Cancer Targeted Therapy

PI3K/mTOR-IN-23 is a dual inhibitor of PI3K and mTOR with IC₅₀ values of 49 and 41 nM. PI3K/mTOR-IN-23 inhibits cancer cells proliferation.

Afatinib-d₆ (BIBW 2992-d₆) is deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor.

SF2312 ammonium is a phosphonate Antibiotic and Enolase inhibitor, with an IC₅₀ of 18.4 nM against E. coli enolase. SF2312 ammonium reduces intracellular ATP levels and inhibits glycolytic flux. SF2312 ammonium exhibits activity against both Gram-positive and Gram-negative bacteria, and exerts synergistic effects against E. coli when combined with Fosfomycin (HY-B1075A). SF2312 ammonium shows selective toxicity toward gliomas with ENO1 gene knockout. SF2312 ammonium can be used in research related to bacterial infections and gliomas.

Erlotinib-d₆ hydrochloride (CP-358774-d₆ hydrochloride) is the deuterated-labeled Erlotinib Hydrochloride (HY-12008). Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis.

KRpep-2d (TFA) is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research.

Iodo-PEG7-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

TH9028 is an inhibitor of MTHFD1, MTHFD2 and MTHFD2L, with IC₅₀ values of 0.5 nM, 11 nM and 27 nM, respectively. TH9028 reduces replication fork speed, induces replication stress, triggers S-phase arrest, initiates apoptosis, impairs thymidine production, and causes erroneous uracil incorporation into DNA. TH9028 can be used in research related to acute myeloid leukemia.

hsa-miR-221-3p 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.

2'-Fluorothymidine (2'-Fluoro-2'-deoxythymidine) is a nucleoside analog and hCNT inhibitor, with an IC₅₀ of 1.1 μM against hCNT1 and an IC₅₀ of 9.7 μM against hCNT3. 2'-Fluorothymidine undergoes phosphorylation by cytosolic thymidine kinase (TK1) and mitochondrial thymidine kinase (TK2). 2'-Fluorothymidine acts as a backbone stabilizer in oligonucleotide synthesis and can also form radiolabeled candidates. 2'-Fluorothymidine is applicable in tumor-related research.

SYNTi is a PDZ domain inhibitor targeting the syndecan/syntenin protein-protein Interaction. SYNTi exhibits an IC₅₀ value of 400 nM and ligand efficiency (LE) value of 0.24. SYNTi can be used for breast cancer research.

Fmoc-Phe-Lys(Trt)-PAB is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HDAC3/8 ligand-1 (compound 40) is a ligand for target protein for PROTAC that can be used in the synthesis of YX968 (HY-164233).

Nacolomab is an anti-human monoclonal antibody targeting MUC1/CD227. Nacolomab can be used for the research of cancer.

Aminooxy-PEG3-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Fmoc-Gly-Gly-allyl propionate is a cleavable linker that can be used to synthesize Antibody-Drug Conjugates (ADCs).

MY-943 is a potent tubulin polymerization and LSD1 inhibitor with anticancer activity. MY-943 induces G2/M phase arrest and apoptosis, and inhibits cell migration. MY-943 can be used for gastric cancer research.

Desthiobiotin-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain. γ-Acetylenic GABA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

hsa-miR-23a-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.

MC-VC-PAB-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).