DS-9300

DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

DS-9300 inhibits the growth of prostate cancer cell lines with the IC50 values of 0.6, 6.5, 3.4 and 287.2 nM for VCaP, 22Rv1, LNCaP and PC3 cells, respectively, indicating that it could effectively inhibit the growth of prostate cancer cell lines by inhibiting histone acetylation and down-regulating PSA expression[1].

DS-9300 (p.o., 0.3-3 mg/kg, once daily, 33days) shows dose-dependent antitumor activity with 39%, 74% and 109% tumor growth inhibition at 0.3, 1 and 3 mg/kg, respectively, and no significant toxic effects in Castrated VCaP xenograft mouse model[1]. The pharmacokinetic parameters of DS-9300 in BALB/c mice PO(10 mg/kg) IV(1 mg/kg) AUC, AUCu (μM*h) Cmax (μM) T1/2 (h)< Vdss (L/kg) CL, CLu (mL/min/kg) F% 130, 5.33 34 2.4 0.14 1.6, 39 62

[1]. Ryutaro Kanada, et al. Discovery of DS-9300: A Highly Potent, Selective, and Once-Daily Oral EP300/CBP Histone Acetyltransferase Inhibitor. J Med Chem. 2023 Jan 12;66(1):695-715.