Vismodegib (GDC-0449)

目录号:S1082 中文名称:维莫德吉

仅限科研使用

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。

Vismodegib (GDC-0449) Chemical Structure

CAS: 879085-55-9

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172篇:

产品安全说明书

Hedgehog/Smoothened抑制剂选择性比较

相关Hedgehog/Smoothened产品

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 M36wWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTBwMEeyOFgh|ryP MoLoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
HCE-T MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\wcXBKSzVyPUGuN|IzPDdizszN MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
D-542MG NWnsfWM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3r1[2lEPTB;MT64Olc{PyEQvF2= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
23132-87 NEjFfnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUCxV45FUUN3ME20MlQxOTR5IN88US=> M3[xV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
HDLM-2 NGr4S3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTaV5pyUUN3ME24MlA1PzZ4IN88US=> NEjMSnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
ACN NVS3ZWE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnTdZRYUUN3ME24MlUxOTB7IN88US=> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
HuO-3N1 MkfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPSS5ZKSzVyPUmuOlAyODhizszN NGnSWWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
BHT-101 M1TBTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYr4RoRRUUN3ME2xNU4{QCEQvF2= NYnDNHVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
KYSE-150 Mme2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\IR2lEPTB;MUGuOVg1OSEQvF2= Mm\VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
MC-IXC NWq2PVhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTF{LkKyPVIh|ryP M3HhU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
D-423MG MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DTdWlEPTB;MUKuO|Y2PyEQvF2= M1vZfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
NY NYXvfGF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1GyRWlEPTB;MUSuPFkxOyEQvF2= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
HOS NV\tTpFyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPMdWhKSzVyPUG1MlY4OTlizszN NXnOeWM{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
NB7 NWrodXpPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrqZVd5UUN3ME2xOU45QTFizszN NHPBdmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
DMS-273 NYrhUI9HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTF4Lk[3NVMh|ryP MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
MDA-MB-361 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYmxNJB3UUN3ME2xO{4zPzFzIN88US=> M3XsfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
DU-145 M2DDWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTF6LkOyJO69VQ>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
NCI-H82 M3\2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTkOmdKSzVyPUG5Mlg{QDZizszN NEHRTVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
NCI-SNU-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXTTFFKSzVyPUKwMlAyQTZizszN MkD0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
GCT NXPXOIc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17t[mlEPTB;MkCuPFgzPCEQvF2= NEPYd2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
C2BBe1 MkHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTJzLkGwOVgh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
LB2241-RCC NYm2[VFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfj[Y9KSzVyPUKxMlg1PDFizszN M37QN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
COLO-829 NUXhW|RVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTJ{LkG4O|Eh|ryP NV:5RZV1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
EW-11 MoHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzQfYh6UUN3ME2yNk45ODJ{IN88US=> NHiyZlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
NCI-H526 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\EOmlEPTB;MkOuOFcyPyEQvF2= M37ieFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
SF295 M2HRbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn0fpAyUUN3ME2yOE4xOjV{IN88US=> M2e2SVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
D-566MG MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXscYh[UUN3ME2yOU4zQTR|IN88US=> M2niRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFQ4OzRzNz:nQnNCVkeHUkyvZV4>
8505C NFTydWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknlTWM2OD1{NT62N|MyKM7:TR?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
HT-29 M4LW[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJ4LkC0N|Eh|ryP NFTaO5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
NBsusSR MkjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PXTWlEPTB;Mk[uPFAxPiEQvF2= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
BV-173 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTJ6LkOxPFIh|ryP MmPyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
CTB-1 Mnf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fSWGlEPTB;M{CuNVA{OSEQvF2= MoK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOFc{PDF5Lze+V2FPT0WUPD;hQi=>
JAR MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnP3TWM2OD1|Mj61N|cyKM7:TR?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
CAMA-1 M1;iUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTN|LkS2NVUh|ryP NXruRnA2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
CAL-51 MmruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTN2LkexO|Yh|ryP MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly0O|M1OTdxJ{7TRW5ITVJ:L3G+
A172 NX;tOFY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPwcopKSzVyPUO3MlQ6OjFizszN NIO3U5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
QIMR-WIL MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;MPGlEPTB;M{iuNFcxQCEQvF2= NXLUcolnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
AsPC-1 NIr0V3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnT1TWM2OD1|OD60OlUyKM7:TR?= NYTNVmx5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPDd|NEG3M{c,W0GQR1XSQE9iRg>?
MKN7 M{DR[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofVTWM2OD1|OT6wNFc6KM7:TR?= NGLCcXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw1PzN2MUevK|5USU6JRWK8M4E,
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medulloblastoma cell M17jV2FvfGm2dX3vdkBie3OjeR?= NHHCUJFCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBud3W|ZTDt[YR2dGyxYnzhd5RwdWFiY3XscJMhgGWwb3fyZYZ1\WRiaX6gVJRkcCBtLz2gcY92e2ViYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hfHWvb4Kgeo9tfW2nIHH0JFEzNjVibXevb4ctKHCxIHLp[E4> NY\1eoQ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3NVYzQTZpPkG5O|E3Ojl4PD;hQi=>
S12 MVnGeY5kfGmxbjDhd5NigQ>? NYjifVhWPDhiaILz MnPoTY5pcWKrdHnvckBw\iCqdX3hckBUUEhicHH0bJdigSCrbjDtc5V{\SCVMUKgZ4VtdHNiYYPz[ZN{\WRiYYOgS2xKNW2nZHnheIVlKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBi\nSncjC0PEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6KGmwIIDy[ZNmdmOnIH;mJFEhdWdxbVygbJVu[W5iYXzwbIEuOS2jY3nkJIdtgWOxcILveIVqdi5? NEH2XZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUSzPFUzPyd-MkG0N|g2Ojd:L3G+
Shh Light2 NXrreYl2TnWwY4Tpc44h[XO|YYm= Mlz3NE4yKHWP MkH4N|YhcHK| NUjQfmRUUW6qaXLpeIlwdiCxZjDTcY8udWWmaXH0[YQhUGhic3nncoFtdGmwZzDwZZRpf2G7IHnuJI1wfXOnIGPobEBNcWeqdEKgZ4VtdHNiYYPz[ZN{\WRiYYOgd5VxeHKnc4Ppc44hd2ZiR3zpNU1uWk6DIHX4dJJme3Orb36gZZQhOC5zIIXNJI1m[XO3cnXkJIFnfGW{IEO2JIhzeyCkeTDSWE1yWEOUIHHuZYx6e2m|Lh?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzd|NkC2N{c,Ojd5M{[wOlM9N2F-
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A549 NUWwOmZ2SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NEjYbYkyOCC3TR?= NWXyV|BwPDhiaILz NIjjXY1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[XRiMUCgeW0h[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfU4> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR7MUS1PUc,OjR2OUG0OVk9N2F-
HCT116 NVXEfIVrSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3TmWlExKHWP M4D1eVQ5KGi{cx?= MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBifCBzMDD1UUBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5Mi=> NEf0Z2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES5NVQ2QSd-MkS0PVE1PTl:L3G+
NIH/3T3 Mlf4SpVv[3Srb36gZZN{[Xl? MVKxNEB2VQ>? NEnWVppKdmirYnn0bY9vKG:oIFjl[IdmcG:pIIPp[45idGmwZzDpckBud3W|ZTDOTWgwO1R|IHPlcIx{KGG|c3Xzd4VlKGG|IHTve44hemWpdXzheIlwdiCxZjDtVHREUDFibWLORUBmgHC{ZYPzbY9vKGG2IEGwJJVONg>? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR7MUS1PUc,OjR2OUG0OVk9N2F-
MSC M3TQZWZ2dmO2aX;uJIF{e2G7 NFfZVmgzOCC2bzC4NEB2VQ>? NVfTcot3UW6qaXLpeIlwdiCxZjDo[YRo\WixZzDzbYdv[WyrbnegbY4hdW:3c3WgUXNEKGOnbHzzJIF{e2W|c3XkJIF{KGSxd36gdoVofWyjdHnvckBw\iCjbHvhcIlv\SCyaH;zdIhifGG|ZTDheEAzOCC2bzC4NEB2VS5? MlLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2OUG0OVkoRjJ2NEmxOFU6RC:jPh?=
SK-N-MC NYLyNldoeUiWUzDhd5NigQ>? MnzidWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIOu MmnIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
TC32 NIO2XIpyUFSVIHHzd4F6 MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzzMi=> NGLBNnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NIH3T3-Luc NYjs[ZlsTnWwY4Tpc44h[XO|YYm= NWW5NFRSOSC3TR?= NWnwWXR1PDhiaILz M3PKemlvcGmkaYTpc44hd2Zic33vMY1m\GmjdHXkJIhm\GenaH;nJJNq\26jbHnu[{Bx[XSqd3H5JIlvKG2xdYPlJG5KUDOWMz3MeYMh[2WubIOgZZN{\XO|ZXSgZZMh\G:5boLl[5Vt[XSrb36gc4YhT2yrIH3SUmEh\XiycnXzd4lwdiCjdDCxJJVOKGGodHXyJFQ5KGi{czDifUBz\WGuLYTpcYUhWEOUIHHuZYx6e2m|Lh?= NYDhV3JbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0PVk1QDNpPkK5OFk6PDh|PD;hQi=>
C3H10T1/2 M4LZU2Z2dmO2aX;uJIF{e2G7 NWfIcpFHOjRiaILz MmHZTY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigS2vZXTpZZRm\CCJTFmxJI1TVkFiZYjwdoV{e2mxbjDpckBud3W|ZTDDN2gyOFRzL{KgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KFKWLWDDVkBidmGueYPpd{BqdiCycnXz[Y5k\SCxZjCoNXItO2GULETTMFdiWilvN3GtcYV1cHmuLUGtLEhTMS14LX3leIh6dGincIThck0zNXmuKX;jeIFpgWS{bz2xTE1qdmSnbj20MZltKDNvaInkdo95gWKnborvZZRmNg>? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd|MEm4OEc,OjR5M{C5PFQ9N2F-
C3H10T1/2 Ml;uSpVv[3Srb36gZZN{[Xl? MVWyOEBpenN? MVzJcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6NW2nZHnheIVlKEeOSUGgcXJPSSCneIDy[ZN{cW:wIHnuJI1wfXOnIFOzTFExXDFxMjDj[YxteyCjZoTldkAzPCCqcoOgZpkhWlRvUFPSJIFv[Wy7c3nzJIlvKHC{ZYPlcoNmKG:oIG\EN{4> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd|MEm4OEc,OjR5M{C5PFQ9N2F-
NIH/3T3 NFL3dlVHfW6ldHnvckBie3OjeR?= M4nNWVExOCCwTR?= NFPHbmg{PiCqcoO= Ml;JTY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIF{e2W|c3XkJIF{KGSxd37y[Yd2dGG2aX;uJI9nKFOqaD3pcoR2[2WmIFfsbVEhdVKQQTDlfJBz\XO|aX;uJIxmfmWuczDheEAyODBibl2gZYZ1\XJiM{[gbJJ{KGK7IGLUMZFRS1JiYX7hcJl{cXNw NUf5VWE4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4O|M{ODNpPkK4PFc{OzB|PD;hQi=>
C3H10T1/2 NYrs[WlmTnWwY4Tpc44h[XO|YYm= MVixNFAhdk1? NH7VdmI{PiCqcoO= MYTJcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGmwIH3veZNmKEN|SEGwWFEwOiClZXzsd{Bie3Onc4Pl[EBieyCmb4fudoVofWyjdHnvckBw\iCVaHitbY5lfWOnZDDHcIkyKG2UTlGg[ZhxemW|c3nvckBt\X[nbIOgZZQhOTByIH7NJIFnfGW{IEO2JIhzeyCkeTDSWE1yWEOUIHHuZYx6e2m|Lh?= NUjvOIJuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4O|M{ODNpPkK4PFc{OzB|PD;hQi=>
NIH/3T3 NYnuSGZrTnWwY4Tpc44h[XO|YYm= M4fnWVExOCCwTR?= MUezOkBpenN? MWfJcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGmwIH3veZNmKE6LSD:zWFMh[2WubIOgZZN{\XO|ZXSgZZMh\G:5boLl[5Vt[XSrb36gc4YhW2iqLXnu[JVk\WRicITjbFEhdVKQQTDlfJBz\XO|aX;uJIxmfmWuczDheEAyODBibl2gZYZ1\XJiM{[gbJJ{KGK7IGLUMZFRS1JiYX7hcJl{cXNw M1LWWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEezN|A{Lz5{OEi3N|MxOzxxYU6=
C3H10T1/2 NEnDT29HfW6ldHnvckBie3OjeR?= M33F[FExOCCwTR?= MU[zOkBpenN? NHK2e3hKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIFOzTFExXDFxMjDj[YxteyCjc4Pld5Nm\CCjczDkc5dvemWpdXzheIlwdiCxZjDTbIgucW6mdXPl[EBxfGOqMTDtVm5CKGW6cILld5Nqd25ibHX2[Yx{KGG2IEGwNEBvVSCjZoTldkA{PiCqcoOgZpkhWlRvcWDDVkBidmGueYPpd{4> Mmn2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6N{OzNFMoRjJ6OEezN|A{RC:jPh?=
medulloblastoma cell MYrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MWT1dEB1dyB|MDD1US=> NI\h[5k4OiCqcoO= MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKFC2Y3irM{0heDV|LT:tJI1m\HWubH;icIF{fG:vYTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDDwdo9tcW[ncnH0bY9vKHWyIITvJFMxKHWPIHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[Xlw MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh5M{OwN{c,Ojh6N{OzNFM9N2F-
medulloblastoma cell Mn7PRZBweHSxc3nzJIF{e2G7 NYDwV4VCUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBud3W|ZTDQeINpMy9vIIC1N{0wNSCvZXT1cIxw[myjc4TvcYEh[2WubIOgbY1xdGGwdHXkJIlvKGG2aIntbYMhdnWmZTDtc5V{\SCjdDCxNk42KG2pL3vnMEBqeCCkaXSg[o9zKDF3IHPvcpNm[3W2aY\lJIRigXNiYomgWHVPTUxiYYPzZZkv NVjPZ|k3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki4O|M{ODNpPkK4PFc{OzB|PD;hQi=>
NIH/3T3 MXXGeY5kfGmxbjDhd5NigQ>? NVPIfGFFUW6qaXLpeIlwdiCxZjDo[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDlfJBz\XO|ZXSgbY4hdW:3c3WgUmlJNzOWMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGinZHflbI9oNWmwZIXj[YQhT2yrLUKgZYNkfW23bHH0bY9vKGG2IITpdEBw\iCycnntZZJ6KGOrbHnhJIJ6KESDUFmgd5RicW6rbnegZoF{\WRiY3;u[o9k[WxibXnjdo9{[2:yaXOgZY5idHm|aYOu Mn[wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MUC1PVEoRjJ5OEGwOVkyRC:jPh?=
NIH/3T3 M3PIfGZ2dmO2aX;uJIF{e2G7 M1mzW2lvcGmkaYTpc44hd2ZiaHXk[4Vpd2dic3nncoFtcW6pIIDheIh4[XliaX6gcY92e2ViTlnIM|NVOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIhm\GenaH;nMYlv\HWlZXSgV41wNUWJRmCgZ4ltcWG{eTD0doFve2yxY3H0bY9vKGK7IFTBVGkhe3SjaX7pcoch[mG|ZXSgZ49v\m:lYXygcYlkem:|Y3;wbYMh[W6jbInzbZMv NGPPbFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU6OSd-Mke4NVA2QTF:L3G+
medulloblastoma cell MkDBRY51cS22dX3vdkBie3OjeR?= MW\BcpRqNXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViUITjbEswNSCyNUOtM{0hdWWmdXzsc4Jt[XO2b33hJINmdGy|IHntdIxidnSnZDDpckBifGi7bXnjJI52\GVibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiMkCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CC2d3nj[UBl[WmueTD2bYEh\2G4YXflJI1m[XO3cnXkJIV3\XK7IH;0bIVzKGSjeTDkeZJqdmdiY3;tdI92dmRiZH;zbY5oNg>? MnLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5M{m3NVQoRjJ7N{O5O|E1RC:jPh?=
C3H10T1/2 NYj1VWtjTnWwY4Tpc44h[XO|YYm= MX60MlEhfG9iMUCwNEBvVQ>? NFf0T4RCdGyxc4TldolkKGmwaHnibZRqd25ib3[gV41wKGmwIH3veZNmKEN|SEGwWFEwOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJB2em2xcoDoZY1qdmVvaX7keYNm\CCJbHmxJJRz[W6|Y4LpdJRqd26jbDDhZ5Rqfmm2eTDheEA1NjFidH:gNVAxOCCwTTDifUByWEO{IHHuZYx6e2m|Lh?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzB5NEW0NUc,OjNyN{S1OFE9N2F-
C3H10T1/2 MXXGeY5kfGmxbjDhd5NigQ>? M1Lvb|QvOSC2bzCxNFAxKG6P NV;zU|RXS2:vcHX0bZRqfmViaX7obYJqfGmxbjDv[kBUdW9iaX6gcY92e2ViQ{PINVBVOS9{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhW0GJLXnu[JVk\WRiR3zpNUB1emGwc3PybZB1cW:wYXygZYN1cX[rdImgZZQhPC5zIITvJFExODBibl2gZpkheVCFUjDhcoFtgXOrcz6= NIXwNIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C3OFU1OSd-MkOwO|Q2PDF:L3G+
Assay
Methods Test Index PMID
Western blot Bcl-2 / Bax p53 / Cyclin D1 / p21 Gli1 / SOX2 / OCT4 p-GSK3β / GSK3β / p-Akt / Akt / Gli1 Fas / DR4 / DR5 / Cleaved PARP / Bcl-2 / Cleaved caspase-3 / PDGFRα 28195165 26418365 27143997 22087285
Immunofluorescence Gli1 / Gli2 22087285
Growth inhibition assay Cell viability 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]
  • 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。
动物实验:[4]
  • Animal Models: Ptch(+/-)异体移植物模型
  • Dosages: 25 mg/kg,92 mg/kg
  • Administration: 口服

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

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 Completed Drug: Vismodegib Carcinoma Basal Cell University of Michigan Rogel Cancer Center July 15 2015 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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