing expression of BCL6 target genes such as SOCS2 and CXCL11. EWS/FLI1 is a fusion transcription factor found in Ewing sarcoma. EB-TCIP is applicable for studying transcriptional dysregulation in cancer.

PF-562271 hydrochloride (PF-562271 HCl) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

RETRA is an agent of anticancer that acts by exerting anticancer activity in Ewing's sarcoma cells independent of their TP53 status.

FR 900490 is an immunoactive substance produced by a fungus Discosia sp. F-11809. In vitro FR-900490 restores the colony forming units in culture (cfu-c) in bone marrow cells, which were suppressed by immunosuppressive factor obtained from the serum of sa

DC 86M is an antitumor antibiotic isolated from the culture broth of Streptomyces luteogriseus DO-86. DC 86M is active against Gram-positive and Gram-negative bacteria and experimental murine sarcoma 180.

Potent BRD9 degrader. Selectively binds BRD9 and elicits near complete degradation of BRD9 at nanomolar concentrations. Inhibits growth of synovial sarcoma cells in vitro and tumor progression in a synovial sarcoma xenograft mouse model.

YW3-56 is an inhibitor of protein arginine deiminase 2 (PAD2) and PAD4 (IC50s = 0.5-1 and 1-5 μM, respectively).1It inhibits the growth of U2OS osteosarcoma cells (IC50= ~2.5 μM) in a p53-dependent mannerviainduction of SESN2 and subsequent inhibition of mTORC1. YW3-56 (10 mg kg) reduces tumor growth in an S-180 murine sarcoma tumor model. It also inhibits tumor growth in the 1883 MDA-MB-231 breast cancer bone metastasis mouse xenograft model.2 1.Wang, Y., Li, P., Wang, S., et al.Anticancer peptidylarginine deiminase (PAD) inhibitors regulate the autophagy flux and the mammalian target of rapamycin complex 1 activityThe Journal of Biological Chemisty287(31)25941-25952(2012) 2.Wang, S., Chen, X.A., Hu, J., et al.ATF4 gene network mediates cellular response to the anticancer PAD inhibitor YW3-56 in triple-negative breast cancer cellsMol. Cancer Ther.14(4)877-888(2015)

Degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS FLI-expressing Ewing sarcoma cells. Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use. Negative control dTAGV-1-NEG (Cat. No. 6915) also available. FKBP12F36V can be expressed as a fusion with a target protein of interest using genome engineering techniques, via transgene expression or CRISPR-mediated locus-specific knock-in. Custom knock-in cell lines for the dTAG and aTAG platforms are available from our sister brand R&D Systems. Email TPD@bio-techne.com to enquire. Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.

cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when administered at doses of 40 and 80 mg/kg, respectively.2 1.Lovejoy, K.S., Todd, R.C., Zhang, S., et al.cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospectsProc. Natl. Acad. Sci. USA105(26)8902-9807(2008) 2.Hollis, L.S., Amundsen, A.R., and Stern, E.W.Chemical and biological properties of a new series of cis-diammineplatinum(II) antitumor agents containing three nitrogen donors: cis-[Pt(NH3)2(N-donor)Cl]+J. Med. Chem.32128-136(1989)