Luminespib (NVP-AUY922)

Name: Luminespib (NVP-AUY922)
Brand: Selleck Chemicals
SKU: S1069
Rating: 5 (90 reviews)

For research use only.

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

90 publications

Luminespib (NVP-AUY922) Chemical Structure

CAS No. 747412-49-3

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.

Selleck's Luminespib (NVP-AUY922) has been cited by 90 publications

Cancer Cell, 2020, 37(3):371-386

PubMed: 32109374 ( click the link to review the publication )

Cancer Cell, 2019, 35(5):752-766

PubMed: 31085176 ( click the link to review the publication )

Nat Med, 2015, 10.1038/nm.3855

PubMed: 25939062 ( click the link to review the publication )

Cell, 2012, 31;150(5):987-1001.

PubMed: 22939624 ( click the link to review the publication )

Cell Rep, 2021, 34(11):108870

PubMed: 33730585 ( click the link to review the publication )

Haematologica, 2021, 10.3324/haematol.2021.278743

PubMed: 34162179 ( click the link to review the publication )

Cells, 2021, 10(6)1489

PubMed: 34199261 ( click the link to review the publication )

Cell Chem Biol, 2021, S2451-9456(21)00221-X

PubMed: 34077750 ( click the link to review the publication )

Int J Mol Sci, 2021, 22(5)2538

PubMed: 33802597 ( click the link to review the publication )

Sci Rep, 2021, 11(1):11103

PubMed: 34045581 ( click the link to review the publication )

Cell Stress Chaperones, 2021, 10.1007/s12192-021-01193-6

PubMed: 33629253 ( click the link to review the publication )

Neurobiol Dis, 2021, S0969-9961(21)00048-6

PubMed: 33600953 ( click the link to review the publication )

Nat Commun, 2020, 11(1):562

PubMed: 31992715 ( click the link to review the publication )

Genome Med, 2020, 18;12(1):17

PubMed: 32070411 ( click the link to review the publication )

Cell Rep, 2020, 31(12):107800

PubMed: 32579927 ( click the link to review the publication )

Front Immunol, 2020,

PubMed: 32903557 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(13):E4740

PubMed: 32635192 ( click the link to review the publication )

Int J Mol Med, 2020, 45(5):1543-1553

PubMed: 32323753 ( click the link to review the publication )

Exp Lung Res, 2020, 46(6):203-216

PubMed: 32400213 ( click the link to review the publication )

Korean J Physiol Pharmacol, 2020, 1;24(3):241-248

PubMed: 32395075 ( click the link to review the publication )

Nat Commun, 2019, 10(1):402

PubMed: 30679438 ( click the link to review the publication )

J Neurosci, 2019, 39(17):3332-3344

PubMed: 30696728 ( click the link to review the publication )

Cells, 2019, 8(8)

PubMed: 31370342 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(11):2097-2110

PubMed: 31395684 ( click the link to review the publication )
Front Endocrinol (Lausanne), 2019, 10:487

PubMed: 31379752 ( click the link to review the publication )

BMC Cancer, 2019, 19(1):102

PubMed: 30678647 ( click the link to review the publication )

Clin Exp Med, 2019, 10.1007/s10238-019-00587-2

PubMed: 31650359 ( click the link to review the publication )

Hepatology, 2019, 69(2):573-586

PubMed: 29356025 ( click the link to review the publication )

ACS Chem Neurosci, 2019, 10(6):2890-2902

PubMed: 31017387 ( click the link to review the publication )

Transl Lung Cancer Res, 2019, 8(4):340-351

PubMed: 31555510 ( click the link to review the publication )

Autophagy, 2018, 14(6):958-971

PubMed: 29561705 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(24):6548-6555

PubMed: 30154228 ( click the link to review the publication )

Mol Syst Biol, 2018, 14(3):e7858

PubMed: 29507054 ( click the link to review the publication )

J Immunol, 2018,

PubMed: 29445007 ( click the link to review the publication )

J Virol, 2018, 92(5)e01415-17

PubMed: 29212943 ( click the link to review the publication )

J Cell Mol Med, 2018, 22(3):1792-1804

PubMed: 29363851 ( click the link to review the publication )

BMB Rep, 2018, 51(12):660-665

PubMed: 30591093 ( click the link to review the publication )

Oncotarget, 2018, 9(100):37379-37392

PubMed: 30647839 ( click the link to review the publication )

Oncotarget, 2018,

PubMed: 29599910 ( click the link to review the publication )

Oncotarget, 2018, 9(13):11303-11321

PubMed: 29541415 ( click the link to review the publication )

Cancer Lett, 2017, 411:19-26

PubMed: 28987383 ( click the link to review the publication )

Cancer Chemother Pharmacol, 2017, 80(4):673-684

PubMed: 28779264 ( click the link to review the publication )

Biochem Biophys Res Commun, 2017, 487(2):313-319

PubMed: 28412368 ( click the link to review the publication )

Onco Targets Ther, 2017, 10:2219-2226

PubMed: 28458565 ( click the link to review the publication )

Sci Rep, 2017, 7(1):201

PubMed: 28298630 ( click the link to review the publication )

Oncotarget, 2017, 8(61):104193-104205

PubMed: 29262632 ( click the link to review the publication )

Oncotarget, 2017, 8(28):45298-45310

PubMed: 28424411 ( click the link to review the publication )

Oncotarget, 2017, 8(35):58771-58780

PubMed: 28938595 ( click the link to review the publication )
Oncogene, 2016, 35(3):333-43

PubMed: 25823022 ( click the link to review the publication )

Cancer Lett, 2016, 372(1):75-81

PubMed: 26723875 ( click the link to review the publication )

PLoS Genet, 2016, 12(9):e1006279

PubMed: 27588951 ( click the link to review the publication )

Sci Rep, 2016, 6:33710

PubMed: 27641368 ( click the link to review the publication )

J Biol Chem, 2016, 291(19):10332-46

PubMed: 26957545 ( click the link to review the publication )

Horm Cancer, 2016, 7(2):114-26

PubMed: 26858237 ( click the link to review the publication )

PeerJ, 2016, 4:e1683

PubMed: 26893968 ( click the link to review the publication )

Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7

PubMed: ( click the link to review the publication )

Oncotarget, 2016, 7(31):49597-49610

PubMed: 27391062 ( click the link to review the publication )

Oncotarget, 2016, 7(25):38191-38209

PubMed: 27224913 ( click the link to review the publication )

Immun Inflamm Dis, 2016, 4(4):463-473

PubMed: 27980780 ( click the link to review the publication )

PLoS Negl Trop Dis, 2015, 8(2):e2699

PubMed: 24551261 ( click the link to review the publication )

Biochimica et Biophysica Acta, 2015, 10.1016/j.bbamcr.2015.05.012

PubMed: 25982393 ( click the link to review the publication )

Am J Physiol Lung Cell Mol Physiol, 2015, 309(12):L1410-9

PubMed: 26498249 ( click the link to review the publication )

Int J Biol Sci, 2015, 11(8):923-34

PubMed: 26157347 ( click the link to review the publication )

Molecules, 2015, 20(1):1643-60

PubMed: 25608045 ( click the link to review the publication )

Biochemistry, 2015, 10.1021/acs.biochem.5b00148

PubMed: 25905789 ( click the link to review the publication )

PLoS One, 2015, 10(3):e0119832

PubMed: 25780909 ( click the link to review the publication )

Oncol Lett, 2015, 10(2):941-945

PubMed: 26622600 ( click the link to review the publication )

Oncotarget, 2015,

PubMed: 26416354 ( click the link to review the publication )

Oncotarget, 2015, 6(31):31792-804

PubMed: 26397139 ( click the link to review the publication )

Oncoscience, 2015, 2(4):419-427

PubMed: 26097875 ( click the link to review the publication )

Nat Commun, 2014, 5:3361

PubMed: 24553445 ( click the link to review the publication )

Proc Natl Acad Sci USA, 2014, 111(15):E1528-37

PubMed: 24706778 ( click the link to review the publication )
Int J Cancer, 2014, 135(10):2462-74

PubMed: 24706460 ( click the link to review the publication )

Mol Cancer Res, 2014, 12(7):1042-54

PubMed: 24784839 ( click the link to review the publication )

PLoS Negl Trop Dis, 2014, 8(2):e2699

PubMed: 24551261 ( click the link to review the publication )

Am J Respir Cell Mol Biol, 2014, 50(1):170-9

PubMed: 23972231 ( click the link to review the publication )

Cell Signal, 2014, 27(2):293-305

PubMed: 25446253 ( click the link to review the publication )

PLoS One, 2014, 9(10):e111146

PubMed: 25343454 ( click the link to review the publication )

PLoS One, 2014, 9(12):e114506

PubMed: 25503774 ( click the link to review the publication )

Tumour Biol, 2014, 35(8):8193-9

PubMed: 24850175 ( click the link to review the publication )

Mol Oncol, 2013, 7(6):1093-102

PubMed: 23993685 ( click the link to review the publication )

J Biol Chem, 2013, 288(23):16308-20

PubMed: 23599433 ( click the link to review the publication )

J Proteome Res, 2013, 12(8):3697-706

PubMed: 23763277 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2013, 273(2):401-9

PubMed: 24090817 ( click the link to review the publication )

PLoS One, 2013, 8(9):e74257

PubMed: 24066127 ( click the link to review the publication )

PLoS Pathog, 2012, 8(11):e1003048

PubMed: 23209418 ( click the link to review the publication )

Br J Haematol, 2012, 160(4):465-76

PubMed: 23252346 ( click the link to review the publication )

Mol Cell Biochem, 2012, 370(1-2):141-50

PubMed: 22865466 ( click the link to review the publication )

American Society of Clinical Oncology Annual Meeting, 2012, Chicago

PubMed: ( click the link to review the publication )

Mol Cancer, 2011, 10:125

PubMed: 21962244 ( click the link to review the publication )

Purity & Quality Control

Choose Selective HSP (HSP90) Inhibitors

Biological Activity

Description

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	Activity Description	PMID
NCI-SNU-16	MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4Pl[mlEPTB;NEiuN\|E1OiEQvF2=	M4rJRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
SNU-C1	MoH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{Dl[2lEPTB;MkSuPVExPSEQvF2=	Mn;tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H524	MlzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M33rVWlEPTB;MkSuN\|gyOiEQvF2=	Mkj0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H82	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MU\JR\|UxRTJ\|LkW1NlYh\|ryP	NHHsV5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK\|5USU6JRWK8M4E,
RT4	NFj5bnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MX7JR\|UxRTJ\|LkOyPFIh\|ryP	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
LB771-HNC	M2C4Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV:x[4U5UUN3ME2yNk41QDF\|IN88US=>	M4jyeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
SW780	MkXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mkn5TWM2OD1{MT6xN\|E5KM7:TR?=	NYKxbpdYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
NCI-H345	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1LZdmlEPTB;MkGuPFc4QSEQvF2=	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
NCI-H1563	NW\JT2t4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4e3bGlEPTB;MUmuO\|g5QCEQvF2=	NXTtPJk4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
DV-90	NFPMRpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXnJR\|UxRTF6Lkm5OFUh\|ryP	M4K5OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
Hs-578-T	NWrrSXBqT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4XHXmlEPTB;MUiuOVc2QSEQvF2=	Ml\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H2452	NIryXWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHG1eJNKSzVyPUG0Mlc{KM7:TR?=	NID0W2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK\|5USU6JRWK8M4E,
TGBC24TKB	NUjj[IxPT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{PFfmlEPTB;MUOuOVI6KM7:TR?=	NYPH[25QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
SW948	NFTkPHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFfvSFlKSzVyPUGwMlc2OTFizszN	NGrmNlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK\|5USU6JRWK8M4E,
CPC-N	NUfzb5pET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M13XTGlEPTB;MUGuNFA4KM7:TR?=	M3SyNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
SCC-3	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlrmTWM2OD1zMD61Olc6KM7:TR?=	MkXOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
SBC-1	MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXjJR\|UxRTlwOUO2OVYh\|ryP	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
NCI-H187	Ml\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFjENYtKSzVyPUmuOVE5OzVizszN	NFK3ZYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK\|5USU6JRWK8M4E,
NCI-H1838	MnvVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Ml\DTWM2OD16LkWxO\|MyKM7:TR?=	M3f4SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H322M	NGDkb5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{PnR2lEPTB;OT6xOlI5OSEQvF2=	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
TT	MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVf2THo{UUN3ME24MlM{ODB7IN88US=>	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
TCCSUP	NYnxbVhiT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml;FTWM2OD14Lk[wN\|Q6KM7:TR?=	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
LC-1F	MmO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1\lXmlEPTB;Nj6wPVI6OSEQvF2=	NW[1c3dxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
RPMI-8866	M1HjOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2D6NGlEPTB;NT64OFc6OiEQvF2=	MkXwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-H1623	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MY\JR\|UxRTVwOEO1OVYh\|ryP	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
MDA-MB-157	NFfycJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnewTWM2OD13Lk[2OFQ{KM7:TR?=	MnviQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
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NCI-H2227	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVfLe2pIUUN3ME2xMlA1QThzIN88US=>	M161[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
HAL-01	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NW\QNmJIUUN3ME2wMlk6Ozd7IN88US=>	M{jRZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
NCI-H1993	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{OzNWlEPTB;MT6wOFY2PyEQvF2=	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
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MDA-MB-453	M4i3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGHKXFFKSzVyPUCuPVA{ODRizszN	M3TrcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
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PANC-03-27	MlraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NEDUN3FKSzVyPUCuNFEyPjJizszN	M3:0cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
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CAL-85-1	NGH0e3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHrQcVZKSzVyPUCuNFEyQTJizszN	NWnzOmNZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
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BB65-RCC	NIHMXJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NEDaU21KSzVyPUCuNFEzODRizszN	NVPlZ2RWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
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Detroit562	NGfmbo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoX2TWM2OD1yLkCzPFczKM7:TR?=	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
MONO-MAC-6	M4PFemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlHVTWM2OD1yLkCzPFk{KM7:TR?=	Mn7sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
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BT-474	MmnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIjLdYZKSzVyPUCuNFcxPjFizszN	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
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NOMO-1	NW\vNZA4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4XpfGlEPTB;MD6wO\|E4OiEQvF2=	M3LITFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
KM-H2	M4\semdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYPJR\|UxRTBwMEeyOFEh\|ryP	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
EB2	MoG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1XzS2lEPTB;MD6wO\|I5PSEQvF2=	M1\FOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
LU-99A	MnrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUDJR\|UxRTBwMEeyPFch\|ryP	Ml7PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
WSU-NHL	NYmz[YdiT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHnoXWFKSzVyPUCuNFc{OjlizszN	M17KS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
Calu-1	MmnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHXvfXlKSzVyPUCuNFc{OzJizszN	NUjQR5RlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
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GI-ME-N	NHv6W5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2XWeWlEPTB;MD6wO\|QzPiEQvF2=	MkjvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
T98G	MonsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4Dk[GlEPTB;MD6wO\|QzOSEQvF2=	MnTBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
LS-513	MlTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3zsPGlEPTB;MD6wO\|Q2PiEQvF2=	NH\ZSWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK\|5USU6JRWK8M4E,
UACC-257	MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYrJR\|UxRTBwMEe1NFUh\|ryP	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
DK-MG	MoGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MX3JR\|UxRTBwMEe1NlYh\|ryP	NHy0WnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK\|5USU6JRWK8M4E,
CHP-126	MoG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NV[0V4s1UUN3ME2wMlA4PTZ3IN88US=>	M1\wZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
EW-11	M1;xN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVTZOmc2UUN3ME2wMlA4PTN3IN88US=>	Ml\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
Ramos-2G6-4C10	NYfHPXRYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYHBclNDUUN3ME2wMlA4PjR6IN88US=>	NUjxSHo5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
Saos-2	NVrueFJzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWnJR\|UxRTBwMEe1PVch\|ryP	M2rNN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
L-428	NHvxSFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmHUTWM2OD1yLkC3O\|A1KM7:TR?=	NXLWPHRDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
HOP-92	NVzMNGJHT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYjiWnBRUUN3ME2wMlA4PzFzIN88US=>	MkWxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
PANC-08-13	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYXZO\|h7UUN3ME2wMlA4PzF4IN88US=>	M4LONVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2OjF4ND:nQnNCVkeHUkyvZV4>
TUR	MoPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NEDmVo1KSzVyPUCuNFc4OzNizszN	NWjRWVJERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV{MU[0M{c,W0GQR1XSQE9iRg>?
DMS-153	M33SUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MorkTWM2OD1yLkC3O\|M2KM7:TR?=	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
NCI-N87	MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmPUTWM2OD1yLkC3O\|k6KM7:TR?=	NHfOR2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK\|5USU6JRWK8M4E,
ESS-1	M2nrVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MomzTWM2OD1yLkC3PFY5KM7:TR?=	MknsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlUzOTZ2Lze+V2FPT0WUPD;hQi=>
NCI-SNU-1	M{nQdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MV\JR\|UxRTBwMEe4PFgh\|ryP	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVIyPjRxJ{7TRW5ITVJ:L3G+
CP66-MEL	M3e4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV\LdnR6UUN3ME2wMlA4QDh5IN88US=>	NHK3SFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTJzNkSvK\|5USU6JRWK8M4E,
Calu-6	NXv5d\|AzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWTJR\|UxRTBwMEe5OlUh\|ryP	NGXTdlA9[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 Mol Oncol 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 Mol Oncol 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 Oncotarget 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 PeerJ 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 PeerJ 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

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

Kinase Assay:^[3]	- Collapse 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]	- Collapse 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]	- Collapse 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)

References

Solubility (25°C)

In vitro	DMSO	93 mg/mL warmed (199.76 mM)
	Water	Insoluble
	Ethanol	'31 mg/mL
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 1% DMSO+30% polyethylene glycol+1% Tween 80 For best results, use promptly after mixing.	30 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 Download Luminespib (NVP-AUY922) SDF

Molecular Weight	465.54
Formula	C₂₆H₃₁N₃O₅
CAS No.	747412-49-3
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	AUY-922, VER-52296
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)

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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.

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.

Bio Calculators

Molarity Calculator

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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The Serial Dilution Calculator Equation

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Computed Result

C1=C0/X	C1:	LOG(C1):
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Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

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

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.

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HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Inhibitors with Unique Features

Selective HSP90 Inhibitor

NVP-BEP800 : HSP90β-selective, IC50=58 nM.
Most Potent HSP90 Inhibitor

KW-2478 : HSP90, IC50=3.8 nM.
HSP90 Inhibitor in Clinical Trial

17-AAG (Tanespimycin) : Phase III for Gastrointestinal Stromal Tumors.
Newest HSP90 Inhibitor

XL888 : ATP-competitive inhibitor of HSP90 with IC50 of 24 nM.

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Tanespimycin (17-AAG)

Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.

Features:Displays very low toxicity toward normal cells.
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Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.
Alvespimycin (17-DMAG) HCl

Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.

Features:A synthetic derivative Geldanamycin, with lower hepatotoxicity than parent antibiotic & higher potency and bioavailability than the similar derivative 17-AAG.
Geldanamycin (NSC 122750)

Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with K_d of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.
HSP990 (NVP-HSP990)

HSP990 (NVP-HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. NVP-HSP990 induces cell cycle arrest and apoptosis.

Features:NVP-HSP990 is an orally available HSP90 inhibitor and is structurally distinct from other clinical HSP90 inhibitors.
Elesclomol (STA-4783)

Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
Onalespib (AT13387)

Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2.

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Luminespib (NVP-AUY922)