Luminespib (NVP-AUY922)

For research use only. Not for use in humans.

目录号:S1069 别名: AUY-922

Luminespib (NVP-AUY922) Chemical Structure

CAS No. 747412-49-3

Luminespib (AUY-922, NVP-AUY922)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。

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 2216.44 现货
RMB 3853.15 现货
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客户使用Selleck生产的Luminespib (NVP-AUY922)发表文献78篇:

产品安全说明书

HSP (HSP90)抑制剂选择性比较

生物活性

产品描述 Luminespib (AUY-922, NVP-AUY922)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 Mn3ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTR6LkOxOFIh|ryP MmTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
SNU-C1 NIXKWJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXMTWM2OD1{ND65NVA2KM7:TR?= M3;MW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H524 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\WZWlEPTB;MkSuN|gyOiEQvF2= NEfY[Zk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-H82 MnS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HVU2lEPTB;MkOuOVUzPiEQvF2= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
RT4 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTJ|LkOyPFIh|ryP NGPoPIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
LB771-HNC NWixTZhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXyzS4ViUUN3ME2yNk41QDF|IN88US=> M3T2ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
SW780 NH:4bphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmflTWM2OD1{MT6xN|E5KM7:TR?= M2jhd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H345 M1zaOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fjV2lEPTB;MkGuPFc4QSEQvF2= NWHhTlZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
NCI-H1563 NVrSSmN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTF7Lke4PFgh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
DV-90 NH\GXoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTF6Lkm5OFUh|ryP NFnCOFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
Hs-578-T Mo\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVOyZ3FRUUN3ME2xPE42PzV7IN88US=> NIXKflA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-H2452 MlK0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYT0eG83UUN3ME2xOE44OyEQvF2= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
TGBC24TKB M3naN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTF|LkWyPUDPxE1? M4exVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
SW948 NUThZWM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTFyLke1NVEh|ryP NXrsS5JCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
CPC-N NXnrcJA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnWdndKSzVyPUGxMlAxPyEQvF2= NYXPW4JGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
SCC-3 NXv1bnY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{L3XGlEPTB;MUCuOVY4QSEQvF2= M4\XdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
SBC-1 M3zGdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;4WXNKSzVyPUmuPVM3PTZizszN M{LEOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H187 NXLDN2FET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LrVmlEPTB;OT61NVg{PSEQvF2= M4fBU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H1838 NGnYbmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37s[mlEPTB;OD61NVc{OSEQvF2= NIrpXpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-H322M M2fCemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTlwMU[yPFEh|ryP MlixQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
TT NEfFVFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mln2TWM2OD16LkOzNFA6KM7:TR?= NF:4fYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
TCCSUP M2S1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWC1dYZQUUN3ME22MlYxOzR7IN88US=> M3TWSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
LC-1F MoD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17Oc2lEPTB;Nj6wPVI6OSEQvF2= MlTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
RPMI-8866 M2jyfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\5TWM2OD13Lki0O|kzKM7:TR?= M3zxT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H1623 M4WwZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXO4UHpYUUN3ME21Mlg{PTV4IN88US=> NVrSeY53RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
MDA-MB-157 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHld2xKSzVyPUWuOlY1PDNizszN NFLRSoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
ES5 MmLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\od5N4UUN3ME21MlYyOTd6IN88US=> NFLRb4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
A498 NUH1d2x4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTVwMkGyOVEh|ryP MlPIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H1395 Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHoS2ZKSzVyPUWuNVA3OzNizszN Mn:xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
SiHa NWP3TVVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHL3PYZKSzVyPUSuPVUzODNizszN NVfNeXdQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
NCI-H209 NVSwbGZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTRwN{i1O|Ih|ryP NX;SWI5URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
TE-5 MlfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHsR3h[UUN3ME20MlU3OTR5IN88US=> NUPHSpJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
MFM-223 Mm\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zMWGlEPTB;Mz6zOlA6PyEQvF2= M3X5dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
COLO-800 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\pTWM2OD1|LkOzPFk4KM7:TR?= Mk\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
D-283MED NEL4bZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1mzO2lEPTB;Mz6xPFk{PyEQvF2= MkP1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
HCC1395 NF7zcplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVH5XVVwUUN3ME2yMlk5PjB{IN88US=> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
P12-ICHIKAWA MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mle0TWM2OD1{LkiyNFQ3KM7:TR?= M4PS[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
HT55 NWXiTZVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2WyXWlEPTB;Mj62NlAyQSEQvF2= MlnWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
UMC-11 MmrES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHycJdJUUN3ME2yMlc5PzF3IN88US=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
AsPC-1 NUflPVZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXqTWM2OD1{LkWzPVI6KM7:TR?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
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Calu-6 MmHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nDbWlEPTB;MD6wO|k3PSEQvF2= NIHXfpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ALK / ALK / p-AKT / AKT / p-ERK / ERK / TβRI / TβRII; 

PubMed: 23993685     


Cells were treated with or without the indicated doses of 17-DMAG or AUY-922 for 3 h. Changes in ALK-related signaling and TGF-b receptors were analyzed using Western blot analysis. The densitometry values were determined relative to control of H2228 after normalization to b-actin protein.

E-cadherin / Cleaved PARP / Bim; 

PubMed: 23993685     


Cells were treated with crizotinib (1 mM), 17-DMAG (1 mM), or AUY-922 (1 mM) for the indicated times. Cell lysates were subjected to Western blot analysis using the indicated antibodies. The densitometry values were determined relative to control after normalization to b-actin protein.

HSP70 / Grp94 / Grp78 / p-eIF2α / CHOP / IRE1α / p-JNK; 

PubMed: 24796583     


CCA cells were incubated with 0.5 uM NVP-AUY922 for 0, 2, 4, 8, 16, and 24 h. Whole cell lysates were subjected to western blot analysis for HSP70, Grp94, Grp78, p-eIF2α, CHOP, IRE1α, and phosphor-JNK. β-Actin was used as the loading control.

CDK4 / HMGA2 ; 

PubMed: 26893968     


HCT116 cells were treated with NVP-AUY922 at the indicated concentrations for 48 hours. Cell extracts were analyzed using Western blotting with the antibodies for CDK4, Hsp70, and HMGA2, respectively.

23993685 24796583 26893968
Growth inhibition assay
Cell viability; 

PubMed: 26893968     


Cell viability assay was performed to determine the of HCT116 cells treated with various concentrations of NVP-AUY922 for 48 hours. *p < 0.05, **p < 0.01, ***p < 0.001. All experiments were performed in three independent experiments.

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]
- 合并

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]
- 合并
  • 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。
    (Only for Reference)
动物实验:[3]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 93 mg/mL warmed (199.76 mM)
Ethanol 31 mg/mL (66.58 mM)
Water 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):
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/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 465.54
化学式

C26H31N3O5

CAS号 747412-49-3
储存条件 粉状
溶于溶剂
别名 AUY-922

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

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

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID