Fimepinostat_product_DataBase

Bioactivity

Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.

Invitro

Fimepinostat is a potent pan-inhibitor of HDAC classes I and II enzymes and observed that its potency against class I HDACs is similar to that of LBH589 and greater than that of SAHA. Fimepinostat is also a potent inhibitor of class I PI3K kinases with an IC50 of 19, 54, and 39 nM for PI3Kα, PI3Kβ, and PI3Kδ, respectively. Fimepinostat markedly induces p21 protein in H460, a non-small cell lung cancer (NSCLC) cell line. Fimepinostat causes the reduction of both p-STAT3 (Y-705) and p-SRC in RPMI-8226 multiple myeloma cells and reduces both phosphorylated and total protein levels of MET and EGFR as well as HER2 and HER3 in H1975 NSCLC cells and BT-474 breast cancer cells, respectively. Fimepinostat induces caspase-3 and -7 activation in HCT-116 colon cancer cells in a dose-dependent manner. Fimepinostat potently inhibits the growth of cancer cells derived from both hematologic and solid tumors. Fimepinostat potently inhibits the proliferation of cells expressing either mutant or wild-type PI3K[1].

Name

Fimepinostat

CAS

1339928-25-4

Formula

C23H24N8O4S

Molar Mass

508.55

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

PeptideDB

Fimepinostat

CAS: 1339928-25-4 F: C23H24N8O4S W: 508.55