P300/CBP-IN-5

P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC50 of 18.8 nM[1].

Research Areas >> Cancer

IC50: 18.8 nM (p300/CBP)[1]

P300/CBP-IN-5 inhibits p300 LnCap-FGC cellls proliferation with an IC50 of 14.8 nM. P300/CBP-IN-5 inhibits H3K27Ac with an IC50 value of 4.6 nM in PC-3 cells[1].

The effect of P300/CBP-IN-5 (Example 715) on tumor growth is evaluated in subcutaneous, SuDHL-8 (B-cell lymphoma) and 22RV1 (prostate) xenograft tumors implanted in SCID female mice. Human cancer cells are inoculated subcutaneously into the right hind flank of female SCID mice on study day 0. Administration of P300/CBP-IN-5 (7.5 mg/kg/day) is initiated at the time of size match. P300/CBP-IN-5 induces significant tumor growth inhibition in multiple xenograft tumor models (the tumor growth inhibition of 62% in SuDHL-8 xenograft tumor model; 48% in 22RV1 xenograft tumor model)[1].

[1]. Michael Michaelides, et al. Spirocyclic hat inhibitors and methods for their use. WO2016044770A1.