| Identification | Back Directory | [Name]
Heptanamide, 7-[[[2,6-dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]amino]-N-hydroxy- | [CAS]
2709103-20-6 | [Synonyms]
HDAC6-IN-4
Heptanamide, 7-[[[2,6-dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]amino]-N-hydroxy- | [Molecular Formula]
C30H38N2O5 | [MOL File]
2709103-20-6.mol | [Molecular Weight]
506.63 |
| Hazard Information | Back Directory | [Uses]
HDAC6-IN-4 (C10) is a potent, orally active and highly selective HDAC6 inhibitor with an IC50 value of 23 nM. HDAC6-IN-4 induces cancer cells apoptosis and shows significant antitumor efficacy, without obvious toxicity[1]. | [in vivo]
HDAC6-IN-4 (C10) (0-100 mg/kg; i.g.; once daily for 21 days) shows excellent antitumor activity and significantly promoted T cell response in a dose-dependent manner, with no obvious toxicity[1]. | Animal Model: | Five-week-old C57BL/6 mice (immune-related CT26 xenograft model)[1]. | | Dosage: | 50 and 100 mg/kg | | Administration: | Oral gavage, once daily for 21 days | | Result: | Resulted in a substantial tumor growth and tumor tissue size inhibition in a dose-dependent way. Showed significantly high antitumor activity (TGI = 75%) at 100 mg/kg. Raised the plasma IFN-g level and the numbers of CD+ and CD3+CD+ (activated cytotoxic T) cells. Decreased CD4+CD25+CD127low/- T regulatory cells. Showed no obvious toxicity. |
| [IC 50]
HDAC6: 23 nM (IC50); HDAC3: 46 nM (IC50); HDAC2: 172 nM (IC50); HDAC8: 2175 nM (IC50); HDAC1: 3604 nM (IC50) | [References]
[1] Xi Xu, et al. Novel biphenyl-based scaffold as potent and selective histone deacetylase 6 (HDAC6) inhibitors: Identification, development and pharmacological evaluation. Eur J Med Chem. 2022 Apr 5;233:114228. DOI:10.1016/j.ejmech.2022.114228 |
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