Luminespib (NVP-AUY922)

Catalog No.S1069 Synonyms: AUY-922, VER-52296

For research use only.

Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.

Luminespib (NVP-AUY922) Chemical Structure

CAS No. 747412-49-3

Selleck's Luminespib (NVP-AUY922) has been cited by 97 publications

Purity & Quality Control

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Biological Activity

Description Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Targets
HSP90α [1]
(Cell-free assay)
HSP90β [1]
(Cell-free assay)
13 nM 21 nM
In vitro

NVP-AUY922 inhibits proliferation of various human cancer cell lines in vitro, with an average GI50 of 9 nM. [1] The IC50 values of NVP-AUY922 fall in the range of 2 to 40 nM in these gastric cancer cell lines. IC50 value for the BEAS-2B cells is 28.49 nM. Treatment with NVP-AUY922 does not influence the expression of HSP90, but expression of HSP70 gets elevated by NVP-AUY922 treatment. NVP-AUY922 increases the binding of HSP70 to HSP90. NVP-AUY922 causes p23 dissociation from the HSP90 complex and can then recruit HSP70 to the HSP90 complex. [1] After the treatment with NVP-AUY922, expression of receptor tyrosine kinases including VEGFR1, 2, 3 and PDGFRɑ is decreased. A decrease is also noticed in the expression of Akt and phospho-Akt. Meanwhile, treatment with NVP-AUY922 causes decreased expression of HER-2 in NCI-N87 cells. NVP-AUY922 treatment results in binding of HSP90 to client proteins and setting them up as targets for degradation by the proteasome. NVP-AUY922 can influence cell growth by affecting multiple signaling pathways. In addition, treatment with the proteasome inhibitor, MG132, restores expression of thymidylate synthase, which is decreased by NVP-AUY922. NVP-AUY922 increases the expression of cleaved caspase-3 leading to apoptosis in HSC-2 cells.[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-SNU-16 MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTR6LkOxOFIh|ryP MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
SNU-C1 MmDFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rRNGlEPTB;MkSuPVExPSEQvF2= NYjW[3cyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
NCI-H524 NGXud|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\L[2lEPTB;MkSuN|gyOiEQvF2= NVHrWGdmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
NCI-H82 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3oO2JKSzVyPUKzMlU2OjZizszN NV;SVmttRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
RT4 MmrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTJ|LkOyPFIh|ryP M{Pvb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
LB771-HNC M3:wb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vrTGlEPTB;MkKuOFgyOyEQvF2= NVL6N5RiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
SW780 NFrhTHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlSzTWM2OD1{MT6xN|E5KM7:TR?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
NCI-H345 Ml;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvZXHJuUUN3ME2yNU45Pzd7IN88US=> MlvKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H1563 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHpbJl5UUN3ME2xPU44QDh6IN88US=> NETOd2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
DV-90 NHLuNoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoWyTWM2OD1zOD65PVQ2KM7:TR?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
Hs-578-T NE\jWVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTF6LkW3OVkh|ryP NW[5T5AxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
NCI-H2452 NWLPOJZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3FNGZRUUN3ME2xOE44OyEQvF2= NITUfJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
TGBC24TKB MmDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPBVopGUUN3ME2xN{42OjlizszN M{DLeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
SW948 NULMXZhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHucYhKSzVyPUGwMlc2OTFizszN MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
CPC-N NXO2fVhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HYO2lEPTB;MUGuNFA4KM7:TR?= M{LsPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
SCC-3 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jqZWlEPTB;MUCuOVY4QSEQvF2= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
SBC-1 M3rP[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTlwOUO2OVYh|ryP NXHWbZlORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
NCI-H187 NGHwOJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrPNVdRUUN3ME25MlUyQDN3IN88US=> NH35R|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-H1838 MlH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfReVhKSzVyPUiuOVE4OzFizszN MnexQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H322M NVnVSpFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTlwMU[yPFEh|ryP NHiwZWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
TT MoiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfzTWM2OD16LkOzNFA6KM7:TR?= NVrlcWJNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
TCCSUP NGj1fFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTZwNkCzOFkh|ryP NVvGSWpXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
LC-1F MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fwNmlEPTB;Nj6wPVI6OSEQvF2= M4XNRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
RPMI-8866 MnvoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2q5NmlEPTB;NT64OFc6OiEQvF2= NFnyUoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-H1623 NIHJbVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTVwOEO1OVYh|ryP Mm\qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
MDA-MB-157 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mor2TWM2OD13Lk[2OFQ{KM7:TR?= M2jWN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
ES5 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnobVVtUUN3ME21MlYyOTd6IN88US=> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
A498 MmLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUm1VoVxUUN3ME21MlIyOjVzIN88US=> M{fGcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H1395 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTVwMUC2N|Mh|ryP NF7jWJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
SiHa M4rkV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jHZmlEPTB;ND65OVIxOyEQvF2= MormQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H209 NXvFS|VbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j1XGlEPTB;ND63PFU4OiEQvF2= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
TE-5 NWG1OIJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTRwNU[xOFch|ryP NFvF[Xc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
MFM-223 NILaT4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPBTWM2OD1|LkO2NFk4KM7:TR?= M2H3WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
COLO-800 MnTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXFTWM2OD1|LkOzPFk4KM7:TR?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
D-283MED NYLoXmljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2T0TWlEPTB;Mz6xPFk{PyEQvF2= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
HCC1395 M2OxdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTJwOUi2NFIh|ryP MlnDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
P12-ICHIKAWA M2Dzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDQTWM2OD1{LkiyNFQ3KM7:TR?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
HT55 M3TtUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfnUnZKSzVyPUKuOlIxOTlizszN M4f2dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
UMC-11 M1rrWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fYVGlEPTB;Mj63PFcyPSEQvF2= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
AsPC-1 NILL[YxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvLTWM2OD1{LkWzPVI6KM7:TR?= MmHIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H889 NUjnPIlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTJwNU[3NFYh|ryP NXraUmJZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
HCC1143 M1;lWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTJwNUC2OVgh|ryP NHLCSYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
FTC-133 NWPtZmNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHj4UFVKSzVyPUKuOVM3QDlizszN NHPBfII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
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LB2241-RCC NF7Gc3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPjTWM2OD1yLkCzOlQzKM7:TR?= M{e1NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
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GCT M{TMRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7KcGJKSzVyPUCuNFQyPjFizszN MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
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LS-1034 NHPPVotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7HdXVKSzVyPUCuNFQyQTFizszN NVPQUnJZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
LAMA-84 Ml;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M36xbWlEPTB;MD6wOFE4OSEQvF2= NUDPNWYyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
NCI-H358 NUe4dXVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjaeopsUUN3ME2wMlA1OjF{IN88US=> M3L4R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NB13 MoPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HIXmlEPTB;MD6wOFIzPyEQvF2= M2HLblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
TE-9 NID0b3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DEcWlEPTB;MD6wOFI{PyEQvF2= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
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CAL-120 MofqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzpTWM2OD1yLkC0NlQyKM7:TR?= NWK4[FBsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
DJM-1 NVrwXnp6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYexeodtUUN3ME2wMlA1Ojd{IN88US=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
VA-ES-BJ NH3VT|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTBwMESyPVIh|ryP NFPU[4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
SK-MEL-24 Moj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXuTJhKSzVyPUCuNFQzQDNizszN NGjUdJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
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COLO-680N MoO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwMES0NFch|ryP MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
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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
In vivo Treatment with NVP-AUY922 causes a robust antitumor response and inhibits p-Akt and VEGF expression in an HSC-2 xenograft model. [2] In BT474, NVP-AUY922 shows complete loss of ERBB2 and substantial depletion of ERα, in addition to reductions in CDK4 and phospho-ERK1/2. [3]

Protocol (from reference)

Kinase Assay:[3]
  • Kinase assay:

    NVP-AUY922 is dissolved in DMSO at a concentration of 10 mM. NVP-AUY922 is assessed against HSP90α, HSP90β, GRP94, TRAP-1, HSP72, and topoisomerase II. Profiling against a panel of kinases has been carried out and screening against a panel of additional enzymes and receptors is performed at Cerep.

Cell Research:[1]
  • Cell lines: Human gastric cancer cells NCI-N87
  • Concentrations: 1 μM
  • Incubation Time: 3 days
  • Method: Human gastric cancer cells NCI-N87 (5-7 ×103 in 50 μL/well) are seeded in 96-well plates and incubated at 37 °C for 24 hours, followed by NVP-AUY922 treatment for 1-3 days at 37 °C. After treatment, the cells are assayed by MTT method and analyzed by microplate reader.
Animal Research:[3]
  • Animal Models: Female NCr athymic mice bearing WM266.4 human melanoma xenografts
  • Dosages: 50 mg/kg
  • Administration: Administered via i.v. or i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 465.54
Formula

C26H31N3O5

CAS No. 747412-49-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCNC(=O)C1=NOC(=C1C2=CC=C(C=C2)CN3CCOCC3)C4=CC(=C(C=C4O)O)C(C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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