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 94 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 M33QNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTlS2txUUN3ME20PE4{OTR{IN88US=> M1fKc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
SNU-C1 Mni1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;XNGlEPTB;MkSuPVExPSEQvF2= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
NCI-H524 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjYdGlKSzVyPUK0MlM5OTJizszN MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
NCI-H82 M3WxbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJ|LkW1NlYh|ryP NVnUbZR2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
RT4 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4C2RWlEPTB;MkOuN|I5OiEQvF2= NX;4RVMyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
LB771-HNC M{\aOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT4TWM2OD1{Mj60PFE{KM7:TR?= NHPXbFI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
SW780 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkG1TWM2OD1{MT6xN|E5KM7:TR?= MlXSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H345 NIT4WlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTJzLki3O|kh|ryP M4D5dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H1563 NIXFS2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPqT3g4UUN3ME2xPU44QDh6IN88US=> NVf5PHlwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
DV-90 M13wZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUntRYsyUUN3ME2xPE46QTR3IN88US=> MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
Hs-578-T NInHZo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP5V4NHUUN3ME2xPE42PzV7IN88US=> NELaZWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-H2452 NHvWO5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfJTWM2OD1zND63N{DPxE1? NIjSTVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
TGBC24TKB MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfiTWM2OD1zMz61Nlkh|ryP NYXYZYpoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
SW948 NF3vNYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\F[|Y3UUN3ME2xNE44PTFzIN88US=> M1LLRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
CPC-N M2LBW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTFzLkCwO{DPxE1? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
SCC-3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTFyLkW2O|kh|ryP NEm5e|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
SBC-1 NWfEUmlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjUc2JKSzVyPUmuPVM3PTZizszN Mom4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H187 NYLPVFN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTjTWM2OD17LkWxPFM2KM7:TR?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
NCI-H1838 NE\uZ2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPG[FRKSzVyPUiuOVE4OzFizszN MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
NCI-H322M NYHFeHdtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjuTJIxUUN3ME25MlE3OjhzIN88US=> NF\r[4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
TT NWTLOnk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DUbmlEPTB;OD6zN|AxQSEQvF2= MmfQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
TCCSUP MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HuOWlEPTB;Nj62NFM1QSEQvF2= M3n3e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
LC-1F MlzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3VWZpKSzVyPU[uNFkzQTFizszN M{fUXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
RPMI-8866 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{X4XWlEPTB;NT64OFc6OiEQvF2= NEDJOoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-H1623 M{TldWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzPOZJKSzVyPUWuPFM2PTZizszN NH;2T249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
MDA-MB-157 MoTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHYTWM2OD13Lk[2OFQ{KM7:TR?= MkXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
ES5 NU\VSG9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLmTWM2OD13Lk[xNVc5KM7:TR?= MnvaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
A498 NF:3Wo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXm4OnZVUUN3ME21MlIyOjVzIN88US=> M2i1dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H1395 NGnUdnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTVwMUC2N|Mh|ryP MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
SiHa NXjXfI9mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTRwOUWyNFMh|ryP NIPGepE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-H209 NVvpTXhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTRwN{i1O|Ih|ryP M{LGUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
TE-5 NEfKR3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILzS25KSzVyPUSuOVYyPDdizszN NX3QdJFFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
MFM-223 MmHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDMdmw2UUN3ME2zMlM3ODl5IN88US=> NXXNe3JbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
COLO-800 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHtZZNKSzVyPUOuN|M5QTdizszN M3XXSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
D-283MED NFfOWXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTNwMUi5N|ch|ryP MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
HCC1395 NYTvdlNlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlraTWM2OD1{Lkm4OlAzKM7:TR?= NX\yPIV7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
P12-ICHIKAWA NIm5OXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGq2NHVKSzVyPUKuPFIxPDZizszN MkKwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
HT55 NH\ReZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTJwNkKwNVkh|ryP MnvZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
UMC-11 NEP1SIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTJwN{i3NVUh|ryP NVPWXnVwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
AsPC-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{j2[mlEPTB;Mj61N|kzQSEQvF2= NHzjbVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK|5USU6JRWK8M4E,
NCI-H889 NF23ZYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\uTWM2OD1{LkW2O|A3KM7:TR?= Mn;uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
HCC1143 MmXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIflbXNKSzVyPUKuOVA3PThizszN M37HZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
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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.
  • (Only for Reference)
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.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 93 mg/mL warmed
(199.76 mM)
Water Insoluble
Ethanol ''31 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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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