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Chemical Structure : FT-6876
Catalog No.: PC-49860Not For Human Use, Lab Use Only.
FT-6876 (FT 6876) is a potent, selective, orally active CBP/p300 bromodomains inhibitor with IC50 of 5/2 nM, respectively, >500-fold selectivity over BRD4 (IC50=2,320 nM) and other bromodomains.
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FT-6876 (FT6876) is a potent, selective, orally active CBP/p300 bromodomains inhibitor with IC50 of 5/2 nM, respectively, >500-fold selectivity over BRD4 (IC50=2,320 nM) and other bromodomains.
FT-6876 inhibits proliferation of AR+ breast cancer cell line MDA-MB-453 (IC50=197 nM).
FT-6876 also potently inhibits the proliferation of AR+ prostate cancer models including the AR-v7 expressing 22Rv1 cells (IC50=600 nM).
FT-6876 is more than 40 times as potent as enzalutamide against MDA-MB-453 cells and preferentially active against breast cancer cell lines expressing high levels of AR.
FT-6876 (10 uM) induces the rapid reduction of H3K27Ac in MDA-MB-453 cells.
FT-6876 modulates ER and AR target genes in MDA-MB-453 cells.
FT-6876 (30 mg/kg, p.o) induced tumor stasis in this model of AR+ TNBC, with reduction of H3K27 and proliferation index.
| M.Wt | 461.56 | |
| Formula | C27H31N3O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Maureen Caligiuri, et al. Target Oncol. 2023 Feb 24. doi: 10.1007/s11523-023-00949-7.
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