Cancer Targeted Therapy

5-(2,3,5-Tri-O-benzyl-beta-D-ribofuranosyl)-3-methyl-2-benzyloxypyridine 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.

Lovastatin-d₉ is the deuterium labeled Lovastatin. Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.

rno-miR-128-2-5p 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.

RIPK1-IN-23 (compound 19) is a RIPK1 inhibitor with potent anti-necroptotic effects in HT-29 cells (EC₅₀ of 1.7 nM). RIPK1-IN-23 shows anti-inflammatory activities.

Antiproliferative agent-52 is a tubulin inhibitor with a porcine tubulin K_D of 29.65 μM. Antiproliferative agent-52 binds to the colchicine-binding site at the α-tubulin and β-tubulin interface and inhibits tubulin polymerization. Antiproliferative agent-52 exhibits antiproliferative activity against tumor cells. Antiproliferative agent-52 serves as a lead compound for development of thienopyrimidine and heterocyclic fused pyrimidines with antiproliferative activity. Antiproliferative agent-52 can be used for the research of ovarian cancer, non-small cell lung cancer.

TTK/PLK1-IN-1 (Formula I) is the inhibitor for threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1) with IC₅₀ of 7 nM and 72 nM. TTK/PLK1-IN-1 regulates spindle assembly checkpoint (SAC), and exhibits antitumor efficacy against TNBC.

YW-N-7 TFA is a PROTAC degrader targeting RET kinase, with an IC₅₀ of 8.4 nM. YW-N-7 TFA inhibits RET kinase activity and induces proteasome-mediated degradation of RET fusion proteins, while enhancing the anti-tumor activity of Selpercatinib (LOXO-292) (HY-114370). YW-N-7 TFA can be used in the research of cancers associated with RET gene abnormalities, including medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer.

WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC₅₀: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell).

BL20-MMAE is an antibody-drug conjugate targeting ROR1, which is formed by conjugating an anti-ROR1 antibody with the Auristatin payload MMAE (HY-15162) via a BL20 linker.

hsa-miR-937-5p 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-448-5p 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-7017-3p 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.

KRAS G12C inhibitor 30 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 2. KRAS G12C inhibitor 30 can be used for the research of cancer.

KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC₅₀ of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC₅₀s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers.

NSC 698600 is a potent PCAF inhibitor, with IC₅₀ of 6.51 µM (PCAF/H3_1-21). NSC 698600 exhibits good activity of inhibiting the proliferation of cancer cells.

hsa-miR-1287-3p 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.

hsa-miR-374b-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.

hsa-miR-4804-5p 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.

Amprenavir (Standard) is the analytical standard of Amprenavir. This product is intended for research and analytical applications. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.

Avicin G is a sphingomyelinase inhibitor and plasma membrane disruptor. Avicin G inhibits the enzymatic activities of neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1), elevates intracellular sphingomyelin levels, and alters the distribution of sphingomyelin. Avicin G interferes with the lateral segregation of GTP- and GDP-bound H-Ras, inhibits the signal output of oncogenic K-Ras and H-Ras, reduces the phosphorylation of ERK and Akt, increases lysosomal pH, and inhibits the endocytic recycling of epidermal growth factor receptor. Avicin G can be used in research related to pancreatic ductal adenocarcinoma and non-small cell lung cancer.