Cancer Targeted Therapy

AURKA-IN-3 (Compound AL8) is an irreversible covalent Aurora kinase A (AURKA) inhibitor with an IC₅₀ value of 23.0 nM. AURKA-IN-3 inhibits the activation of cAMP signaling pathway and phospholipase C (PLC) signaling pathway mediated by AURKA, and reduces the autophosphorylation level of AURKA. AURKA-IN-3 is promising for research of malignant tumors associated with high AURKA expression (e.g., leukemia, lymphoma).

ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer.

DOPE-PEG1000-T7 is a functionalized PEGylated lipid conjugate composed of three modular components: dioleoylphosphatidylethanolamine (DOPE) as the lipid anchoring group, a polyethylene glycol (PEG) spacer arm with a molecular weight of 1000 Da, and T7 peptide (HAIYPRH) as the terminal targeting/functional ligand. DOPE-PEG1000-T7 can be incorporated into liposomes, lipid nanoparticles (LNPs), or other nanocarriers to confer ligand-directed targeting capability against transferrin receptor (TfR/CD71) on the surface of cancer cells and brain endothelial cells.

2-Amino-6-O-methyl-2’-O-methyl purine riboside is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc.

Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the K_i of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer.

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

Carboxy-PEG4-phosphonic acid ethyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

ERα ligand 4 is a ligand of ERα and can be used for the synthesis of PROTACs, such as NEP168 (HY-180959).

VEGFR-2-IN-11 (Compound 8h) is a potent VEGFR-2 inhibitor with an IC₅₀ of 60.27 nM. VEGFR-2-IN-11 shows antitumor activity and induces cell apoptosis.

hsa-miR-8088 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.

mmu-miR-370-5p 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.

mmu-miR-6997-5p 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.

rno-miR-32-3p 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.

Tos-PEG3-O-C1-CH3COO (PROTAC Linker 6) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

HPK1-IN-2 TFA is an orally active HPK1 inhibitor (IC₅₀ < 0.05 µM) with antitumor activity. HPK1-IN-2 TFA inhibits the activity of Lck (IC₅₀ <0.05 µM) and Flt3 (IC₅₀ < 0.05 µM) kinases.

hsa-miR-3074-3p 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.

hsa-miR-4524b-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.

hsa-miR-5692b 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.

Tubulin inhibitor 48 (compound 16) is an anti-cancer agent targeting tubulin. Tubulin inhibitor 48 has an IC₅₀ of 0.1 and 0.07 μM for LN-229 and Capan-1 cell, respectively.

FDU73 is a potent and selective BTK PROTAC degrader with a DC₅₀ value of 2.9 nM (JeKo-1). FDU73 degrades BTK via the ubiquitin-proteasome system. FDU73 exerts antiproliferative effects on cancer cells. FDU73 can be used for the research of B-cell malignancies.