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Results for "

phase I clinical trial

" in MedChemExpress (MCE) Product Catalog:

4

Inhibitors & Agonists

1

Inhibitory Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13590
    CEP-7055

    		VEGFR Cancer
    CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
    CEP-7055
  • HY-15334
    CEP-5214

    		VEGFR Cancer
    CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
    CEP-5214
  • HY-P992446
    PUR001

    		NTPDase Cancer
    PUR001 is a monoclonal antibody targeting NTPDase 1 (CD39). PUR001 blocks the hydrolysis of extracellular ATP and ADP into AMP by inhibiting CD39, reduces the production of immunosuppressive adenosine, and increases extracellular ATP concentration to activate anti-tumor immune responses. PUR001 can be used in studies related to solid tumors .
    PUR001
  • HY-168168
    (5aS,6R,6aR)-MK-8666

    		Endogenous Metabolite Metabolic Disease
    (5aS,6R,6aR)-MK-8666 is a selective GPR40 agonist with activity in promoting fatty acid-induced insulin secretion in pancreatic β cells and intestinal enteroendocrine cells. (5aS,6R,6aR)-MK-8666 has been studied for the inhibition of type 2 diabetes and has shown significant blood glucose lowering effects. Although (5aS,6R,6aR)-MK-8666 is considered to have potential inhibitory advantages, its development was stopped in Phase I clinical trials due to liver safety issues .
    (5aS,6R,6aR)-MK-8666

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