(E)-Daporinad 是一种烟酰胺磷酸核糖基转移酶的小分子抑制剂，具有潜在的抗肿瘤和抗血管生成活性，IC50为 0.09 nM。

Daporinad is a small molecule inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase), with potential antineoplastic and antiangiogenic activities.

对于携带CIA的小鼠, APO866（0.12 mg/kg）可以改善关节破坏和白细胞浸润.C.B.-17 SCID小鼠的人急性髓细胞白血病,淋巴母细胞淋巴瘤和白血病的异种移植模型中,腹腔注射APO866（20 mg/kg ）,能够抑制肿瘤生长.

在多种血液恶性肿瘤细胞中,APO866（0.09-27 nM）通过诱导胞内NAD 和 ATP 的损耗,能够以剂量依赖的方式诱导产生细胞毒性活性。在HFFF2细胞内, APO866（10 nM）能够抑制前B细胞克隆增强因子诱导的MMP-3, CCL2和CXCL8 的分泌。

High Throughput Screening: FITC-MBM1 at 15 nM and menin at 150 nM in the FP buffer are mixed and incubated for 1h in the dark at room temperature. For point screening, the 0.2 μL of each compound (20 μM final concentration, 1% DMSO) is added to 20 μL of the aliquot of the protein-peptide mixture and incubated on 384-well plates in the dark at room temperature for 1h. In confirmation screening, the serial dilution plates with compounds in DMSO are prepared and used to titrate the menin-FITC-MBM1 complex. Change in fluorescence polarization is monitored at 525 nm after excitations at 495 nm using the PHERAstar microplate reader (BMG) and applied to determine IC50 values with the Origin 7.0 program.

For MTT assays, 0.5 × 106 cells/mL is plated in triplicate on 96-well plates. APO866 (0.01 nM-100 nM) is added in 50 μL of culture medium, with culture medium alone serving as control. After 72 or 96 hours of incubation, 15 μL of dye solution is added to each well and cells are incubated for an additional 4 hours. Stop solution (100 μL/well) is added for 1 hour and the absorbance is read at 570 nm on a spectrophotometer. For trypan blue dye exclusion staining, 0.5 × 105 cells/well is grown in 6-well plates with 1 mL media in the absence or presence of APO866 for 96 hours. Cells from each sample are incubated with 10 μL trypan blue solution (at a 1:1 ratio [vol/vol] for 1 minute). Cell survival is determined by calculating proportion of live (unstained) cells. (Only for Reference)

658084-64-1

C24H29N3O2

391.515

(E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE;APO866;FK866;达珀利奈;Daporinad

Ethanol:72 mg/mL (183.9 mM)
DMSO:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years