XAV-939 化学構造
分子量: 312.31

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製品説明

  • Compare Wnt/beta-catenin Inhibitors
    Wnt/beta-catenin製品生物活性の比較
  • 研究分野
  • XAV-939のメカニズム

製品の説明

生物活性

製品説明 XAV-939 は小分子選択阻害剤、Wnt通路転写因子β- catenin調節の転写を抑制、TNKS1 と TNKS2を作用すると、 IC50 がそれぞれ 11 nM 、 4 nMとなる.
ターゲット TNKS1 TNKS2
IC50 11 nM 4 nM [1]
In vitro試験 XAV-939 specifically inhibits tankyrase PARP activity. XAV-939 dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 μM XAV-939 exposure. Treatment of human lymphoblasts with 1.0 μM XAV-939 results in marked elevation of tankyrase 1 levels. [1] XAV-939 is axin stabilizing agent. XAV-939 stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. XAV-939 stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. XAV-939 deregulates the Wnt/b-catenin pathway which has been implicated in many cancers. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Sf-21 NFr0ZnlMcW6jc3WgRZN{[Xl? MnnXNVgvPzVizszN M17VO|YxKG2rbh?= MmLySG1UVw>? MkDOTY5pcWKrdHnvckBw\iCQLYTldo1qdmGuIFfTWE11[WepZXSgWG5MWzJiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjByNUOg{txO MW[yN|g4QTR|MR?=
HEK293T NVzme2k5TnWwY4Tpc44hSXO|YYm= M13DZ2ROW09? MU\Jcohq[mm2aX;uJI9nKFewdDDzbYdv[WyrbnegZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDmc5J{c2:uaX6tbY5lfWOnZDDjRW1RKHKnc4DvcpNmKGWuZX3lcpQh[WO2aY\heIlwdiC5aYToJGlEPTBib3[gNE4xPzhizszN M{LtdlI{QDd7NEOx
HEK293T NYXBZ2FsTnWwY4Tpc44hSXO|YYm= NXHVOVJ[OTBizszN MknWSG1UVw>? NHq4dXZKdmirYnn0bY9vKG:oIHLleIEu[2G|ZXnuMYRmeGWwZHXueEBk[W6xbnnjZYwhX262MzDwZZRpf2G7IIfpeIghUUN3MDDv[kAxNjB3MTFOwG0> MU[yNlE6OTV3Nx?=
HEK293T NGXqfWRHfW6ldHnvckBCe3OjeR?= NEG5fIwzPCCq NWnoV5FzTE2VTx?= M3XOVWlvcGmkaYTpc44hd2ZibX;1d4UhX262M1Ggd4lodmGuaX7nJJdqfGhiSVO1NEBw\iByLkC3PEDPxE1? M{Lpe|IzOjZyMkCz
SW480 M1\COGZ2dmO2aX;uJGF{e2G7 M2PSU|ExKM7:TR?= NXy4RYVwOjRiaB?= M1vmNGROW09? Mo[yV5Ri[mmuaYrheIlwdiCxZjDBfIlvOiC5aYToJGVEPTBib3[gNE4{PzFizszN M4nzOlIzOjZyMkCz
HEK293T M3\6TWZ2dmO2aX;uJGF{e2G7 NHf5SZo2OCEQvF2= NWDENnl1TE2VTx?= MmDYTIF{KG6xIFXm[oVkfCCxbjDmc5J{c2:uaX6tbY5lfWOnZDDjRW1RKHOrZ37hcIlv\yCrbjDoeY1idiCKRVuyPVNVKGOnbHzzJINw\XiycnXzd4lv\yCFUlW= M{fo[lIzOjZyMkCz
IEC-6 NFzt[YNHfW6ldHnvckBCe3OjeR?= NULidIFYPiCq MkXvRY51[WexbnnzeEBi[3Srdnn0fUBifCCEZYThMYNifGWwaX6vWGNHKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhX262LUPhMYlv\HWlZXSgZZhqdjJiZYjwdoV{e2mxbjD3bZRpKEmFNUCgc4YhOC54NDFOwG0> NXnZOJNROjRyNkC0PFk>
IEC-6 MWDGeY5kfGmxbjDBd5NigQ>? NHTZTWY3KGh? MX7BcpRi\2:waYP0JIFkfGm4aYT5JIF1KEKndHGtZ4F1\W6rbj;UR2Yh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBYdnRvM3GtbY5lfWOnZDDs[5I2KGW6cILld5Nqd25id3n0bEBKSzVyIH;mJFIvQSEQvF2= Moj5NlQxPjB2OEm=
DLD1 MUXGeY5kfGmxbjDBd5NigQ>? M3nHVlIxKM7:TR?= MV2yOEBp MV\EUXNQ MUPJcohq[mm2aX;uJI9nKHSjbnv5doF{\SCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFSFRj3k[ZBmdmSnboSgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7 NEHzbIgzPDV{N{e5Ni=>
DLD1 NU[2bo9rS3m2b4TvfIlkKEG|c3H5 M3rRO|IxKM7:TR?= NX7vdYZ1OTBiZB?= NIjpSIpFVVOR NE\nPFREgXSxdH;4bYNqfHliYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36= NUHldIFMOjR3Mke3PVI>
VERO NYnLVnNKTnWwY4Tpc44hSXO|YYm= NWTE[HE3OjVizszN M{DUWmROW09? NVHiZ|ZVTGm|dIXyZoV{KFCDUjDi[Yx1KHO7boTo[ZNqeyxiYX\m[YN1cW6pIITo[UBi[3SrbjDjfZRwe2unbHX0c44tKGOnbHygd4hieGViYX7kJINmdGxiYXTo[ZNqd25? MYWyOVM{Ojh2NR?=
HeLa NUHsdoRLTnWwY4Tpc44hSXO|YYm= M4m0RVExKM7:TR?= NYDJO25qPDhiaB?= M1XWOXJm\HWldHnvckBw\iCleYTvdIxie22rYzDkbZN1emmkdYTpc44h[W6mIH71Z4xm[XJidILhcpNtd2OjdHnvckBw\iEQsj3jZZRmdmmw NYrR[Wd{OjVyNkG0PVk>
SiHa NX[zdoFETnWwY4Tpc44hSXO|YYm= NUD0[mZiOTBizszN M13WdFQ5KGh? NYX1VJJ{WmWmdXP0bY9vKG:oIHP5eI9xdGG|bXnjJIRqe3S{aXL1eIlwdiCjbnSgcpVkdGWjcjD0doFve2yxY3H0bY9vKG:oIN8yMYNifGWwaX6= NWr6fYJSOjVyNkG0PVk>

... Click to View More Cell Line Experimental Data

In vivo試験
臨床試験
特集

プロトコル (参考用のみ)

細胞アッセイ: [1]

細胞株 WTK1 lymphoblasts
濃度 1.0 μM
反応時間 8 hours
実験の流れ XAV-939 is solubilized in DMSO at 55 °C to make a 10 mM stock solution which may be diluted later to a working concentration of 100 μM. WTK1 lymphoblasts treated with either DMSO or 1.0 μM XAV-939 for 8 hours are loaded into independent wells of a 4-20% gradient SDS-PAGE every 2 hours over the course of 6 hours. At each time point, DMSO and XAV-939 samples are loaded into wells immediately adjacent to the prior time point. The corresponding load times at 0, 2 and 4 hours results in total run times of 2, 4 and 6 hours respectively. The gel is analyzed via western blot for DNA-PKcs following completion of the final run time and is quantified after normalization to actin loading controls.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download XAV-939 SDF
分子量 312.31
化学式

C14H11F3N2OS

CAS No. 284028-89-3
保管 3年-20℃
2年-80℃in solvent
別名 NVP-XAV939
溶解度 (25°C) * In vitro DMSO 12 mg/mL (38.42 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG 400+0.5% Tween 80+5% Propylene glycol 30mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol

文献中の引用 (21)

Frequently Asked Questions

  • Question 1
    I want to inject XAV 939 (Cat # S1180) into mice through I.P. and just wonder what kind of solvent/solution I can use for this.

    Answer: S1180 XAV-939 can be dissolved in 4% DMSO+corn oil at 1 mg/ml as a clear solution. When preparing the solution, please dissolve the compound in DMSO clearly first. You can sonicate and warm it in water bath at about 45 degree to help dissolving. Then dilute with corn oil.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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