Luminespib (NVP-AUY922)

目录号:S1069 别名: AUY-922, VER-52296

仅限科研使用

Luminespib (AUY-922, NVP-AUY922, VER-52296)是一种高效的HSP90抑制剂,无细胞试验中作用于HSP90α/βIC50为13 nM /21 nM,对HSP90家族成员GRP94和TRAP-1具有稍弱的作用,与任何小分子HSP90配体均可紧密结合。Luminespib (AUY-922, NVP-AUY922)可有效下调并使IGF-1Rβ蛋白不稳定,从而导致抑制生长、自噬和凋亡。Phase 2。

Luminespib (NVP-AUY922) Chemical Structure

CAS: 747412-49-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2620.46 现货
RMB 1303.22 现货
RMB 3853.15 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Luminespib (NVP-AUY922)发表文献99篇:

产品安全说明书

HSP (HSP90)抑制剂选择性比较

相关HSP (HSP90)产品

生物活性

产品描述 Luminespib (AUY-922, NVP-AUY922, VER-52296)是一种高效的HSP90抑制剂,无细胞试验中作用于HSP90α/βIC50为13 nM /21 nM,对HSP90家族成员GRP94和TRAP-1具有稍弱的作用,与任何小分子HSP90配体均可紧密结合。Luminespib (AUY-922, NVP-AUY922)可有效下调并使IGF-1Rβ蛋白不稳定,从而导致抑制生长、自噬和凋亡。Phase 2。
靶点
HSP90α [1]
(Cell-free assay)
HSP90β [1]
(Cell-free assay)
13 nM 21 nM
体外研究

体外研究时NVP-AUY922抑制多种人类肿瘤细胞系的增殖,GI50平均值为9 nM。NVP-AUY922作用于胃癌细胞时IC50值为2到40 nM。NVP-AUY922作用于BEAS-2B细胞IC50为28.49 nM。使用NVP-AUY922时不影响HSP90的表达,但是提高HSP70的表达。NVP-AUY922增强HSP70与HSP90的结合能力。NVP-AUY922造成p23与HSP复合体的分离。NVP-AUY922能使HSP70结合到HSP90复合体。使用NVP-AUY922,引起酪氨酸激酶受体如VEGFR1, 2, 3和PDGFR-ɑ的表达下降,Akt和p-Akt也下降。另外,NVP-AUY922作用于NCI-N87细胞,引起HER2表达下降。NVP-AUY922提高HSP90与目标蛋白的结合力,然后通过蛋白酶使蛋白降解。NVP-AUY922可以改变多条信号通路而影响细胞生长。此外,使用蛋白酶抑制剂MG132,恢复由于使用NVP-AUY922而降低的胸核苷酸合酶的重新表达。[1]NVP-AUY922提高cleaved caspase-3的表达,及导致HSC-2 细胞凋亡。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-SNU-16 MnXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnqbY9KSzVyPUS4MlMyPDJizszN MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
SNU-C1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDiTWM2OD1{ND65NVA2KM7:TR?= M13TV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H524 NG\IUFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFX5[IxKSzVyPUK0MlM5OTJizszN M2XkblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H82 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTJ|LkW1NlYh|ryP NX3SUXg6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
RT4 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXDTWM2OD1{Mz6zNlgzKM7:TR?= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
LB771-HNC MoLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nBeGlEPTB;MkKuOFgyOyEQvF2= NIDEcGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
SW780 MnzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nI[GlEPTB;MkGuNVMyQCEQvF2= Mn2zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H345 M1iwV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\Ico94UUN3ME2yNU45Pzd7IN88US=> MnvYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H1563 Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;ZTGlEPTB;MUmuO|g5QCEQvF2= MlOzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
DV-90 NInDd5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33J[2lEPTB;MUiuPVk1PSEQvF2= NYLn[YRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
Hs-578-T MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTF6LkW3OVkh|ryP MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
NCI-H2452 NELzXGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vmV2lEPTB;MUSuO|Mh|ryP NEX5TVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
TGBC24TKB NITFWIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInhPW5KSzVyPUGzMlUzQSEQvF2= NXnoPFBbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
SW948 NWX5Tm04T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTFyLke1NVEh|ryP NEfOVXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
CPC-N NFmwWmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGH0R5ZKSzVyPUGxMlAxPyEQvF2= NUD4fXBnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
SCC-3 M2LKRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moq3TWM2OD1zMD61Olc6KM7:TR?= NHHRbGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
SBC-1 M1P0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjINZl7UUN3ME25Mlk{PjV4IN88US=> NXPPTnFORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
NCI-H187 M4D4O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTtTWM2OD17LkWxPFM2KM7:TR?= MoHOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H1838 MnrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnf0TWM2OD16LkWxO|MyKM7:TR?= MkfEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H322M MnPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjuTWM2OD17LkG2NlgyKM7:TR?= M1;4fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
TT NHWySY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXQTWM2OD16LkOzNFA6KM7:TR?= M3LnflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
TCCSUP M3zF[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGftU4xKSzVyPU[uOlA{PDlizszN NX;DXI5pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
LC-1F MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\NZlZKSzVyPU[uNFkzQTFizszN M3S3N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
RPMI-8866 NVfXWnY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHy1bVdKSzVyPUWuPFQ4QTJizszN NFXJZo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-H1623 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPwTWM2OD13LkizOVU3KM7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
MDA-MB-157 M{DmO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vudmlEPTB;NT62OlQ1OyEQvF2= NY\ufpZ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
ES5 MmnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGP6[lRKSzVyPUWuOlEyPzhizszN NX3NN|N4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
A498 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPnTWM2OD13LkKxNlUyKM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
NCI-H1395 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3X3NGlEPTB;NT6xNFY{OyEQvF2= Mkn2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
SiHa NHvqeWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPiTWM2OD12Lkm1NlA{KM7:TR?= NWrWPWt4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
NCI-H209 NW[4VIdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{K0VmlEPTB;ND63PFU4OiEQvF2= NH3SbFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
TE-5 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTRwNU[xOFch|ryP NFv0fmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
MFM-223 NXjLXol7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjBepF4UUN3ME2zMlM3ODl5IN88US=> NFHJXlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
COLO-800 NFHBS4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3e3e2lEPTB;Mz6zN|g6PyEQvF2= NVnwNY1YRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
D-283MED NIrz[otIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTNwMUi5N|ch|ryP NYDSXYRPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
HCC1395 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlruTWM2OD1{Lkm4OlAzKM7:TR?= NGHZcGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
P12-ICHIKAWA NWPTR29zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfpZ2lKSzVyPUKuPFIxPDZizszN MlvoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
HT55 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33D[GlEPTB;Mj62NlAyQSEQvF2= NWjzdWRIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
UMC-11 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vnWmlEPTB;Mj63PFcyPSEQvF2= NIPmWXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
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ESS-1 M2\5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInQbopKSzVyPUCuNFc5PjhizszN NEHTdGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-SNU-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoK5TWM2OD1yLkC3PFg5KM7:TR?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
CP66-MEL NVvQd2ZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTBwMEe4PFch|ryP NITVbFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
Calu-6 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfqTWM2OD1yLkC3PVY2KM7:TR?= NIDyWWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
Assay
Methods Test Index PMID
Western blot p-ALK / ALK / p-AKT / AKT / p-ERK / ERK / TβRI / TβRII E-cadherin / Cleaved PARP / Bim HSP70 / Grp94 / Grp78 / p-eIF2α / CHOP / IRE1α / p-JNK CDK4 / HMGA2 23993685 24796583 26893968
Growth inhibition assay Cell viability 26893968
体内研究 使用NVP-AUY922可引起强的抗癌反应,可抑制HSC-2移植瘤模型中p-Akt和VEGF的表达。[2] 在12种实验肿瘤中观察到5种肿瘤衰退。体重降低<5%,且与HSP90相关的生物标签明显改变。BT474中, ERBB2完全缺失,ERα耗尽,且CDK4和磷酸化ERK1/2降低。[3]

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)

激酶实验:[3]
  • 激酶实验:

    NVP-AUY922溶解在DMSO中,浓度为10mM。通过作用于HSP90α, HSP90β, GRP94, TRAP-1, HSP72,和拓扑异构酶II评估NVP-AUY922的活性。

细胞实验:[1]
  • Cell lines: 人类胃癌细胞系NCI-N87
  • Concentrations: 1 μM
  • Incubation Time: 3天
  • Method: 人类胃癌细胞NCI-N87按5-7×103密度接种在96孔板中,每孔接种50ul,在37oC下温育24小时,然后用NVP-AUY922处理1到3天。实验处理后,使用MTT实验测细胞活力,用酶标仪分析。
动物实验:[3]
  • Animal Models: 携带WM266.4人类黑色素移植瘤的雌性NCr无胸腺鼠
  • Dosages: 50 mg/kg
  • Administration: 静脉注射或腹腔注射

溶解度(25°C)

体外

* 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 465.54
化学式

C26H31N3O5

CAS号 747412-49-3
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
NCT01772797 Completed Drug: LDK378|Drug: AUY922 Anaplastic Lymphoma Kinase (ALK)|Non-small Cell Lung Cancer Novartis Pharmaceuticals|Novartis June 2013 Phase 1
NCT01752400 Completed Drug: AUY922 Non Small Cell Lung Cancer Massachusetts General Hospital January 2013 Phase 2
NCT01613950 Completed Drug: AUY922|Drug: BYL719 Stomach Neoplasms Esophageal Neoplasms Metastatic Gastric Cancer Mutated PI3KCA Protein Overexpressed HER2 Protein Novartis Pharmaceuticals|Novartis December 2012 Phase 1
NCT01484860 Terminated Drug: AUY922 Adenocarcinoma of the Pancreas|Metastatic Disease University Health Network Toronto|Novartis Pharmaceuticals January 2012 Phase 2
NCT01402401 Terminated Drug: AUY922|Drug: Trastuzumab Advanced Gastric Cancer Novartis Pharmaceuticals|Novartis November 2011 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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