Cancer Targeted Therapy

mmu-miR-7060-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

rno-miR-466c-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

CL 5343 (Standard) is the analytical standard of CL 5343. This product is intended for research and analytical applications. CL 5343 (5-Amino-1,3,4-thiadiazole-2-sulfonamide) is an inhibitor of human carbonic anhydrase B (HCA-B). CL 5343 can serve as a CA9 ligand to achieve the targeted delivery of maytansinoid to the cell membrane of SKRC52 renal cancer cells.

Biotin-PEG5-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Tos-PEG2-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

StA-IFN-1 is an inhibitor for type I interferon (IFN), that inhibits the activation of IFNβ with an IC₅₀ of 4.1 μM.

EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFR^{L858R/T790M/C797S} with an IC₅₀ value of 0.053 μM, and has a relatively weak effect on EGFR^WT (IC₅₀: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFR^{L858R/T790M/C797S} with an IC₅₀ of 0.052 μM.

Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC₅₀ values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFR^wt, EGFR^L858R/T790M, EGFR^L858R and EGFR^T790M, respectively.

JAK3-IN-16 (compound 6) is a covalent JAK3 inhibitor.

Pantoprazole-d₆ is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC₅₀ of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).

Dihydrouracil-Ph-2-Me-piperidine is an E3 ligase ligand. Dihydrouracil-Ph-2-Me-piperidine can be used to synthesize PROTAC HPK1 Degrader-6 (HY-178459)

Trastuzumab deruxtecan (DAR2) (T-DXd (DAR2); DS-8201 (DAR2); DS-8201a (DAR2)) is a low-drug-load derivative control preparation of Trastuzumab deruxtecan (HY-138298A) with a drug-to-antibody ratio (DAR) of 2. Trastuzumab deruxtecan (T-DXd; DS-8201a; DS-8201) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer.

2-(1-Piperazinyl)pyrimidine (Standard) is the analytical standard of 2-(1-Piperazinyl)pyrimidine. This product is intended for research and analytical applications. 2-(1-Piperazinyl)pyrimidine is the major metabolite of Tandospirone (HY-14558).

hsa-miR-2682-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation.

FOXM1-IN-2 is a FOXM1 inhibitor, with antineoplastic activity.

FGFR3-IN-1 (compound 1) is a fibroblast growth factor receptor (FGFR) inhibitor, with IC₅₀s of 40 nM, 5.1 nM, and 12 nM for FGFR1, 2, and 3, respectively. FGFR3-IN-1 can be used for the research of bladder cancer.

AKT-IN-11 is one of the most effective antibacterial agents against human hepatoma BEL-7402 cell line with an IC₅₀ value of 1.15μM.

EGFR T790M/L858R-IN-3 (compound B1) is a EGFR^L858R/T790M inhibitor with IC₅₀ value of 13?nM. EGFR T790M/L858R-IN-3 shows anti-tumour activity in H1975 cells with an IC₅₀ value of 0.087 μΜ. EGFR T790M/L858R-IN-3 inhibits cell migration in A549 cells and induces apoptosis in H1975 cells.

hsa-miR-548f-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.