| Identification | Back Directory | [Name]
2-Propenoic acid, 3-[4'-[2-(hydroxyamino)-1-methyl-2-oxoethoxy]-3'-tricyclo[3.3.1.13,7]dec-1-yl[1,1'-biphenyl]-4-yl]-, (2E)- | [CAS]
2487526-28-1 | [Synonyms]
GEM144
2-Propenoic acid, 3-[4'-[2-(hydroxyamino)-1-methyl-2-oxoethoxy]-3'-tricyclo[3.3.1.13,7]dec-1-yl[1,1'-biphenyl]-4-yl]-, (2E)- | [Molecular Formula]
C28H31NO5 | [MOL File]
2487526-28-1.mol | [Molecular Weight]
461.55 |
| Hazard Information | Back Directory | [Uses]
GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts[1]. | [in vivo]
GEM144 (50 mg/kg; p.o., bid, 5 days a week, for 3-4 weeks) significantly reduces tumor burden of MM487 with TGI of 72% in xenografts mice[1]. | Animal Model: | Female CD-1 nude mice (injected with MM473 and MM487)[1] | | Dosage: | 50 mg/kg | | Administration: | PO, bid, 5 days a week, for 3-4 weeks | | Result: | Significantly reduced tumor burden of MM487 with TGI of 72%. |
| [IC 50]
HDAC11: 8.23 μM (IC50) | [References]
[1] Dallavalle S, et al. Antitumor activity of novel POLA1-HDAC11 dual inhibitors. Eur J Med Chem. 2022;228:113971. DOI:10.1016/j.ejmech.2021.113971 |
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