[CAS NO. 658084-64-1] Daporinad

Name: Daporinad
Brand: Arctom Scientific
SKU: SLK-S2799

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PRODUCTS SPECIFICATIONS [658084-64-1]

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Catalog

SLK-S2799

Brand

Selleck

CAS

658084-64-1

DESCRIPTION [658084-64-1]

Overview

MDL	MFCD10565943
Molecular Weight	391.51
Molecular Formula	C24H29N3O2
SMILES	C(=O)(N1CCC(CCCCNC(/C=C/C=2C=CC=NC2)=O)CC1)C3=CC=CC=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.5542 mL	12.7711 mL	25.5421 mL
5 mM	0.5108 mL	2.5542 mL	5.1084 mL
10 mM	0.2554 mL	1.2771 mL	2.5542 mL
50 mM	0.0511 mL	0.2554 mL	0.5108 mL

Description

Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase () with of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers . Phase 1/2.

Targets

NMPRTase ^[5]
(Cell-free assay)

0.4 nM(Ki)

In vitro

APO866 at low concentrations ranging from 0.09-27 nM induces dose-dependent cytotoxicity in 41 hematologic malignant cells including acute myeloid leukemia [AML], acute lymphoblastic leukemia [ALL], mantle cell lymphoma [MCL], chronic lymphocytic leukemia [CLL], 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.

In vivo

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.

References

[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.
[5] Hasmann M, et al. Cancer Res. 2003 , 63(21):7436-42.

Synonyms

2-Propenamide, N-[4-(1-benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-, (2E)-

(2E)-N-[4-(1-Benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2-propenamide

FK 866

K 22.175

APO 866