Cancer Targeted Therapy

Tetrazine-Ph-NHCO-PEG4-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Tetrazine-Ph-NHCO-PEG4-NH-Boc is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.

PROTAC SMARCA2/4-degrader-33 (compound I-277) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC₅₀s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment.

OPSS-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

FGFR-IN-18 (Compound KF7) is a lysine-targeting FGFR covalent inhibitor, with IC₅₀s of: 1.1 nM for FGFR2, 1.3 nM for FGFR1, 31.5 nM for FGFR4. FGFR-IN-18 also has affinity for FGFR3 (inhibition rate of 52% at 10 nM). FGFR-IN-18 covalently modifies Lys485 (an reactive site of FGFRs).

Ras Inhibitory Peptide (VPPPVPPRRR) is a Ras inhibitor with antitumor activity.

Ras modulator-1 is a modulator of Ras. Ras modulator-1 is an active compound extracted from patent US20120302581.

hsa-miR-4531 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-5698 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-7-2-3p 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.

EGFR-IN-132 (Compound 23) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC₅₀ of 1.6, 0.025, 0.019, 0.022, and 0.029 nM. EGFR-IN-132 exhibits good pharmacokinetics characteristics with high oral exposure.

KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC₅₀ = 0.29 μM) and BGC-823 gastric cancer cells (IC₅₀ = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer.

FRAGHIT-4 is an estrogen receptor alpha (ERα) inhibitor. FRAGHIT-4 exhibits antineoplastic activity against breast cancer via targeting ER signaling. FRAGHIT-4 can be used for the research of breast cancer.

mmu-miR-497b 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.

mmu-miR-7056-3p 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.

rno-miR-455-3p 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.

Alkyne-ethyl-PEG1-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Alkyne-ethyl-PEG1-Boc is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

SB-590885 GMP is SB-590885 (HY-10966) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SB-590885 is a BRAF/c-Raf kinase inhibitor that selectively targets B-Raf, and it amplifies the ERK/MAPK signaling pathway in RAS-activated cells. SB-590885 effectively inhibits the malignant proliferation, transformation and tumorigenicity of oncogenic B-Raf cells; it also induces the proliferation of erythroid progenitor cells, delays their differentiation and promotes hemoglobin synthesis, thereby improving ineffective erythropoiesis and reducing apoptosis. SB-590885 exerts a synergistic effect with TGF-β inhibitors and glucocorticoids, significantly promoting the formation of erythroid colonies in cells from patients with Diamond-Blackfan anemia (DBA). SB-590885 is mainly used in relevant studies on DBA, cisplatin-induced myelosuppression-related anemia, and pan-cancers such as melanoma and colorectal cancer.

PARP7-IN-19 (compound 5a) is an inhibitor of PARP7 ( IC₅₀ ≤10nM). PARP7-IN-19 can be used in the research area of tumors.

mmu-miR-1942 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.

mmu-miR-6372 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.