Wortmannin

For research use only. Not for use in humans.

目录号:S2758 别名: KY 12420 中文名称:渥曼青霉素

Wortmannin Chemical Structure

CAS No. 19545-26-7

Wortmannin (KY 12420)是一种首次命名的PI3K抑制剂,在无细胞试验中IC50为3 nM,对 PI3K 家族的选择性较低。Wortmannin 可抑制自噬体的形成,并有效抑制DNA-PK/ATM,在无细胞试验中IC50为16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。

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客户使用Selleck生产的Wortmannin发表文献183篇:

产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 Wortmannin (KY 12420)是一种首次命名的PI3K抑制剂,在无细胞试验中IC50为3 nM,对 PI3K 家族的选择性较低。Wortmannin 可抑制自噬体的形成,并有效抑制DNA-PK/ATM,在无细胞试验中IC50为16 nM和150 nM。Wortmannin 也能抑制 PLK1 的活性。
靶点
PI3K [3]
(Cell-free assay)
DNA-PK [12]
(Cell-free assay)
ATM [12]
(Cell-free assay)
MLCK [1]
(Cell-free assay)
3 nM 16 nM 150 nM 170 nM
体外研究

钙或肽底物不影响Wortmannin对MLCK的抑制,但高浓度的ATP会减弱此种抑制。Wortmannin直接与MLCK催化结构域相互作用,导致不可逆转的酶活性减弱。Wortmannin对cAMP依赖蛋白激酶,cGMP依赖的蛋白激酶,钙调蛋白依赖激酶II,和蛋白激酶C均无抑制作用。[1] Wortmannin抑制由fMLP诱导的PtdInsP3(磷脂酰肌醇3,4,5-三磷酸化)形成,IC 50为5 nM 。在人中性粒细胞中,Wortmannin剂量为100 nM时可发挥完全抑制作用,增加PtdInsP2水平,且对PtdInsP和 PtdIns没有影响;Wortmannin可动态调控F-actin水平对fMLP刺激的肌动蛋白聚合无影响。[2]在RBL-2H3细胞中,Wortmannin通过结合110-kDa蛋白,不可逆的抑制磷酸肌醇3激酶(PI3-kinase)活性(IC 50为3 nM)对,对Pi4-kinase没有影响。Wortmannin也抑制Fc epsilon RI介导的组胺分泌和白三烯释放,对酪氨酸激酶Lyn无影响。[3]在大鼠脂肪细胞中,剂量为0.1 μM的 Wortmannin可完全抑制胰岛素诱导的己糖吸收,二不影响异丙肾上腺素刺激的脂肪分解活性。[4] 在人脐静脉内皮细胞中,在IGF-1的存在下,Wortmannin抑制胰岛素诱导一氧化氮生产,IC50为500nM。[5]在中国仓鼠卵巢细胞中, Wortmannin以50 μM剂量可抑制DNA双链断裂(DSB)修复,但对DSB水平无影响或单链断裂(SSB)酶活无影响。Wortmannin可加强电离辐射(红外)诱导的细胞毒作用,但本身无毒性。[6] Wortmannin抑制水球样激酶(PLK 1)活性,IC 50为24nM,造成细胞G 2 / M阻滞。[7] 在人巨噬细胞中,Wortmannin增加 Toll样受体(TLR)介导的白细胞介素- 6的积累,EC 50 = 50 nM。在小鼠巨噬细胞中,Wortmannin显着增强TLR诱导一氧化氮合酶(iNOS)的表达和亚硝酸盐积累。Wortmannin激活核因子-κB和上调细胞因子mRNA量。[8] Wortmannin也抑制水球样激酶(PlK)1和PlK 3,在有丝分裂中发挥重要作用。Wortmannin治疗可能导致可减少由DNA损伤诱导的p53丝氨酸20位磷酸化。[9] 在SW 1990细胞中,Wortmannin可抑制透明质酸诱导Akt磷酸化和细胞运动/迁移。[10]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A459 NUPVO5lDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;YclMzNjVizszN NFHMbWUyNTRiZB?= MoPNSG1UVw>? M1XBZYVvcGGwY3XzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25idILlZZRu\W62IIfpeIghfGGvb4jp[oVv M{LoWFI2PDlyM{iz
H1703 NHXKcVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nESFIvPSEQvF2= MnzhNU01KGR? MVLEUXNQ MVvlcohidmOnczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKHS{ZXH0cYVvfCC5aYToJJRidW:6aX\lci=> Mly4NlU1QTB|OEO=
HUVECs M1rWdGN6fG:2b4jpZ4l1gSCDc4PhfS=> MW[xNFAhdk1? MojBNlQhcA>? NIXRZlFifHSnboXheIV{KHSqZTDhZpJw\2G2aY\lJIVn\mWldIOgc4Yh[2GueXPvd4lvKG:wIG\STU1qdmS3Y3XkJIN6fG:2b4jpZ4l1gQ>? NUnWfY91OjV2NUCxPFY>
APRE-19 MYHBdI9xfG:|aYOgRZN{[Xl? MoLLOUDPxE1? NV20UJVHOjRiaB?= MYjhZo9tcXOqZYOgSmxbNW2nZHnheIVlKHC{bz3zeZJ3cX[jbD;hcpRqNWGyb4D0c5NqeyCjY4Tpeol1gQ>? NFmzVJkzPTN{OU[xOy=>
MDA-MB-231 Mm\KRZBweHSxc3nzJGF{e2G7 MkfsNeKh|ryPwrC= Mmq0OFghcA>? MnP1SG1UVw>? NEjRfIZl\WO{ZXHz[ZMhfGinIHPlcIwhe3W{dnn2ZYwhfHKnYYTl[EB4cXSqIEK1JO69VSCxZjDGNUBweiCIMjFCpC=> MWSyOVMxODl|Mh?=
MCF7 M131emZ2dmO2aX;uJGF{e2G7 MWmxNFAhdk1? M{W5elI1KGh? M{HWUoVtcW2rbnH0[ZMhTTJvaX7keYNm\CCDUlWtUJVkKGGldHn2bZR6 MV2yOVE4OjV3Nx?=
HT-29  MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e0T|EvPcLiwsXN M1nOPVk3KGh? NUTMUZpU\GWlcnXhd4V{KGOnbHyg[5Jwf3SqIIfobYNpKGOjbjDi[UBqdmirYnn0[YQh[nliS2nORS=> MnHpNlUxOTJzMkO=
MO59K  MV3DfZRwfG:6aXPpeJkhSXO|YYm= MoHoOeKh|ryP MkmxO{Bl NEKyb2lFVVOR M1ryNYVvcGGwY3XzJJRp\SCleYTveI95cWOrdImgc4Yh\XSxcH;zbYRmKG:{IHPpd5Bt[XSrbh?= M3\NUFI1QTV|NU[x
MO59J MVvDfZRwfG:6aXPpeJkhSXO|YYm= M2PB[VXDqM7:TR?= NUfq[FFLPyCm M1LuS2ROW09? NES3WIxmdmijbnPld{B1cGViY4n0c5RwgGmlaYT5JI9nKGW2b4Dvd4ll\SCxcjDjbZNxdGG2aX6= MkXpNlQ6PTN3NkG=
MO59K  NFXKcJJCeG:ydH;zbZMhSXO|YYm= M1L3PFExKM7:TR?= MVKyOEBp Mn3PSG1UVw>? NYq3NJJlcW6lcnXhd4V{KHSqZTDEV2IhdGW4ZXygbY5lfWOnZDDifUBmfG:yb4Pp[IUhd3JiY3nzdIxifGmw MVKyOFk2OzV4MR?=
MO59J NE\qVGtCeG:ydH;zbZMhSXO|YYm= MWexNEDPxE1? NXvTNFRYOjRiaB?= M3XMSGROW09? MVrpcoNz\WG|ZYOgeIhmKESVQjDs[ZZmdCCrbnT1Z4VlKGK7IHX0c5Bwe2mmZTDvdkBkcXOybHH0bY4> NGK4fXkzPDl3M{W2NS=>
HepG2 NGfhbIRHfW6ldHnvckBCe3OjeR?= Mki0NVAxKG6P MkX6NE42KGh? M33qTWROW09? NIjpeVBjdG:la4OgUWEucW6mdXPl[EBCc3RicHjvd5Bpd3K7bHH0bY9v M37veVI1QDZ|M{Ww
A549  NF\BPY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYezJOK2VcLi M1LDXFIhcA>? Mmqwd5VxeHKnc4Pld{Bx\W2ndILlfIVlNWmwZIXj[YQhSWu2IHHu[EBIW0t|zsKgZYN1cX[jdHnvckwhWy2yaHHz[UBienKnc4SsJINmdGxiYYDvdJRwe2m|IHHu[EBk[XOyYYPlMVMh[WO2aY\heIlwdg>? M1LFfVI1QDR5OE[z
A549  M2D5emZ2dmO2aX;uJGF{e2G7 MYWxNOKh|ryvwrC= NXGxTZljOTZiaB?= Mkf6SG1UVw>? NVnrUm94dW:mdXzheIV{KHSqZTDJRXYhemWybHnjZZRqd25iYX7kJINifXOnczDy[ZRmdnSrb36gc4YhVlBiaX6geIhmKG63Y3zleZMv NIDRVHAzPDhyMkGxNS=>
SK-N-LO NWf5[WVDTnWwY4Tpc44hSXO|YYm= MkG3NVAxKG6P M{Wx[FAvPSCq M3PUfYRm[3KnYYPld{B1cGVic4TpcZVt[W62IHXm[oVkfHNib3[gcY9zeGirbnWgc44hSWu2IIDoc5NxcG:{eXzheIlwdg>? M1vnbVI1PjV2NkC2
HL-60 NX\vT3RFTnWwY4Tpc44hSXO|YYm= NVjBbodVOC5zwrFOwG0> M1L3WVczKGh? NIXyTJBjdG:la4Og[IF{[XSrbnniMYlv\HWlZXSgZ4VtdCCmaX\m[ZJmdnSrYYTpc44> MmTmNlQ3ODd{N{O=
HepG2  NE\DN4tHfW6ldHnvckBCe3OjeR?= M2HFSVIxOCCwTR?= NVPFVHRjOC53IHi= M2m0d4F1fGWwdXH0[ZMhTm:6TzDwbI9{eGixconsZZRqd25? NYDxVlJsOjR3M{WxPVI>
H520 MXjGeY5kfGmxbjDBd5NigQ>? M4OxclExyqEQvF2= NYLJNpVoOSCq Ml\hSG1UVw>? NVjTfHZX\GWlcnXhd4V{KGOnbHz1cIFzKHCqb4PwbI8uSUuWIIDyc5RmcW5ibHX2[Yx{ NXnLVZR5OjR2NEe5N|U>
H1975 MoTRSpVv[3Srb36gRZN{[Xl? MX6xNOKh|ryP MYexJIg> MVfEUXNQ NXLGU5M1\GWlcnXhd4V{KGOnbHz1cIFzKHCqb4PwbI8uSUuWIIDyc5RmcW5ibHX2[Yx{ MnHTNlQ1PDd7M{W=
MG-63 MWDBdI9xfG:|aYOgRZN{[Xl? NH7ubY8yOCEEtV2= M4PPZ|EzKGh? MVXlcohidmOnczDEVE1qdmS3Y3XkJIFxd3C2b4Ppdy=> M1LNS|I1OzV6M{Cx
5637 MYHBdI9xfG:|aYOgRZN{[Xl? MoezNVDDqM7:TR?= NGX5[Go1OCCvaX6= MmTBdoV3\XK|ZYOgdFIyX0GIMTDlfJBz\XO|aX;uMEBETEtiZYjwdoV{e2mxbjygZY5lKGOnbHygbY5pcWKrdHnvckBqdmS3Y3XkJIJ6KG[3Y3;p[IFv Mo\KNlQ{OzN6Nki=
HEK-293 NWjpTYNSTnWwY4Tpc44hSXO|YYm= NFXHTIwyPTCwTR?= MXOxOkBp MmLuSG1UVw>? MVXk[YNz\WG|ZYOgR3JVKGGldHn2bZR6 MmTCNlQ{OjR|Nk[=
SW480  MUnGeY5kfGmxbjDBd5NigQ>? NWCzeI1EOTVybl2= MXuyNEBp M3vkcWROW09? NUfJd|NNemWmdXPld{Bk\WyudXzhdkBi[2O3bYXsZZRqd25ib3[g{tIu[2G2ZX7pci=> NYHJUGIzOjR|MkSzOlY>
HepG2 MUTGeY5kfGmxbjDBd5NigQ>? NV65VGJ[OTByIH7N NFjBXZkzPCCq MXPheJRmdnWjdHXzJJRp\SClb3zvcolmeyCxZjD0bIUhfHWvb4KgZ4VtdHNid3n0bEB2eHKnZ4XsZZRqd25ib3[gRYt1OQ>? M3;OWVI1Ojl5NUGw
HCT 116  NFzyWHFHfW6ldHnvckBCe3OjeR?= NGSzd4gyODBibl2= M4DLVFI1KGh? MkXIZZR1\W63YYTld{B1cGViY3;sc45q\XNib3[geIhmKHS3bX;yJINmdGy|IIfpeIghfXC{ZXf1cIF1cW:wIH;mJGFsfDF? NH;xU40zPDJ7N{WxNC=>
BEL/FU M{jh[GZ2dmO2aX;uJGF{e2G7 NXjXT4RFOSCvTR?= M3jwflI1KGh? M17nTYRm[3KnYYPld{Bxem:2ZXnuJIxmfmWuczDv[kB1cGViUFmzT{9Cc3RicHH0bJdigQ>? MmjkNlQzOzJyOUm=
Huh7  MUfGeY5kfGmxbjDBd5NigQ>? NYnr[VFjO8LizszN MlfMNUBp NHXmcIJz\WS3Y3XzJJRp\SC4aYL1d{BmdnS{eTDpcpRwKHSqZTDj[Yxtew>? MlHYNlQyQDRzOU[=
A-375 NWW1PHFmSXCxcITvd4l{KEG|c3H5 MWS0M|gh|ryP MYiyOEBp MV7lcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqe8Li M1nJZ|I1OTF|MUez
A-375-TS  NG\t[mtCeG:ydH;zbZMhSXO|YYm= NXvJV4tiPC96IN88US=> NHL0WFYzPCCq NX3MdGRk\W6qYX7j[ZMhXFKDSVytbY5lfWOnZDDhdI9xfG:|aYRCpC=> NGfKRVEzPDFzM{G3Ny=>
Mel-HO MVfBdI9xfG:|aYOgRZN{[Xl? MWO0M|gh|ryP Ml3nNlQhcA>? M4[ze4VvcGGwY3XzJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m|wrC= NIXOWHAzPDFzM{G3Ny=>
Mel-HO-TS M1\pNGFxd3C2b4Ppd{BCe3OjeR?= NV[xZ4pnPC96IN88US=> MXuyOEBp MkPy[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXQEoB?= MWSyOFEyOzF5Mx?=
MeWo M1rVdmFxd3C2b4Ppd{BCe3OjeR?= M1HiVVQwQCEQvF2= NVrjTGIyOjRiaB?= M3z5[4VvcGGwY3XzJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m|wrC= MlHmNlQyOTNzN{O=
Mel-2a Mn7sRZBweHSxc3nzJGF{e2G7 NFj2XoY1NzhizszN NHP2W2IzPCCq M3n4ZoVvcGGwY3XzJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m|wrC= NHHUS4ozPDFzM{G3Ny=>
MDA-MB-231 M4faUWZ2dmO2aX;uJGF{e2G7 MlrUNQKBmzRyMDDuUS=> Ml;tOEBp Mlmxd5VxeHKnc4Pld{BCc3RicHjvd5Bpd3K7bHH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWqyNlkxPjJ3OR?=
MDA-MB-231 NGrsO5hHfW6ldHnvckBCe3OjeR?= MWS0NFAhdk1? NWD4VpF5PCCq NUD3V5BH\GWlcnXhd4V{KE2PUD25JIFv\CCLTD24JJBzd3SnaX6gbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MlrRNlI6ODZ{NUm=
Jurkat NFjMbXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV64PY1HOC5{NT2xMlI2KM7:TR?= MUWyOE81QCCq NY\PPY5DTE2VTx?= NGTNcG9qdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hcW5iYn;0bEB1cW2nLTDhcoQh\G:|ZT2g[IVx\W6mZX70JI1idm6nch?= NULtPVNPOTl5NUexPFU>
Namalwa NV7yR2ZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e3dlAvOjVvMT6yOUDPxE1? M4Da[FI1NzR6IHi= M{XxcWROW09? M1HRXYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLTDk[ZBmdmSnboSgcYFvdmW{ MWGxPVc2PzF6NR?=
Jurkat NHzpSIVCeG:ydH;zbZMhSXO|YYm= NUjKVppwOC5{NT2xMlI2KM7:TR?= Ml74NlQwPDhiaB?= NXTK[4JRTE2VTx?= M2O0e4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZo91cCC2aX3lMUBidmRiZH;z[U0h\GWyZX7k[Y51KG2jbn7ldi=> MlLZNVk4PTdzOEW=
Namalwa MlTZRZBweHSxc3nzJGF{e2G7 Mmm1NE4zPS1zLkK1JO69VQ>? NInnbnIzPC92ODDo NGTrT4dFVVOR M4LVcIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNiaX6gZo91cCC2aX3lMUBidmRiZH;z[U0h\GWyZX7k[Y51KG2jbn7ldi=> MoXjNVk4PTdzOEW=
K562 M3HvTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnEOmVVOjRiaB?= NIGxUoZKSzVyPUK1xtExNjF2IH7N NFztVlYyQTZ4MkO2NS=>
SW1990 NY\GSoxMTnWwY4Tpc44hSXO|YYm= NGjGUo0xNjBzLUGg{txO NGDRclkyKGh? M{n3colvcGmkaYTzJGhCNWmwZIXj[YQhSWu2IIDoc5NxcG:{eXzheIlwdg>? MkjZNVk1PjlyMkC=
RT112  M2Tidmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHpNVDDqM7:TR?= MVeyOEBp NYL4NGZmTE2VTx?= M{jPb4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBIOi:PIHPlcIx{ NHvDUFcyQDd6N{izNi=>
MHG-U1 MoLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVWxNOKh|ryP M17NVlI1KGh? NGCx[5RFVVOR M4rFdIRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBIOi:PIHPlcIx{ NGTx[4UyQDd6N{izNi=>
SMMC-7721 MVXBdI9xfG:|aYOgRZN{[Xl? M{O0NFIxOMLibl2= MlHFNlQhcA>? NVS0TZBpcW6lcnXhd4V{KEOKWD3pcoR2[2WmIHHwc5B1d3Orcx?= MoH2NVc2PTdzOUG=
SMMC-7721 MX;GeY5kfGmxbjDBd5NigQ>? M122flIxOMLibl2= MWOyOEBp NHqxPWZ2eC2{ZXf1cIF1\XNizsKxMFRIXDFiZYjwdoV{e2mxbh?= M3XDcVE4PTV5MUmx
HeLa MX;GeY5kfGmxbjDBd5NigQ>? M{j4clExOMLibl5CpC=> MUKxJIg> NEDLVYdidHSncoOgeIhmKG2xcoDoc4xw\3lib3[geIhmKHS{YX7z[oVzemmwIILlZ5lkdGmwZzDjc41x[XK2bXXueC=> NH;Fd|MyPjh7MEmxOS=>
MRC5VI NVuxWXJDTnWwY4Tpc44hSXO|YYm= MUSxNk42KG2P MVewMlUhcA>? MWTEUXNQ NWftd|Zo[WKxbHnzbIV{KHSqZTDT[ZI1PzNxVHjyN|A5yqCyaH;zdIhwenmuYYTpc44hd2ZiQXv0VGtDyqB? MlLHNVYzOjd|OUS=
AT5BIVA NYLGdZE2TnWwY4Tpc44hSXO|YYm= MonjNVIvPSCvTR?= M3vQNFAvPSCq NGLHUY5FVVOR M{XEdIFjd2yrc3jld{B1cGViU3XyOFc{N1SqckOwPOKheGixc4Doc5J6dGG2aX;uJI9nKEGtdGDLRuKh MWexOlIzPzN7NB?=
M059J NGnxO4JHfW6ldHnvckBCe3OjeR?= MmDJNVIvPSCvTR?= MU[wMlUhcA>? M4fWdmROW09? NGG3RVdi[m:uaYPo[ZMhfGinIGPldlQ4Oy:WaIKzNFjDqHCqb4PwbI9zgWyjdHnvckBw\iCDa4TQT2LDqA>? NHHDNFQyPjJ{N{O5OC=>
HeLa NXfDNndzTnWwY4Tpc44hSXO|YYm= NIraSWcyOi53IH3N NXvhXplUOC53IHi= M{jGcWROW09? MXjhZo9tcXOqZYOgeIhmKFOnckS3N{9VcHJ|MElCpJBpd3OyaH;yfYxifGmxbjDv[kBCc3SSS1NCpC=> M{TCZVE3OjJ5M{m0
N2a NXXKTYpHSXCxcITvd4l{KEG|c3H5 NVzjWo5jOC5zLUGwJO69VQ>? NYLFe2w6OiCq MYLpcoR2[2W|IHTlZ5Jm[XOnZDDj[YxtKH[rYXLpcIl1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MnvHNVU5PDJ5Nke=
Jurkat  MoXwT4lv[XOnIFHzd4F6 NFrpNFBKSzVyIH;mJFI1KG6P NEG4d4wyPTZ4NEWxPS=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p-GSK3β / GSK3β / Bcl-xl / Bax / Caspase-3 / Cleaved caspase-3; 

PubMed: 25344912     


Four esophageal cancer cell lines were treated with different concentrations of wortmannin for 48 h, and cell lysates were collected for Western blot analysis of p-AKT, AKT, p-GSK3β, GSK3β, Bcl-xL, Bax, caspase-3, and cleaved caspase-3.

25344912
Immunofluorescence
DNMT1; 

PubMed: 24001151     


PC3 cells were treated with DMSO or wortmannin (1 μM) for 24 hours. DNMT1 and DNMT3B cellular localization was visualized by immunofluorescent staining. After 24h of treatment, cells were fixed in methanol, incubated with the indicated antibodies, stained with Alexa Fluor 594-tagged secondary antibodies and counterstained with DAPI. Slides were then mounted and examined under a fluorescence microscope. The bright field images of PC3 cells treated with DMSO or wortmannin (1 μM) for 24 hours are shown (right panel).

24001151
Growth inhibition assay
Cell viability; 

PubMed: 25344912     


MTT assay was used to determine the effects of different concentrations of wortmannin on viability of esophageal cancer cells lines KYSE150, HKESC-1, KYSE270, and T.Tn. Bars, SD; * P < 0.05; **, P < 0.01; ***, P < 0.001 compared with DMSO-treated cells.

25344912
体内研究 Wortmannin剂量为1mg/kg可抑移植瘤小鼠中SW1990的腹膜转移,无重量损失。[10] Wortmannin抑制在小鼠正常组织(肺,心脏和脑组织匀浆)及肿瘤组织中的phosphatidylinositide 3- B激酶(PKB)/磷酸化Akt,在剂量为0.7 mg/kg时无死亡或急性毒性。与gemcitabine联合使用时,可大大增加细胞凋亡和抑制原位肿瘤生长,两种药物单独使用都无以上效果。[11]

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)

动物实验:[11]
- 合并
  • Animal Models: 人胰腺癌细胞 PK1s.c.和原位注入SCID免疫缺陷小鼠。
  • Dosages: 0.175, 0.35, 和0.7 mg/kg
  • Administration: 静脉注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 85 mg/mL (198.39 mM)
Water Insoluble
Ethanol 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):
5% DMSO+40% PEG 300+5% Tween 80+ddH2O
5mg/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 428.43
化学式

C23H24O8

CAS号 19545-26-7
储存条件 粉状
溶于溶剂
别名 KY 12420

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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

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

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PI3K Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID