FK866 (APO866, Daporinad)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase)，无细胞试验中IC50为0.09 nM。

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

达珀利奈；Daporinad; APO866; FK-866; FK 866; APO 866; APO-866

White to yellow solid

Ethanol：78 mg/mL (199.22 mM)

NMPRTase

APO866 at low concentrations ranging from 0.09-27 nM induces dose-dependent cytotoxicity in 41 hematologic malignant cells including acute myeloid leukemia , acute lymphoblastic leukemia , mantle cell lymphoma , chronic lymphocytic leukemia , and T-cell lymphoma. APO866 at low concentrations ranging from 0-10 nM induces cell death, this effect is independent of caspase activation but is associated with depolarization of mitochondrial membrane. APO866 at concentrations ranging from 0-10 nM dose-dependently induces depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells. APO866 at concentration of 10 nM inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells.

APO866 administered intraperitoneally at dose of 20 mg/kg twice a day for 4 days, repeat weekly over 3 weeks, prevents and abrogats tumor growth in C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia. APO866 at dose of 0.12 mg/kg/hour prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA.

[1] Nahimana A, et al. Blood, 2009, 113(14), 3276-3286.

[2] Evans L, et al. Arthritis Rheum, 2011, 63(7), 1866-1877.

[3] Olesen UH, et al. Mol Cancer Ther, 2010, 9(6), 1609-1617.

[4] Zoppoli G, et al. Exp Hematol, 2010, 38(11), 979-988.