Cancer Targeted Therapy

PQ-1 is a gap junction enhancer.

IDO1-IN-21 (compound 10m) is an IDO1 inhibitor (IC₅₀ = 0.64 μM). IDO1-IN-21 effectively inhibits tumor growth in mice.

2’,3’,5’-Tri-O-acetyl-5-methoxycarbonylmethyl-2-thiouridine 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.

HDAC-IN-61 (compound 12k) is a potent and orally active HDAC inhibitor. HDAC-IN-61 has anticancer active with an IC₅₀ value of 30 nM for Bel-7402 cell. HDAC-IN-61 can be used in research of cancer.

MAT2A inhibitor 6 (Compound 3N-h) is a specific MAT2A inhibitor with oral activity and yellow fluorescence (IC₅₀=26 nM), capable of visualizing MAT2A both in vitro and in vivo (λex = 430 nm, λem = 585 nm). MAT2A inhibitor 6 can induce apoptosis and has anticancer activity, which can be used in cancer research.

EGFR kinase inhibitor 6 (Compound 4b) is an orally active inhibitor for epidermal growth factor receptor (EGFR) kinase, with IC₅₀ of 24.34 μM. EGFR kinase inhibitor 6 induces apoptosis. EGFR kinase inhibitor 6 exhibits anticancer and anti-inflammatory activity with low toxicity (LD₅₀ range: 500-2000 mg/kg).

HSP90-IN-33 (compound 24e) is a potent Hsp90 inhibitor with K_d values of ≥200, 7.3 µM for Hsp90α, Hsp90β, respectively. HSP90-IN-33 induces apoptosis and cell cycle arrest at G0/G1 phase. HSP90-IN-33 decreases the protein expression of ERα, CDK4 and Akt.

DSPE-PEG5000-BR2 is a PEG compound which composed of DSPE and a BR2. BR2 is a targeting peptide composed of 17 amino acids with the sequence RAGLQFPVGRLLRRLLR. It has the ability to assist cells to penetrate the membrane and can specifically target certain cells or tissues.

BY13 is a SRC-3 PROTAC degrader with a DC₅₀ of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model.

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

Cryptophycin analog 1 is an ADC payload. Cryptophycin analog 1 shows anticancer activity. Cryptophycin analog 1 displays cell activity an order of magnitude more potent than approved ADC payloads MMAE and DM1.

mmu-miR-297b-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-684 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-7689-3p 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-581 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.

hsa-miR-7848-3p 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.

CAIX-IN-17 is a carbonic anhydrase IX (CAIX) inhibitor with an IC₅₀ of 61 nM and accumulates specifically in CAIX-expressing xenograft tumors. CAIX-IN-17 can be labeled with ⁶⁸Ga and acts as a CAIX-targeted PET tracer for detection of clear-cell renal cell carcinoma.

(6E)-1,7-Bis(4-hydroxyphenyl)-6-hepten-3-one (compound7) is a nature product isolated from rhizomes of Curcuma kwangsiensis. (6E)-1,7-Bis(4-hydroxyphenyl)-6-hepten-3-one has inhibitory effect on NO production induced by LPS in macrophages with an IC₅₀ value of 8.93 μM.

FS102 is a selective Fc fragment with antigen binding (Fcab) that targets HER2 with a K_D value of 0.8 nM. FS102 induces the degradation of HER2, activates Caspase 3/7 and disrupts the integrity of the cell membrane, triggering apoptosis of tumor cells. FS102 is promising for research of cancers such as breast cancer, gastric cancer, and colorectal cancer.

hsa-miR-361-5p 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.