Daporinad (FK866, APO866)

Name: Daporinad (FK866, APO866)
Brand: Selleck Chemicals
SKU: S2799
Rating: 5 (33 reviews)

For research use only.

Catalog No.S2799

33 publications

Daporinad (FK866, APO866) Chemical Structure

CAS No. 658084-64-1

Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with IC50 of 0.09 nM in a cell-free assay. Daporinad (FK866, APO866) triggers autophagy. Phase 1/2.

Selleck's Daporinad (FK866, APO866) has been cited by 33 publications

Cell Metab, 2020, 31(3):564-579

PubMed: 32130883 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Nat Biotechnol, 2017, 35(5):463-474

PubMed: 28319085 ( click the link to review the publication )

Cancer Discov, 2016, 6(7):727-39

PubMed: 27231123 ( click the link to review the publication )

Biomed Pharmacother, 2021, 140:111693

PubMed: 34029951 ( click the link to review the publication )

Oncol Lett, 2021, 21(5):390

PubMed: 33777213 ( click the link to review the publication )

Genome Med, 2021, 13(1):28

PubMed: 33593430 ( click the link to review the publication )

Mol Ther, 2020, S1525-0016(20)30482-2

PubMed: 33002419 ( click the link to review the publication )

Mol Ther Nucleic Acids, 2020, 1;20:801-811

PubMed: 32438315 ( click the link to review the publication )

Front Cell Dev Biol, 2020, 17;8:191

PubMed: 32363189 ( click the link to review the publication )

Oxid Med Cell Longev, 2020, 2020:7308386

PubMed: 33149812 ( click the link to review the publication )

Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669

PubMed: 32238439 ( click the link to review the publication )

Cell Microbiol, 2020, 22(1):e13115

PubMed: 31509891 ( click the link to review the publication )

Toxicol In Vitro, 2020, 65:104808

PubMed: 32087266 ( click the link to review the publication )

Cell Commun Signal, 2020, 18(1):16

PubMed: 32005247 ( click the link to review the publication )

Leukemia, 2020, 10.1038/s41375-019-0692-5

PubMed: 31896781 ( click the link to review the publication )

Nat Commun, 2019, 10(1):3790

PubMed: 31439867 ( click the link to review the publication )

Cancers (Basel), 2019, 11(12)

PubMed: 31795447 ( click the link to review the publication )

J Cell Physiol, 2019, 10.1002/jcp.28910

PubMed: 31141164 ( click the link to review the publication )

Life Sci, 2019, 225:20-28

PubMed: 30928408 ( click the link to review the publication )

Mol Psychiatry, 2018, 10.1038/s41380-018-0061-1

PubMed: 29728703 ( click the link to review the publication )

Nat Commun, 2018, 9(1):502

PubMed: 29402884 ( click the link to review the publication )

Cell chemical biology, 2018, 10.1016/j.chembiol.2017.12.008

PubMed: 29307841 ( click the link to review the publication )
Cell Physiol Biochem, 2018, 49(6):2463-2482

PubMed: 30261504 ( click the link to review the publication )

J Cell Physiol, 2018, 233(9):7402-7414

PubMed: 29663373 ( click the link to review the publication )

Mol Med Rep, 2018, 17(4):6163-6173

PubMed: 29436637 ( click the link to review the publication )

Neural Plast, 2017, 2017:7019803

PubMed: 28656112 ( click the link to review the publication )

Cancer Lett, 2016, 379(1):1-11

PubMed: 27233476 ( click the link to review the publication )

Drug Des Devel Ther, 2015, 9:1555-84

PubMed: 25792811 ( click the link to review the publication )

Drug Des Devel Ther, 2015, 10.2147/DDDT.S75976

PubMed: ( click the link to review the publication )

Mol Endocrinol, 2014, 28(3):395-405

PubMed: 24438340 ( click the link to review the publication )

PLoS One, 2014, 9(10):e111146

PubMed: 25343454 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Transferase Inhibitors

Biological Activity

Description

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. ^[1] APO866 at concentration of 10 nM inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells. ^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
SH-SY5Y	NIf3U5NEgXSxdH;4bYNqfHliYYPzZZk>			MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDv[kB1d3SjbDDj[YxtfWyjcjDORWQpWClibHX2[YwtKEmFNUCgQUAxNjByMEWg{txONg>?	NEDPUnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUm2NVE5Oyd-MUm5OlEyQDN:L3G+
SH-SY5Y	NF3lVHpEgXSxdH;4bYNqfHliYYPzZZk>		M1TVb\|Q5KGi{cx?=	Mn3iR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2guW1l3WTDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5yMEG3JO69VS5?	M2DGU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OU[xNVg{Lz5zOUm2NVE5OzxxYU6=
HT1080	MkLrR5l1d3SxeHnjbZR6KGG\|c3H5		NIn3NXU3KGSjeYO=	NU\hNnJNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRzMEiwJINmdGy\|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkG2JO69VS5?	M3vKWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{OwNFE2Lz5{MUOzNFAyPTxxYU6=
A549	NY[xcndFS3m2b4TvfIlkcXS7IHHzd4F6		NYPjeJNNPiCmYYnz	M4HJZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgOkBl[Xm\|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOTZizszNMi=>	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN\|MECxOUc,OjF\|M{CwNVU9N2F-
HCT116	M1PFcWN6fG:2b4jpZ4l1gSCjc4PhfS=>		M1j5WVYh\GG7cx?=	MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOkBl[Xm\|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOTZizszNMi=>	MmmzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF\|M{CwNVUoRjJzM{OwNFE2RC:jPh?=
SNU638	M{TIZWN6fG:2b4jpZ4l1gSCjc4PhfS=>		NHLi[pk3KGSjeYO=	Ml36R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25WPjN6IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjF4IN88UU4>	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN\|MECxOUc,OjF\|M{CwNVU9N2F-
MCF7	M4LjfWFvfGm2dX3vdkBie3OjeR?=	NITBTJUyOCC3TR?=	MX[2JIRigXN?	NYe5fHlGSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BifCBzMDD1UUBi\nSncjC2JIRigXNiYomgV3JDKGG\|c3H5MEBKSzVyIE2gNE43QCEQvF2u	Mm\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF\|M{CwNVUoRjJzM{OwNFE2RC:jPh?=
K562	NVXhXYZKS3m2b4TvfIlkcXS7IHHzd4F6		NGnlNJc3KGSjeYO=	MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IE[g[IF6eyCkeTDTVmIh[XO\|YYmsJGlEPTBiPTCyNEDPxE1w	M1;YOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{OwNFE2Lz5{MUOzNFAyPTxxYU6=
A2780	M4rVZWN6fG:2b4jpZ4l1gSCjc4PhfS=>		MUC3NkBpenN?	MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG\|c3H5MEBKSzVyIE2gNE4xODFizszNMi=>	NGDac\|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xO\|c5PCd-MkO2NVc4QDR:L3G+
NYH	NF31eJlEgXSxdH;4bYNqfHliYYPzZZk>		MlnwN{B4\WWtcx?=	NX3Y[ZVVS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVlmKIHPlcIx{KGGodHXyJFMhf2Wna4OgZpkh[2yxbn;n[Y5q[yC\|dYL2bZZidCCjc4PhfUwhVER3MDC9JFAvODBzNTFOwG0v	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5OUmxOUc,OjN4N{m5NVU9N2F-
K562	NUfZUGh3S3m2b4TvfIlkcXS7IHHzd4F6		NYPOR5JnQTZiaILz	NI\wcFhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjByN{Kg{txONg>?	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5OUmxOUc,OjN4N{m5NVU9N2F-
A2780	NXTwOZcxSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NEjUNXU4OiCqcoO=	M2H4RmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO\|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO\|IhcHK\|IHL5JHNTSi2kYYPl[EBucWO{b4DsZZRmKHKnYXTldkBidmGueYPpd{whUUN3MDC9JFAvODBzIN88UU4>	NUX3SpZnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVkyOThpPkKzPFU6OTF6PD;hQi=>
NYH	NHfjS3dEgXSxdH;4bYNqfHliYYPzZZk>			MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOXWgh[2WubIOgZpkh[2yxbn;n[Y5q[yCjc4PhfUwhUUN3MDC9JFAvODBzNTFOwG0v	Mnv6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
A2780	M{HVW2N6fG:2b4jpZ4l1gSCjc4PhfS=>		NVrWcHFvPzJiaILz	NFXyU41EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO\|YYmsJGlEPTBiPTCwMlAxOTZizszNMi=>	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
HepG2	NXTyWm9WTnWwY4Tpc44h[XO\|YYm=		MmraNUBpeg>?	NWe1ZWdqUW6qaXLpeIlwdiCxZjDORW1RXCCrbjDoeY1idiCKZYDHNkBk\WyuczD1d4lv\yCdMUTDYU1vcWOxdHnuZY1q\GVxUGLQVEBieyC\|dXLzeJJifGViYYPz[ZN{\WRiYYOg[o9zdWG2aX;uJI9nKFtzNFPdMY5q[2:2aX7hcYll\SCvb37vcpVkdGWxdHnk[UBi\nSncjCxJIhzKGK7IHzpdZVq\CC\|Y3nueIltdGG2aX;uJINwfW62aX7nJIFv[Wy7c3nzMEBKSzVyIE2gNE4xODJ{IN88UU4>	NVS2NY9zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
PC3	M2nVU2N6fG:2b4jpZ4l1gSCjc4PhfS=>			MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR\|Mh[2WubIOgZpkh[2yxbn;n[Y5q[yCjc4PhfUwhUUN3MDC9JFAvODB\|ODFOwG0v	Mn;6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
A2780	MWHDfZRwfG:6aXPpeJkh[XO\|YYm=			M2\RXWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVAhRSByLkCwOVch\|ryPLh?=	M3f2dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
A431	NH\z[FdEgXSxdH;4bYNqfHliYYPzZZk>			MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJIJ6KGOub37v[4VvcWNiYYPzZZktKEmFNUCgQUAxNjByNkGg{txONg>?	NGXJN\|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
MCF-7	MnLqR5l1d3SxeHnjbZR6KGG\|c3H5		M1e1cVczKGi{cx?=	MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2YuPyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVAhRSByLkCwO\|Qh\|ryPLh?=	M1PkOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
MCF7	NWrreHE1S3m2b4TvfIlkcXS7IHHzd4F6			NIWyUm9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVAhRSByLkCwPFQh\|ryPLh?=	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
HCT116	NXX5S21JS3m2b4TvfIlkcXS7IHHzd4F6		NGjnVIo4OiCqcoO=	NYm3PZZNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy\|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDXV3QuOSCjc4PhfUwhUUN3MDC9JFAvODFyOTFOwG0v	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF4NEC4Okc,OjRzNkSwPFY9N2F-
SKOV3	M3PwSmN6fG:2b4jpZ4l1gSCjc4PhfS=>			NWOydFI5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNiYomgZ4xwdm:pZX7pZ{Bie3OjeTygTWM2OCB;IECuNlEyKM7:TT6=	M3\vclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
HCT116	NYrBNVJJS3m2b4TvfIlkcXS7IHHzd4F6		MWq3NkBpenN?	M2rMdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEGST{i2Ok1z\XOrc4ThcpQhcHWvYX6gTGNVOTF4IHPlcIx{KGG\|c3Xzd4VlKGG\|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OCB;IECuPVQ3KM7:TT6=	NI[w[GE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
A2780	M17GXmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NVHjd2dxPzJiaILz	NHOwWJVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO\|gxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIHHzd4F6NCCLQ{WwJF0hOC5yMEGg{txONg>?	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRyNUSxPUc,OjR2MEW0NVk9N2F-
A2780	NHX4e3hHfW6ldHnvckBie3OjeR?=		M1PSe\|czKGi{cx?=	M3HETWlvcGmkaYTpc44hd2ZiTlHNVHQhcW5iaIXtZY4hSTJ5OECgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OCB;IECuNFAyKM7:TT6=	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUK3NUc,Ojd3NEGyO\|E9N2F-
DE3	NVG0VZdwTnWwY4Tpc44h[XO\|YYm=		NWrnbWJOOTVibXnudy=>	NFGwNmpKdmirYnn0bY9vKG:oIHj1cYFvKG[3bHygcIVv\3SqIFOteIVzdWmwYXygTIl{Pi22YXfn[YQhVkGPUGSg[ZhxemW\|c3XkJIlvKEW\|Y3jldolkcGmjIHPvcIkhWm:\|ZYT0ZUApTEV\|KTDj[YxteyC3c3nu[{BvcWOxdHnuZY1q\GViYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiMUWgcYlveyCycnnvdkB1dyC\|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BqdiCycnXz[Y5k\SCxZjDQVnBRNCCLQ{WwJF0hOC5yMEOg{txONg>?	NFzaOIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVI4OSd-Mke1OFEzPzF:L3G+
SH-SY5Y	Mm\wR5l1d3SxeHnjbZR6KGG\|c3H5		M2\x[VU3KGi{cx?=	NEDjR5dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC1OkBpenNiYomgUXRVKGG\|c3H5MEBGSzVyIE2gNE4xODN2IN88UU4>	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF4NUe0Nkc,OjhzNkW3OFI9N2F-
A2780	M2rpfWN6fG:2b4jpZ4l1gSCjc4PhfS=>			M2XqTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTygTWM2OCB;IECuNFA1OiEQvF2u	NESyUo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG2OVc1Oid-MkixOlU4PDJ:L3G+
PC3	NIH3XVhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NEK2dnk2KGSjeYO=	M2HGOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBqdmO3YnH0[YQh\m:{IEWg[IF6eyCkeTDD[YxtNXSrdHXyJGdtdyC{ZXHn[Y51KGKjc3XkJIF{e2G7LDDJR\|UxKD1iMD6wNFU4KM7:TT6=	NXf2SGdFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2NVA6QDRpPkK4OlExQTh2PD;hQi=>
HepG2	MnXNR5l1d3SxeHnjbZR6KGG\|c3H5		MU[3NkBpenN?	MVfDfZRwfG:6aXPpeJkhcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCwMlg6KM7:TT6=	NVO3SJF1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4PFU5OzRpPkK4PFg2QDN2PD;hQi=>
MDA-MB-231	MlHsR5l1d3SxeHnjbZR6KGG\|c3H5		NHjIXVQ4OiCqcoO=	NXj2eooxS3m2b4TvfIlkcXS7IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCxMlMh\|ryPLh?=	NHe1Oo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi4OVg{PCd-Mki4PFU5OzR:L3G+
HCT116	NGXpeI1EgXSxdH;4bYNqfHliYYPzZZk>		NHrpVWM4OiCqcoO=	Ml\rR5l1d3SxeHnjbZR6KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFEvPiEQvF2u	NEPsUoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEi4OVg{PCd-Mki4PFU5OzR:L3G+
HepG2	M3nqUmN6fG:2b4jpZ4l1gSCjc4PhfS=>		MXK3NkBpenN?	MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjh7IN88UU4>	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTN2OEiwPEc,Ojl\|NEi4NFg9N2F-
HCT116	NUfJN\|ZlS3m2b4TvfIlkcXS7IHHzd4F6		NGf3NWM4OiCqcoO=	M{CycWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLk[g{txONg>?	NYDHWIxRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzOFg5ODhpPkK5N\|Q5QDB6PD;hQi=>
A549	NIPuN4JEgXSxdH;4bYNqfHliYYPzZZk>		MnLSO\|IhcHK\|	Mmq5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUA{NjdizszNMi=>	NWrMXY41RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzOFg5ODhpPkK5N\|Q5QDB6PD;hQi=>
SH-SY5Y	MorMRZV1d3CqYXf5JIF{e2G7		NHP3dos1OCCqcoO=	NH7LV5ZKdmS3Y4Tpc44hd2ZiYYX0c5Bp[We7IHnuJIh2dWGwIGPIMXN[PVliY3XscJMh[XO\|ZYPz[YQh[XNiTFOzM5Bpd3OyaH;0bYR6dGW2aHHuc4xidWmwZTDjc5VxdGmwZzDh[pRmeiB2MDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	M1TB[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OU[xNVg{Lz5zOUm2NVE5OzxxYU6=
MCF7	NXr1OHVnSW62aYT1cY9zKGG\|c3H5		NFz2NYI3KGSjeYO=	NF60bmZCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IE[g[IF6eyCkeTDTVmIh[XO\|YYm=	NVfTdHZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzN\|AxOTVpPkKxN\|MxODF3PD;hQi=>
MDCK	M13sSmZ2dmO2aX;uJIF{e2G7	M2\jelExKHWP		M{exd2FxeGG{ZX70JJBmem2nYXLpcIl1gSCjY4Lvd5Mh[XCrY3HsJJRwKGKjc3;sZZRmemGuIIPp[IUhcW5iZH;nJG1FS0tiY3XscJMh[XRiMUCgeW0h[nliTFOtUXMwVVNiYX7hcJl{cXN?	M{m4UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OEW5NVE5Lz5{M{i1PVEyQDxxYU6=
DU145	NHPEb3hEgXSxdH;4bYNqfHliYYPzZZk>			NG\UZ2REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCkeTDjcI9vd2enbnnjJIF{e2G7	M{HmbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MU[0NFg3Lz5{NEG2OFA5PjxxYU6=
MCF7	NX\J[GVmS3m2b4TvfIlkcXS7IHHzd4F6		NYnneplUQTZiaILz	M37CU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JINtd26xZ3XubYMh[XO\|YYm=	NWnoT3lVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
HCT116	NYrvRYM3TnWwY4Tpc44h[XO\|YYm=			MVfS[ZNqe3SjbnPlJIZi[3SxcjygdoF1cW9ib3[gTWM2OCCob4KgRXBQQDZ4LYLld4l{fGGwdDDoeY1idiCKQ2SxNVYh[2WubIOgeI8hUUN3MDDmc5IhcHWvYX6gTGNVOTF4IHPlcIx{	Ml7xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
A2780	NYTBTI95SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NFrBb3M4OiCqcoO=	M1rrUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUK3PFAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZkhcW5icILld4Vv[2Vib3[gcolkd3SrbnHtbYRmKG2xbn;ueYNt\W:2aXTl	M332WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEC1OFE6Lz5{NESwOVQyQTxxYU6=
Sf9	MlPjSpVv[3Srb36gZZN{[Xl?		NELNb3A{OCCvaX7z	NHnGUIxKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKGi3bXHuJGMufGW{bXnuZYwhUGm\|L3\sZYcufGGpZ3XkJGhFSUNzIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVZkmgbY5{\WO2IHPlcIx{KGGodHXyJFMxKG2rboOgZpkh\my3b4Lld4NmdmOnIHHzd4F6	NYHkWnh7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzOFg5ODhpPkK5N\|Q5QDB6PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	SIRT1; PubMed: 29905535 Aging (Albany NY) Human retinal pigment epithelial cells (ARPE-19) were treated with different doses (0.01-10μM) of FK866 and expression of SIRT1 was evaluated by western blotting. p-AMPK / AMPK / p-EIF2A / EIF2A / p-4EBP1 / 4EBP1; PubMed: 29541451 Cancer Metab CEM PA cells were treated with 5 and 100 nM FK866 for 48 h. Western blot showing expression of AMPK, mTOR, 4EBP1, and EIF2A in CEM PA cells. AKT / pAKT(Ser-473) / mTOR / p-mTOR(Ser-2448); PubMed: 26542945 BMC Cancer Jurkat cells were treated for 48 h with or without (Mock) the indicated concentration of FK866. Thereafter, cells were lysed and the levels of total and p-Akt (Ser-473), total and p-MTOR (Ser-2448), total and p-4EBP1 (Ser-65 and Thr-70).	29905535 29541451 26542945
Immunofluorescence	pMLKL; PubMed: 29996103 Cell Rep Immunofluorescence for pMLKL (monoclonal pMLKL antibody, red, phospho S358) and nuclei (DAPI, blue) in THP-1 cells treated with the indicated concentrations of FK866 for 6 hr. Scale bars, 10 μm. phGSK3β; PubMed: 22207684 Haematologica Representative DUOLINK images of phospho-GSK3β (Ser9) protein expression in HL60 cells treated with 10 nM of FK866 for 96 h or 100 nM of AC93253 for 48 h, or with DMSO as a control. ph-β-catenin ; PubMed: 22207684 Haematologica Representative images of inactive phospho-β-catenin (Ser33/37) protein expression in HL60 cells treated with 10 nM of FK866, 100 nM of AC93253 or DMSO as a control	29996103 22207684
Growth inhibition assay	Cell viability ; PubMed: 27462772 Oncotarget Twenty-three PDAC-derived PCCs were treated for 72 h with increasing concentrations of FK866 ranging from 0 to 1000 nM. The horizontal dotted line indicates 50% cell viability. PCCs with the highest sensitivity are highlighted by a blue line and those wit䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ	27462772

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. ^[1] APO866 at dose of 0.12 mg/kg/hour prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA. ^[2]

Protocol

Cell Research:

^[1]

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Cell lines: 41 hematologic malignant cell lines
Concentrations: 0 - 10 nM
Incubation Time: 72 hours or 96 hours
Method:
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)

Animal Research:

^[1]

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Animal Models: C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.
Dosages: 20 mg/kg
Administration: administered intraperitoneally twice a day for 4 days, repeated weekly over 3 weeks
(Only for Reference)

References

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Solubility (25°C)

In vitro	Ethanol	78 mg/mL (199.22 mM)
	DMSO	Insoluble
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O For best results, use promptly after mixing.	4mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Daporinad (FK866, APO866) SDF

Molecular Weight	391.51
Formula	C₂₄H₂₉N₃O₂
CAS No.	658084-64-1
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	C1CN(CCC1CCCCNC(=O)C=CC2=CN=CC=C2)C(=O)C3=CC=CC=C3

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00435084	Completed	Drug: APO866	B-cell Chronic Lymphocytic Leukemia	Onxeo	February 2007	Phase 1\|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
We are considering the use of S2799 for in vivo injections, Any suggestions for the formula?
Answer:
The vehicle we recommend for S2799 in vivo study is 45% Propylene glycol (dissolve first) +5% Tween 80+ddH2O. You can dissolve the compound in Propylene glycol first and then dilute with water with Tween 80. The solution is clear and can be used for injection.

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Daporinad (FK866, APO866)