Cancer Targeted Therapy

Hydroxy-PEG2-(CH2)2-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG2-(CH2)2-Boc is extracted from patent WO2004008101A2 (compound 196). Hydroxy-PEG2-(CH2)2-Boc is also a PROTAC linker that can be used in the synthesis of PROTACs.

CNDAC hydrochloride is a metabolite of the orally active agent Sapacitabine (HY-16445), and a nucleoside analog. CNDAC hydrochloride induces DNA damage and apoptosis.

TDI-6118 (Compound 5) is a potent brain-penetrant inhibitor of EZH2. EZH2-IN-12 has the potential for the research of central nervous system malignancies.

(R)-(+)-Aminoglutethimide is a potent and orally active aromatase inhibitor. (R)-(+)-Aminoglutethimide has the potential for the research of breast cancer.

(S)-Navlimetostat (example 16-7) is the S-enantiomer of Navlimetostat. (S)-Navlimetostat is a PRMT5/MTA complex inhibitor, with an IC₅₀ of 7070 nM.

7-O-(Amino-PEG4)-paclitaxel is a PEG-class Drug-linker conjugates for ADC, containing a paclitaxel moiety and a amino group. The amine group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. 7-O-(Amino-PEG4)-paclitaxel can be used in the synthesis of Antibody-Drug Conjugates (ADCs).

Tisolagiline methylsulfate (KDS2010) is the selective, reversible and orally active inhibitor for MAO-B with an IC₅₀ of 8 nM. Tisolagiline methylsulfate exhibits neuroprotective and anti-neuroinflammatory activities.

MS152 is an orally active, blood-brain barrier penetrant inhibitor of EHMT2/G9a and EHMT1/GLP, with IC₅₀s of 76 nM and 126 nM, repsectively. MS152 reduces H3K9me2 levels and reactivates maternally silenced Prader-Willi syndrome (PWS) genes. MS152 significantly improves perinatal lethality and growth retardation in mouse models, and is applicable to research related to Prader-Willi syndrome.

DGKα-IN-2 (example 48) is a DGKα inhibitor with the IC₅₀ of 0.9 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.

Dioxybenzone (Benzophenone-8; UV-24) is an organic compound used to block UVB and short-wave UVA (ultraviolet) radiation. Dioxybenzone has orally activity. Dioxybenzone exhibits estrogenic disrupting effect. Dioxybenzone up-regulates inflammatory cytokines. Dioxybenzone can be used for cancer, reproductive system disease and inflammatory disease study.

Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research.

FmocNH-PEG3-CH2CH2NH2 (hydrochloride) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Viscidulin III is a compound isolated from the roots of Scutellaria planipes (L.). Viscidulin III can inhibit the proliferation of HL-60 (IC50= 17.4μM). Viscidulin III is a potential natural tumor inhibitor.

m-PEG12-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. m-PEG12-OH is also a non-cleavable 12 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC₅₀ of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research.

Kuwanon H is a selective non-peptide bombesin receptor antagonist and platelet activation inhibitor. Kuwanon H also acts as a specific antagonist of GRP-preferring receptors, with a K_i value of 290 nM for mouse GRP-R and 6500 nM for rat NMB-R. Kuwanon H inhibits the phosphorylation of AKT, mTOR, ERK, cPLA₂ and p38, and upregulates TRIB3. It induces endoplasmic reticulum stress, apoptosis and autophagosome formation. Kuwanon H blocks calcium mobilization, mitogenic signaling, DNA synthesis, dense granule secretion, thromboxane A₂ generation and integrin αIIb/β₃ activity. It inhibits collagen-induced platelet aggregation and fibronectin adhesion, and delays clot retraction. Kuwanon H inhibits melanoma cell growth in vitro and in vivo, and enhances the sensitivity of melanoma cells to CDDP. It can be used in research related to melanoma, small cell lung cancer and thrombosis.

Amino-PEG3-C2-sulfonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC₅₀ values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model.

CXCL-CXCR1/2-IN-1 is an orally active ELR⁺CXCL-CXCR1/2 pathway inhibitor with an EC₅₀ of 42.7 nM for CXCR2. CXCL-CXCR1/2-IN-1 shows anticancer and antiangiogenic effects.

Mal-PEG36-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.