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 MXnLbY5ie2ViQYPzZZk> M33NNFE5Njd3IN88US=> MVO2NEBucW5? MmjVSG1UVw>? MmjmTY5pcWKrdHnvckBw\iCQLYTldo1qdmGuIFfTWE11[WepZXSgWG5MWzJiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjByNUOg{txO MW[yN|g4QTR|MR?=
HEK293T M1\tN2Z2dmO2aX;uJGF{e2G7 NFTnOYZFVVOR MmrFTY5pcWKrdHnvckBw\iCZboSgd4lodmGuaX7nJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[g[o9ze2uxbHnuMYlv\HWlZXSgZ2FOWCC{ZYPwc45{\SCnbHXt[Y51KGGldHn2ZZRqd25id3n0bEBKSzVyIH;mJFAvODd6IN88US=> NGrwPGEzOzh5OUSzNS=>
HEK293T NETTU5FHfW6ldHnvckBCe3OjeR?= MXixNEDPxE1? M1K2[GROW09? M4\me2lvcGmkaYTpc44hd2ZiYnX0ZU1k[XOnaX6t[IVx\W6mZX70JINidm:waXPhcEBYdnR|IIDheIh4[Xlid3n0bEBKSzVyIH;mJFAvODVzIN88US=> M2nUWVIzOTlzNUW3
HEK293T M4TtUmZ2dmO2aX;uJGF{e2G7 NFXWOIszPCCq NUDROYxsTE2VTx?= MnzvTY5pcWKrdHnvckBw\iCvb4Xz[UBYdnR|QTDzbYdv[Wyrbnege4l1cCCLQ{WwJI9nKDBwMEe4JO69VQ>? NFHDPGgzOjJ4MEKwNy=>
SW480 MVnGeY5kfGmxbjDBd5NigQ>? M3PxelExKM7:TR?= M2fMe|I1KGh? NGD2O5BFVVOR MmnlV5Ri[mmuaYrheIlwdiCxZjDBfIlvOiC5aYToJGVEPTBib3[gNE4{PzFizszN MnXnNlIzPjB{MEO=
HEK293T M2rBT2Z2dmO2aX;uJGF{e2G7 MomwOVAh|ryP NFS4dlFFVVOR NUfD[Is4UGG|IH7vJGVn\mWldDDvckBnd3K|a3;sbY4ucW6mdXPl[EBkSU2SIIPp[45idGmwZzDpckBpfW2jbjDISWszQTOWIHPlcIx{KGOxZYjwdoV{e2mwZzDDVmU> MnzQNlIzPjB{MEO=
IEC-6 MnXYSpVv[3Srb36gRZN{[Xl? M3XZWVYhcA>? MWjBcpRi\2:waYP0JIFkfGm4aYT5JIF1KEKndHGtZ4F1\W6rbj;UR2Yh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBYdnRvM3GtbY5lfWOnZDDhfIlvOiCneIDy[ZN{cW:wIIfpeIghUUN3MDDv[kAxNjZ2IN88US=> M3;jdlI1ODZyNEi5
IEC-6 NGPGdIxHfW6ldHnvckBCe3OjeR?= Mni4OkBp MnnlRY51[WexbnnzeEBi[3Srdnn0fUBifCCEZYThMYNifGWwaX6vWGNHKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhX262LUPhMYlv\HWlZXSgcIdzPSCneIDy[ZN{cW:wIIfpeIghUUN3MDDv[kAzNjlizszN MmrINlQxPjB2OEm=
DLD1 NGGzbZBHfW6ldHnvckBCe3OjeR?= NYTtVmo3OjBizszN NI\6R2YzPCCq M4L3ZmROW09? M322TWlvcGmkaYTpc44hd2ZidHHub5lz[XOnIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiVFPGMYRmeGWwZHXueEB1emGwc3PybZB1cW:wYXygZYN1cX[rdIm= M1:w[FI1PTJ5N{my
DLD1 MYHDfZRwfG:6aXOgRZN{[Xl? MUGyNEDPxE1? MUmxNEBl NHvjT4xFVVOR MVfDfZRwfG:6aXPpeJkh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25? NFr6fnUzPDV{N{e5Ni=>
VERO MnnGSpVv[3Srb36gRZN{[Xl? MWSyOUDPxE1? NV7WSllWTE2VTx?= MUjEbZN1fXKkZYOgVGFTKGKnbISgd5lvfGinc3nzMEBi\m[nY4TpcochfGinIHHjeIlvKGO7dH;zb4Vt\XSxbjygZ4VtdCC|aHHw[UBidmRiY3XscEBi\Ginc3nvci=> NYOycJFUOjV|M{K4OFU>
HeLa MmfCSpVv[3Srb36gRZN{[Xl? Mm\kNVAh|ryP MVS0PEBp MnO1VoVlfWO2aX;uJI9nKGO7dH;wcIF{dWmlIHTpd5RzcWK3dHnvckBidmRiboXjcIVieiC2cnHud4xw[2G2aX;uJI9nKM7{LXPheIVvcW5? Mk\ONlUxPjF2OUm=
SiHa MonHSpVv[3Srb36gRZN{[Xl? M1;NeFExKM7:TR?= M4LiTFQ5KGh? NIHQZ5BT\WS3Y4Tpc44hd2ZiY4n0c5Bt[XOvaXOg[Il{fHKrYoX0bY9vKGGwZDDueYNt\WG{IITyZY5{dG:lYYTpc44hd2ZizsKtZ4F1\W6rbh?= NXfWcIZKOjVyNkG0PVk>

... 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 2年-20℃
6月-80℃in solvent
別名 NVP-XAV939
溶解度 (25°C) * In vitro DMSO 12 mg/mL (38.42 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
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)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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