Cancer Targeted Therapy

DOTA-ECL1i is a conjugate of the CCR2 inhibitor ECL1i (HY-P11553) and DOTA. When radiolabeled with ⁶⁸Ga, DOTA-ECL1i serves as a PET tracer that targets CCR2 expression. DOTA-ECL1i can be used in research related to pulmonary fibrosis, cardiac injury, abdominal aortic aneurysm inflammation, atherosclerosis, head and neck cancer, and pancreatic cancer.

NH2-PEG2-methyl acetate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Pomalidomide-PEG5-C2-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.Pomalidomide-PEG5-C2-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.

Pomalidomide-5-C9-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.Pomalidomide-5-C9-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.

Chrysomycin A (Chr-A), an antibiotic, can be obtained from Streptomyces. Chrysomycin A exhibits antitumor and anti-tuberculous and MRSA activities. As for glioblastoma, Chrysomycin A inhibits the proliferation, migration, and invasion of cancer cells through the Akt/GSK-3β/β-catenin signaling pathway.

Kisspeptin-54(human) TFA (Metastin(human) TFA) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) TFA binds to rat and human GPR54 receptors with K_i values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) TFA hinders tumor metastasis and stimulates gonadotropin secretion.

RPARPAR acetate is a CendR tumor-penetrating peptide. RPARPAR acetate directly binds to the NRP-1 and NRP-2 receptors on the surface of tumor cells, triggering cellular internalization, vascular extravasation, and penetration into tumor tissues. RPARPAR acetate serves as an efficient ligand for targeting nanocarriers to NRP-1-positive tumors. RPARPAR acetate is applicable in research on tumor targeting and drug delivery.

Zemlikafusp alfa (IPH6501) is a tetra-specific NK cell engager that targets CD20, CD16a, NKp46 and carries an IL-2 variant. Zemlikafusp alfa (IPH6501) is used in research for the treatment of relapsed/refractory B-cell non-Hodgkin lymphoma.

Oncrasin-60 (NSC-741909) is a compound with antitumor activity that is active against multiple cancer cell lines in vitro and can induce tumor regression in vivo, with its mechanism involving JNK activation and STAT3 inhibition.

Lys-Nε-SPDB-DM4 is a agent-linker conjugate composed of a potent a tubulin inhibitor DM4 and a linker Lys-Nε-SPDB to make antibody agent conjugate (ADC).

Azido-PEG9-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG9-alcohol is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

hsa-miR-100-5p 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.

MS012 is a selective GLP inhibitor (IC₅₀=7 nM). MS012 can be used in research of GLP dysregulation, including cancer, inflammatory diseases, and neuroregenerative disorders.

hsa-miR-518f-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.

Neu5Ac-2Galβ1-3Glc-oxazoline-(2)Me (Compound G12) sodium is a disaccharide linker. Neu5Ac-2Galβ1-3Glc-oxazoline-(2)Me sodium can be efficiently recognized by the endo-glycosidase Endo-S2 and can be directedly transferred to the conserved N-glycosylation site (Asn297 position) of the antibody's Fc domain through enzymatic catalytic reactions, thereby achieving site-specific modification of the antibody. Neu5Ac-2Galβ1-3Glc-oxazoline-(2)Me sodium can be used for for the synthesis of antibody-conjugated drugs (ADCs).

mmu-miR-326-3p 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.

Blidarvetug is a veterinary monoclonal antibody targeting MS4A1/CD20, which can be used to study CD20-positive B-cell lymphoma in dogs.

mmu-miR-466l-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.

RAD51-IN-3 (Example 66A) is an inhibitor of Rad51.

CDK12-IN-8 (Compound Cpd143) is an orally active and highly selective inhibitor of cyclin-dependent kinase 12 (CDK12). CDK12-IN-8 inhibits CDK12-mediated phosphorylation of the C-terminal domain (CTD) serine 2 of RNA polymerase II, interfering with gene transcription elongation and DNA damage repair pathways. CDK12-IN-8 is promising for research of cancers with high CDK12 expression such as small cell lung cancer and triple-negative breast cancer.