Daporinad (FK866, APO866)

目录号:S2799

Daporinad (FK866, APO866) Chemical Structure

Molecular Weight(MW): 391.51

Daporinad (FK866, APO866)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。Phase 1/2。

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RMB 737.65 现货
RMB 1405.61 现货
RMB 3025.95 现货
RMB 4662.84 现货
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客户使用Selleck该产品发表文献11篇:

客户使用该产品的6个实验数据:

  • Bar graph showing the effect of the PBEF inhibitor FK866 on PLB-induced autophagy in PC-3 cells. Data are presented as the mean ± SD of three independent experiments. *P<0.05; **P<0.01; and ***P<0.001 by one-way ANOVA.

    Drug Des Devel Ther, 2015, 9: 1511-54. Daporinad (FK866, APO866) purchased from Selleck.

    Effect of metabolic inhibitors on SRC-1 protein levels. A549 cells grown in glucose-containing medium were treated with NAM or FK866 at the indicated concentration.

    Mol Endocrinol 2014 28(3), 395-405. Daporinad (FK866, APO866) purchased from Selleck.

  • Paraffin-embedded tumor sections derived from MiaPaCa-2 were stained with H&E or anti-Ki67 antibodies (Scale bar: 100 μm); apoptotic cells were visualized by TUNEL staining (green) and counterstained with DAPI (blue) (Scale bar: 10 μm). The proliferation index and apoptotic index in tumor sections were also quantified. These animal experiments were repeated once (n = 5mice per treatment group).

    Cancer Lett, 2016, 379(1):1-11.. Daporinad (FK866, APO866) purchased from Selleck.

    Immunofluorescence analysis of Aggrecan and Collagen II expression in NP cells.

    Cell Physiol Biochem, 2018, 49(6):2463-2482. Daporinad (FK866, APO866) purchased from Selleck.

  • Inhibition of NAMPT enzymatic activity decreases osteoclast recruitment in the bone remodeling model. FK866‐loaded osmotic pumps were implanted 48 hr before maxillary‐molar extraction. Rats were sacrificed 4 days after tooth extraction. Osteoclast recruitment and activity were analyzed by TRAP enzymatic staining (a) and quantified (b, c and d). N.Oc/BPm: number of TRAP+ osteoclasts per mm of bone surface, Oc.S:BS (%): resorption surface, N.Nc: mean number of nuclei per osteoclast. Magnification ×200. Boxes are delimited by the first and third quartiles (Q1, Q3) and the line shows the median. Outliers are represented by the extreme values, defined as values lower then Q1—1.5 IQR (Inter Quartile Range) or higher then Q3 + 1.5 IQR. (+) represents the mean, *p ≤ 0.05, **p ≤ 0.01 by the Mann-Whitney U-test.

    J Cell Physiol, 2018, 233(9):7402-7414. Daporinad (FK866, APO866) purchased from Selleck.

    Western blot analysis showing that myelin basic protein (MBP) expression was higher in the NAM group compared to the other three groups at 14 d after stroke induction.

    Neural Plast, 2017, 2017:7019803. Daporinad (FK866, APO866) purchased from Selleck.

产品安全说明书

Transferase抑制剂选择性比较

生物活性

产品描述 Daporinad (FK866, APO866)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。Phase 1/2。
靶点
NMPRTase [5]
(Cell-free assay)
0.4 nM(Ki)
体外研究

APO866在0.09-27 nM的低浓度范围内会在41血液恶性肿瘤细胞中诱导产生细胞毒性,包括急性髓细胞白血病[AML],急性淋巴细胞白血病 [ALL], 套细胞淋巴瘤[MCL], 慢性淋巴细胞白血病[CLL]和 T细胞淋巴瘤,这种毒性具有剂量依赖特性. APO866在0-10 nM的低浓度范围内会诱导细胞死亡,这一效果与线粒体膜去极化有关而与半胱天冬酶的激活无关。APO866在0-10 nM的浓度范围内会诱导胞内NAD 和 ATP 的损耗和多种血液肿瘤细胞的死亡,这一效果具有剂量依赖特性[1] 。10 nM APO866 会抑制HFFF2细胞内 PBEF诱导的 MMP-3, CCL2和CXCL8 的分泌 [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SH-SY5Y cells Ml[xR5l1d3SxeHnjxsBie3OjeR?= NXrae5VJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0hvU2m1XUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZidH;0ZYwh[2WubIXsZZIhVkGGKGCpJIxmfmWuLDDJR|UxRTBwNTDuUS=> MYKxPVk3OTF6Mx?=
human A2780 cells NWDyfoF7WHKxbHnm[ZJifGmxbjDhd5NigQ>? M1\6SFczKGh? NWP2[IppSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NF0yKG6P NXGxTm04OjR2MEW0NVk>
human NYH cells NYfjSmJPS3m2b4TvfIlkyqCjc4PhfS=> M3\3XlMhf2Wna4O= M2LSV2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5[UCClZXzsd{Bi\nSncjCzJJdm\Wu|IHL5JINtd26xZ3XubYMhe3W{dnn2ZYwh[XO|YYmsJGlEPTB;MT61JI5O M323RlI{Pjd7OUG1
human HepG2 cells NIjKXW1HfW6ldHnvckBie3OjeR?= MVixJIg> NFjveXNKdmirYnn0bY9vKG:oIF7BUXBVKGmwIHj1cYFvKEincFeyJINmdGy|IIXzbY5oKFtzNFPdMY5q[2:2aX7hcYll\S:SUmDQJIF{KHO3YoP0doF1\SCjc4Pld5Nm\CCjczDmc5Ju[XSrb36gc4YhYzF2Q22tcolkd3SrbnHtbYRmKG2xbn;ueYNt\W:2aXTlJIFnfGW{IEGgbJIh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegZY5idHm|aYOsJGlEPTB;Mj6yJI5O NYrJSIRuOjRzNkSwPFY>
human PC3 cells MVHDfZRwfG:6aXRCpIF{e2G7 MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZpkh[2yxbn;n[Y5q[yCjc4PhfUwhUUN3ME2zMlghdk1? NHWzZ5EzPDF4NEC4Oi=>
human A431 cells NGLHTXNEgXSxdH;4bYPDqGG|c3H5 Mlj6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVYvOSCwTR?= NEDlfFczPDF4NEC4Oi=>
human K562 cells NHj5TYJEgXSxdH;4bYPDqGG|c3H5 MX25OkBp NWrVVIdOS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVcvOiCwTR?= NELmVWgzOzZ5OUmxOS=>
human MCF-7 cells NGDl[odEgXSxdH;4bYPDqGG|c3H5 NVux[IRsPzJiaB?= MlPQR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHNTdiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxRTdwNDDuUS=> NHL1PWMzPDF4NEC4Oi=>
human HCT116 cells M2PmUWN6fG:2b4jpZ:Kh[XO|YYm= M4fLT|czKGh? MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KFeVVD2xJIF{e2G7LDDJR|UxRTFyLkmgcm0> MmPtNlQyPjRyOE[=
human HT1080 cells NX60UlJbS3m2b4TvfIlkyqCjc4PhfS=> MmjUOkBl[Xm| NFmwXZVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXDFyOECgZ4VtdHNiYX\0[ZIhPiCmYYnzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjF4IN88US=> MliyNlE{OzByMUW=
human HCT116 cells NHTUfoNEgXSxdH;4bYPDqGG|c3H5 MoDIOkBl[Xm| M2DDV2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA3KGSjeYOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOTZizszN NXHoTlhZOjF|M{CwNVU>
human A549 cells NVvOSZhPS3m2b4TvfIlkyqCjc4PhfS=> NWfLS|JrPiCmYYnz MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IE[g[IF6eyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6xOkDPxE1? MkXvNlE{OzByMUW=
human SNU638 cells NUP4b4Q4S3m2b4TvfIlkyqCjc4PhfS=> MkTZOkBl[Xm| NI\OeXBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUVlV4M{igZ4VtdHNiYX\0[ZIhPiCmYYnzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjF4IN88US=> NVXwfYNpOjF|M{CwNVU>
human SKOV3 cells MlfXR5l1d3SxeHnjxsBie3OjeR?= NIi0UYJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyCkeTDjcI9vd2enbnnjJIF{e2G7LDDJR|UxRTJzMTDuUS=> NY\DRZc1OjRzNkSwPFY>
human MCF7 cells NUC2RZZETnWwY4Tpc44h[XO|YYm= Mm\aNVAh|ryP NUW0eoRpPiCmYYnz MoPkRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDheEAyOCC3TTDh[pRmeiB4IHThfZMh[nliU2LCJIF{e2G7LDDJR|UxRTBwNkig{txO Ml;UNlE{OzByMUW=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
SIRT1; 

PubMed: 29905535     


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     


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     


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     


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     


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     


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     


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
体内研究 用C.B.-17 SCID 小鼠建立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,腹腔注射APO866 ,一天两次,一次20 mg/kg 一周4天, 重复三周以上可以抑制肿瘤生长。 [1]对于携带CIA的小鼠, 0.12 mg/kg/小时剂量的 APO866 可以通过抑制PBEF 来防止关节破坏和白细胞浸润[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

+ 展开
  • Cell lines: 41血液恶性肿瘤细胞系
  • Concentrations: 0 - 10 nM
  • Incubation Time: 72 小时或 96小时
  • Method:

    MTT 分析流程, 细胞按每毫升0.5 &time 106 个的密度接种到96孔板,接种三份。将APO866 (0.01 nM-100 nM) 加到50 μL 培养基中, 空白培养基作为对照。 孵育 72或 96 小时后每孔加入15 μL 染料溶液继续孵育 4 小时。 然后每孔加入100 μL 终止液孵育 1小时,用分光光度计测量570 nm 处吸光度。台盼蓝染色分析流程, 细胞按每孔0.5 &time105 个接种到6孔板,每孔加入1 mL培养基,在含有或缺少 APO866的情况下孵育 96 小时。 每孔取10μL 细胞样品与10 μL 台盼蓝孵育1分钟(体积比1:1)。细胞存活情况通过计算未染色的细胞个数来获得。


    (Only for Reference)
动物实验:

[1]

+ 展开
  • Animal Models: 人急性髓细胞白血病,淋巴瘤以及白血病的C.B.-17 SCID 小鼠异种移植模型
  • Formulation: 用0.9% 生理盐水配制
  • Dosages: 20 mg/kg
  • Administration: 腹腔注射一天两次,连续四天,重复3周以上
    (Only for Reference)

溶解度 (25°C)

体外 Ethanol 78 mg/mL (199.22 mM)
DMSO Insoluble
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
45% Propylene glycol (dissolve first)+5% Tween 80+ddH2O
15mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 391.51
化学式

C24H29N3O2

CAS号 658084-64-1
储存条件 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00435084 Completed B-cell Chronic Lymphocytic Leukemia Onxeo February 2007 Phase 1|Phase 2
NCT00431912 Completed Cutaneous T-cell Lymphoma Onxeo February 2007 Phase 2
NCT00435084 Completed B-cell Chronic Lymphocytic Leukemia Onxeo February 2007 Phase 1|Phase 2
NCT00431912 Completed Cutaneous T-cell Lymphoma Onxeo February 2007 Phase 2
NCT00432107 Completed Melanoma Onxeo July 2006 Phase 2
NCT00432107 Completed Melanoma Onxeo July 2006 Phase 2

技术支持

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    We are considering the use of S2799 for in vivo injections, Any suggestions for the formula?

  • 回答:

    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.

Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID