Cancer Targeted Therapy

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC₅₀ of 8 nM.

TAS1553 is a potent, orally active protein-protein interaction (PPI) inhibitor with an IC₅₀ values of 0.0396 μM. TAS1553 inhibits DNA replication and reduces intracellular dATP pool. TAS1553 induces apoptosis. TAS1553 can be used for cancer research.

Brolucizumab (DLX1008) is a single-chain anti-VEGF-A antibody fragment with low picomolar affinity (K_D=1.05 pM). Brolucizumab can be used for the research of cancer.

Cosibelimab (CK-301) is a high-affinity, fully human PD-L1-blocking monoclonal antibody that binds PD-L1 and blocks its interaction with PD-1. Cosibelimab exhibits antitumor efficacy.

PROTAC IDO1 Degrader-1 is a potent IDO1 (Indoleamine 2,3-dioxygenase 1) PROTAC degrader with a DC₅₀ of 2.84 μM. PROTAC IDO1 Degrader-1 forms a ternary complex with IDO1 and the CRBN E3 ligase, and induces polyubiquitination of IDO1 followed by proteasomal degradation via the ubiquitin-proteasome system. PROTAC IDO1 Degrader-1 is applicable for related research on cancer immunity.

Praluzatamab is a monoclonal antibody targeting the activated leukocyte cell adhesion molecule (ALCAM/CD116). Praluzatamab can be used to synthesize Praluzatamab ravtansine (antibody-drug conjugates). Praluzatamab can be used for research of cancers.

Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC₅₀<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model.

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC₅₀ of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC₅₀=80 nM).

NSC 146109 hydrochloride (XI-011 hydrochloride) is a p53 activator and MDMX inhibitor. NSC 146109 hydrochloride inhibits MDMX gene transcription, downregulates MDMX mRNA and protein levels, stabilizes p53 and activates the transcriptional activity of p53. NSC 146109 hydrochloride induces cancer cell apoptosis (apoptosis) and inhibits the growth of transformed cells. NSC 146109 hydrochloride inhibits the growth of xenograft tumors. NSC 146109 hydrochloride can be used in research related to breast cancer and cervical cancer.

WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a K_d of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC₅₀ of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.

Anti-Mouse 4-1BB/CD137 Antibody (3H3) is an anti-mouse 4-1BB/CD137 IgG2a κ agonistic monoclonal antibody. Anti-Mouse 4-1BB/CD137 Antibody (3H3) can effectively activate memory T cells and inhibit tumors by increasing Bcl-xL and granzyme B levels. Anti-Mouse 4-1BB/CD137 Antibody (3H3) can be used for research on cancer such as lymphoma and colon cancer.

Vorsetuzumab (Anti-Human CD70 Recombinant Antibody) is a human anti-CD70 antibody. Vorsetuzumab enhances macrophage-related phagocytosis of renal carcinoma cells, shows inhibitory efficacy against Burkitt’s lymphoma.

TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4_DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity.

Denikitug (GS-1811; JTX-1811) is a humanized monoclonal antibody against CCR8 receptor with a K_D of 16.8 pM. Denikitug specifically binds to human CCR8, inhibits CCL1-induced downstream CCR8 signaling. Denikitug selectively depletes cells expressing CCR8 via antibody-dependent cellular cytotoxicity (ADCC). Denikitug promotes anti-tumor immunity and can be used for the research of cancer and immunology.

TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC₅₀ values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma.

GN25 is a specific p53-Snail binding inhibitor with antitumor effects.

SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research.

GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC₅₀=41 nM), BRD3 (IC₅₀=31 nM), and BRD4 (IC₅₀=22 nM).

Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC₅₀: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers.

Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidine synthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs.