2709103-20-6

Name	Heptanamide, 7-[[[2,6-dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]amino]-N-hydroxy-
CAS	2709103-20-6
Molecular Formula	C30H38N2O5
Molecular Weight	506.63
MOL File	2709103-20-6.mol

Synonyms

HDAC6-IN-4 Heptanamide, 7-[[[2,6-dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]amino]-N-hydroxy-

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Chemical Properties

density	1.131±0.06 g/cm3(Predicted)
pka	9.48±0.20(Predicted)

Hazard Information

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⁺CD127^low/- 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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