Vismodegib (GDC-0449)

For research use only. Not for use in humans.

目录号:S1082 中文名称:维莫德吉

Vismodegib (GDC-0449) Chemical Structure

CAS No. 879085-55-9

Vismodegib (GDC-0449)是一种新型有效的,特异性hedgehog抑制剂,无细胞试验中IC50为3 nM,也会抑制P-gp,IC50为3.0μM。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1179.52 现货
RMB 730.63 现货
RMB 3046.91 现货
RMB 8763.3 现货
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客户使用Selleck生产的Vismodegib (GDC-0449)发表文献153篇:

产品安全说明书

Hedgehog/Smoothened抑制剂选择性比较

生物活性

产品描述 Vismodegib (GDC-0449)是一种新型有效的,特异性hedgehog抑制剂,无细胞试验中IC50为3 nM,也会抑制P-gp,IC50为3.0μM。
靶点
Hedgehog [1]
(Cell-free assay)
3 nM
体外研究

GDC-0449有效抑制hedgehog通路,是一种新型及特定合成的小分子抑制剂,IC50为3nM。[1] GDC-0449作用于Hedgehog信号通路,阻断Hedgehog配位体,即细胞表面受体PTCH 及SMO的活性,从而阻断Hedgehog信号通路。在组织生长和修复方面,Hedgehog信号通路意义重大。Hedgehog通路信号的异常激活,及不受控制的细胞增殖,可能与Hedgehog配位体,即细胞表面受体PTCH 及SMO的突变有关。在体外,GDC-0449在不抑制胰脏细胞增殖的前提下阻止原代胰脏移植物的生长,这项结果最近已经应用到临床。GDC-0449也抑制ABCG2, P-糖蛋白, 及和MDR有关联的重要MRP1 ABC载体。GDC-0449也阻断其他多种ABC载体。ABC载体属于一个膜蛋白家族,它的过量表达和耐药性有关,这也是治疗癌症的一个重大障碍。GDC-0449强抑制两种ABC载体,ABCG2/BCRP和ABCB1/P-糖蛋白,也温和抑制ABCC1/MRP1。在ABCG2过量表达的HEK293细胞中, GDC-0449可以提高荧光ABCG2底物BODIPY-哌唑嗪的保持力,也可用米托蒽醌再次处理这些细胞,产生抗肿瘤的ABCG2底物。实验使Madin-Darby犬的肾脏细胞中过量表达P糖蛋白或者MRP1,GDC-0449 提高了钙黄绿素-AM的保持力,然后载用秋水仙素处理这些细胞。另外,用米托蒽醌,托泊替康,SN-38处理的过量表达ABCG2的人类非小细胞肺癌细胞NCI-H460/par和NCI-H460/MX20,用GDC-0449再次处理。GDC-0449 作用于ABCG2 和 Pgp 的IC50值分别为1.4μM和 3.0 μM。[2]GDC-0449 改变细胞内Ca2+ 平衡,且作用于抗cisplatin的肺癌细胞, 抑制细胞生长。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
IGROV-1 M3;ucGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rqfWlEPTB;MD6wO|I1QCEQvF2= MmfvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
HCE-T MnW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUmyVYR4UUN3ME2xMlMzOjR5IN88US=> MmD2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
D-542MG NH\DSWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXMSVRKSzVyPUGuPFY4OzdizszN NHnqOYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
23132-87 NHexU29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfVTWM2OD12LkSwNVQ4KM7:TR?= M1\j[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
HDLM-2 NYXNRWVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHUUJRKSzVyPUiuNFQ4PjZizszN MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
ACN NGL4ZZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRThwNUCxNFkh|ryP M4jT[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
HuO-3N1 M4TqWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPySodKSzVyPUmuOlAyODhizszN Mon2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
BHT-101 NX\DVW4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rXOmlEPTB;MUGuN|gh|ryP MnrjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
KYSE-150 M1;NUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2m2[GlEPTB;MUGuOVg1OSEQvF2= MkTJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
MC-IXC NHLSPVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPKOYdKSzVyPUGyMlIzQTJizszN M2njdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
D-423MG MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYi1PWFtUUN3ME2xNk44PjV5IN88US=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
NY Mmj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTF2Lki5NFMh|ryP M4DzSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
HOS MojtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXUPZFKSzVyPUG1MlY4OTlizszN M{P6V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
NB7 NUTFXIxpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTF3Lki5NUDPxE1? NWDPUGE4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
DMS-273 NEjjVpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHNOVNKSzVyPUG2MlY4OTNizszN Ml3DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
MDA-MB-361 M3zINGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\qZlZ2UUN3ME2xO{4zPzFzIN88US=> MnHPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
DU-145 M{LHXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTF6LkOyJO69VQ>? NX6zfFhvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
NCI-H82 NH\2WoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGriV29KSzVyPUG5Mlg{QDZizszN M3j1e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
NCI-SNU-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HyO2lEPTB;MkCuNFE6PiEQvF2= M4j2W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
GCT M332cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLJe4ZKSzVyPUKwMlg5OjRizszN M{fncFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
C2BBe1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1v4eGlEPTB;MkGuNVA2QCEQvF2= Mn[2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
LB2241-RCC NWXZ[FliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFT2XI5KSzVyPUKxMlg1PDFizszN NWjlTndZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
COLO-829 MnPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDmWVd2UUN3ME2yNk4yQDdzIN88US=> NW\qZmJxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
EW-11 NGnlTFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYe0TYsxUUN3ME2yNk45ODJ{IN88US=> Mm[wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
NCI-H526 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTDbFF7UUN3ME2yN{41PzF5IN88US=> NETETGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
SF295 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2j0emlEPTB;MkSuNFI2OiEQvF2= NWHBPI95RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
D-566MG NXjmbpZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknETWM2OD1{NT6yPVQ{KM7:TR?= M{DQflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
8505C NYfQclJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTJ3Lk[zN|Eh|ryP NF3sdlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
HT-29 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTJ4LkC0N|Eh|ryP NFP6TYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
NBsusSR NF;2NYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnrTWM2OD1{Nj64NFA3KM7:TR?= MoOxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
BV-173 NFuzXIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTJ6LkOxPFIh|ryP MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
CTB-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTNyLkGwN|Eh|ryP NYHyfIFERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
JAR MoO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml6xTWM2OD1|Mj61N|cyKM7:TR?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
CAMA-1 MnviS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTN|LkS2NVUh|ryP M1TpN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
CAL-51 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTN2LkexO|Yh|ryP MnHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
A172 NIe3OWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWOye3lUUUN3ME2zO{41QTJzIN88US=> M3zNN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
QIMR-WIL NHfmXXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fCVGlEPTB;M{iuNFcxQCEQvF2= NH[1S|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
AsPC-1 Mn3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTN6LkS2OVEh|ryP NXLLPHp5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
MKN7 NYLMNWNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj4d|VHUUN3ME2zPU4xODd7IN88US=> MmfxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
ONS-76 Mo\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjaRox[UUN3ME20N{4{ODV5IN88US=> M3XzWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
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medulloblastoma cell M3\rbmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NGfNNHB2eCC2bzCzNEB2VQ>? NUf1Z4hVPzJiaILz NXXDbVNvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDQeINpMy9vIIC1N{0wNSCvZXT1cIxw[myjc4TvcYEh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwheHKxbHnm[ZJifGmxbjD1dEB1dyB|MDD1UUBi\nSncjC3NkBpenNiYomgUXRUKGG|c3H5Mi=> MlHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6N{OzNFMoRjJ6OEezN|A{RC:jPh?=
medulloblastoma cell NXTrXnZRSXCxcITvd4l{KGG|c3H5 MULJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIH3veZNmKFC2Y3irM{0heDV|LT:tJI1m\HWubH;icIF{fG:vYTDj[YxteyCrbYDsZY51\WRiaX6gZZRpgW2rYzDueYRmKG2xdYPlJIF1KDF{LkWgcYcwc2duIHnwJIJq\CCob4KgNVUh[2:wc3XjeZRqfmViZHH5d{BjgSCWVV7FUEBie3OjeT6= MoHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6N{OzNFMoRjJ6OEezN|A{RC:jPh?=
NIH/3T3 NGn2c4xHfW6ldHnvckBie3OjeR?= NUCzdnVTUW6qaXLpeIlwdiCxZjDo[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDlfJBz\XO|ZXSgbY4hdW:3c3WgUmlJNzOWMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGinZHflbI9oNWmwZIXj[YQhT2yrLUKgZYNkfW23bHH0bY9vKGG2IITpdEBw\iCycnntZZJ6KGOrbHnhJIJ6KESDUFmgd5RicW6rbnegZoF{\WRiY3;u[o9k[WxibXnjdo9{[2:yaXOgZY5idHm|aYOu MmDNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PVEoRjJ5OEGwOVkyRC:jPh?=
NIH/3T3 MlqwSpVv[3Srb36gZZN{[Xl? MlzQTY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gbIVl\2Wqb3etbY5lfWOnZDDTcY8uTUeIUDDjbYxq[XK7IITyZY5{dG:lYYTpc44h[nliRFHQTUB{fGGrbnnu[{Bj[XOnZDDjc45nd2OjbDDtbYNzd3Olb4DpZ{BidmGueYPpd{4> M1;UUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OEGwOVkyLz5{N{ixNFU6OTxxYU6=
medulloblastoma cell MWLBcpRqNXS3bX;yJIF{e2G7 MV;BcpRqNXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViUITjbEswNSCyNUOtM{0hdWWmdXzsc4Jt[XO2b33hJINmdGy|IHntdIxidnSnZDDpckBifGi7bXnjJI52\GVibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiMkCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CC2d3nj[UBl[WmueTD2bYEh\2G4YXflJI1m[XO3cnXkJIV3\XK7IH;0bIVzKGSjeTDkeZJqdmdiY3;tdI92dmRiZH;zbY5oNg>? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd|OUexOEc,Ojl5M{m3NVQ9N2F-
C3H10T1/2 MXPGeY5kfGmxbjDhd5NigQ>? NFLWS5g1NjFidH:gNVAxOCCwTR?= M{Hs[GFtdG:|dHXybYMhcW6qaXLpeIlwdiCxZjDTcY8hcW5ibX;1d4UhSzOKMUDUNU8zKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gdJVzdW:{cHjhcYlv\S2rbnT1Z4VlKEeuaUGgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7IHH0JFQvOSC2bzCxNFAxKG6PIHL5JJFRS3JiYX7hcJl{cXNw NIrIcFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C3OFU1OSd-MkOwO|Q2PDF:L3G+
C3H10T1/2 NIjacItHfW6ldHnvckBie3OjeR?= NGG3Z401NjFidH:gNVAxOCCwTR?= NXO1e4ZNS2:vcHX0bZRqfmViaX7obYJqfGmxbjDv[kBUdW9iaX6gcY92e2ViQ{PINVBVOS9{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhW0GJLXnu[JVk\WRiR3zpNUB1emGwc3PybZB1cW:wYXygZYN1cX[rdImgZZQhPC5zIITvJFExODBibl2gZpkheVCFUjDhcoFtgXOrcz6= M3flfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEe0OVQyLz5{M{C3OFU1OTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Bcl-2 / Bax; 

PubMed: 28195165     


GDC-0449 treatment affected the expression levels of cell cycle-related protein levels. U251 cells were treated with 0.1% DMSO or GDC-0449 at the indicated concentrations for 24 h. Cells were then harvested and examined using Western blot analysis with the indicated antibodies.

p53 / Cyclin D1 / p21; 

PubMed: 28195165     


GDC-0449 treatment affected the expression levels of cell cycle-related protein levels. U251 cells were treated with 0.1% DMSO or GDC-0449 at the indicated concentrations for 24 h. Cells were then harvested and examined using Western blot analysis with the indicated antibodies.

Gli1 / SOX2 / OCT4; 

PubMed: 26418365     


The activation of Hedgehog pathways and CSC markers were tested by immunoblotting analysis in Hs578T and BT549 cells. β‐Actin was used as a loading control.

p-GSK3β / GSK3β / p-Akt / Akt / Gli1; 

PubMed: 27143997     


Cells were pretreated with or without 30 μM GDC-0449 for 2 h before TMT treatment. After incubation with 3.75 μM TMT for another 24 h, the expression levels of proteins were determined through Western blot analysis.

Fas / DR4 / DR5 / Cleaved PARP / Bcl-2 / Cleaved caspase-3 / PDGFRα; 

PubMed: 22087285     


Pancreatic CSCs were treated with GDC-0449 (0, 1, 5 and 10 µM) for 48 h. The expression of Fas, DR4/TRAIL-R1, DR5/TRAIL-R2, PARP cleavage, Bcl-2, and Caspase-3 by the Western blot analysis. β-Actin was used as a loading control.

28195165 26418365 27143997 22087285
Immunofluorescence
Gli1 / Gli2; 

PubMed: 22087285     


GDC-0449 inhibits expression of Gli1 and Gli2 in human pancreatic CSCs. The cells were seeded on fibronectin-coated coverslips and treated with GDC-0449 (10 µM) for 48 h. Subsequently, cells were fixed with 4% paraformaldehyde, blocked in 10% normal goat serum and stained with Gli1 and Gli2 primary antibodies (1∶100) for 16 h at 4°C and washed with PBS. Afterwards, cells were incubated with fluorescently labeled secondary antibody (1∶200) along with DAPI (1 mg/ml) for 1 h at room temperature and cells were mounted and visualized under a fluorescent microscope. For better visuality, the color of DAPI was changed from blue to red.

22087285
Growth inhibition assay
Cell viability; 

PubMed: 29042665     


GDC-0449 improves the anti-proliferation activity in NIH-3T3 cells but not in BxPC-3, Panc-1, MIAPaca-2 and SW1990 cells when cultured alone. The cytotoxicities of GDC-0449, Dox or Dox with GDC-0449 (5 μM or 10 μM) were measured by performing a 48-h MTT assay in BxPC-3 (A), Panc-1 (B), MIAPaca-2 (C), SW1990 (D) and NIH-3T3 (E) cells. Apoptosis rate was detected by flow cytometry (Annexin V staining) analysis after treatment with Dox (200 nM) with or without GDC-0449 for 24 h (F). Data are presented as the mean ± SD. *P < 0.05, **P < 0.01.

29042665
体内研究 GDC-0449已经用于治疗动物模型的成髓细胞瘤。[2] GDC-0449 抑制原代胰腺移植瘤生长,但是不抑制细胞增殖。GDC-0449按25 mg/kg 以上剂量口服给药髓母细胞瘤Ptch(+/-)异体移植物模型,引起细胞衰退,按92 mg/kg剂量处理两种配位体依赖的结肠直肠癌模型D5123和1040830,每天处理两次,抑制肿瘤生长。分析Hh通路活性和 PK/PD 模型显示GDC-0449抑制 Gli1,IC50值与GDC-0449作用于髓母细胞瘤和D5123模型的IC50值差不多(分别为0.165 μM ±11.5% 和0.267 μM ±4.83%)。[4]

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:[2]
- 合并
  • Cell lines: MDCKII细胞
  • Concentrations: 20 μM
  • Incubation Time: 2小时
  • Method: MDCKII细胞按每孔3x105密度接种在24孔板中。培养液包含不同药物,实验组为50 µM VP,50 µM吲哚美辛,或者20 µM GDC-0449溶解在DMSO中,对照组只含有DMSO。然后加入非荧光的钙黄绿素-AM,最终浓度达到1.0 µM。然后在37oC温育2小时。细胞用含Ca2+,Mg2+的Hank's平衡盐溶液buffer冲洗2次,然后震荡1小时溶解在含0.01% Triton X-100的磷酸缓冲液中,然后放在4oC下过夜。溶解的物质然后转移到96孔板上,钙黄绿素引起的荧光信号用分光光度法定量。所有的实验操作需在暗中进行,所有的读数用平均值±SEM表示。
    (Only for Reference)
动物实验:[4]
- 合并
  • Animal Models: Ptch(+/-)异体移植物模型
  • Dosages: 25 mg/kg,92 mg/kg
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 84 mg/mL (199.38 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+50% ddH2O
12.5mg/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 421.3
化学式

C19H14Cl2N2O3S

CAS号 879085-55-9
储存条件 粉状
溶于溶剂
别名 N/A

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、SDS / 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、SDS / 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03610022 Recruiting Drug: Treatment with vismodegib Metastatic Basal Cell Carcinoma|Locally Advanced Basal Cell Carcinoma University Hospital Bordeaux September 3 2018 Phase 4
NCT03035188 Unknown status Drug: Vismodegib Basal Cell Carcinoma SRH Wald-Klinikum Gera GmbH January 2017 Phase 2
NCT02781389 Completed -- Basal Cell Carcinoma University Hospital Essen|OnkoDataMed GmbH April 29 2016 --
NCT02593760 Completed Other: Placebo|Drug: Ruxolitinib|Drug: Vismodegib Myelofibrosis Hoffmann-La Roche January 25 2016 Phase 1
NCT02648048 Completed Drug: Pirfenidone|Drug: Vismodegib Idiopathic Pulmonary Fibrosis Hoffmann-La Roche January 15 2016 Phase 1
NCT02436408 Active not recruiting Drug: Vismodegib Carcinoma Basal Cell University of Michigan Rogel Cancer Center July 15 2015 Phase 4

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID