Luminespib
Based on 26 publication(s) in Google Scholar
Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
For research use only. We do not sell to patients.
- Purity: 99.40%
- CAS No.: 747412-49-3
- Formula: C26H31N3O5
- Molecular Weight:465.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Luminespib
More- Blood. 2018 Jul 19;132(3):307-320. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2017 Sep 4;8(1):422. [Abstract]
- Leukemia. 2019 Jun;33(6):1373-1386. [Abstract]
- J Biomed Sci. 2021 Jul 23;28(1):55. [Abstract]
- Pharmacol Res. 2020 Jan;151:104512. [Abstract]
- Clin Cancer Res. 2018 Feb 15;24(4):794-806. [Abstract]
- Cancer Lett. 2024 Nov 25:217354. [Abstract]
- NPJ Precis Oncol. 2025 Apr 25;9(1):122. [Abstract]
- Cell Rep. 2025 Jun 30;44(7):115936. [Abstract]
- Cancer Cell Int. 2021 Jun 5;21(1):291. [Abstract]
- Eur J Med Chem. 2024 Aug 28:278:116801. [Abstract]
- Biochem Pharmacol. 2026 May:247:117785. [Abstract]
- J Chem Theory Comput. 2018 Jul 10;14(7):3859-3869. [Abstract]
- Int J Mol Sci. 2021 Jun 11;22(12):6309. [Abstract]
- Nanomedicine. 2026 May 13:102957. [Abstract]
- Cancers (Basel). 2021 Feb 23;13(4):927. [Abstract]
- J Biol Chem. 2024 Feb;300(2):105633. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Viruses. 2021 Apr 2;13(4):610. [Abstract]
- Am J Cancer Res. 2024 May 15;14(5):2072-2087. [Abstract]
- SLAS Discov. 2020 Feb;25(2):195-206. [Abstract]
- Stem Cell Res. 2014 Sep;13(2):284-99. [Abstract]
- SSRN. 2025 Feb 7.
- bioRxiv. 2024 Jul 25.
- Cold Spring Harb Mol Case Stud. 2020 Jun 12;6(3):a004853. [Abstract]
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WB
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WB
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Cell Proliferation/Viability Assay
Biological Activity
|
HSP90α 7.8 nM (IC50) |
HSP90β 21 nM (IC50) |
GRP94 535 nM (IC50) |
TRAP-1 85 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.001 μM
Compound: NVP-AUY922
|
Antiproliferative activity against human A2780 cells after 72 hrs
Antiproliferative activity against human A2780 cells after 72 hrs
|
[PMID: 24980703] |
| A2780 | IC50 |
0.006 μM
Compound: NVP
|
Cytotoxicity against human A2780 cells assessed as cell growth inhibition
Cytotoxicity against human A2780 cells assessed as cell growth inhibition
|
[PMID: 32305165] |
| A549 | GI50 |
0.01 μM
Compound: 1; AUY-922
|
Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay
|
[PMID: 32683166] |
| A549 | GI50 |
0.026 μM
Compound: NVP-AUY922
|
Growth inhibition of human A549 cells after 72 hrs by SRB assay
Growth inhibition of human A549 cells after 72 hrs by SRB assay
|
[PMID: 25313505] |
| A549 | IC50 |
0.0082 μM
Compound: NVP-AUY922
|
Antiproliferative activity against human A549 cells assessed as cell growth inhibition
Antiproliferative activity against human A549 cells assessed as cell growth inhibition
|
[PMID: 26112442] |
| A549 | IC50 |
39 nM
Compound: NVP-AUY922
|
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay
|
[PMID: 32352777] |
| A549 | IC50 |
60 nM
Compound: AUY922
|
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
|
[PMID: 29698859] |
| BT-474 | IC50 |
0.01 μM
Compound: NVP-AUY922
|
Induction of Her2 degradation in human BT474 cells assessed as inhibition of signal by immunocytochemistry
Induction of Her2 degradation in human BT474 cells assessed as inhibition of signal by immunocytochemistry
|
[PMID: 24980703] |
| BT-474 | IC50 |
0.031 μM
Compound: 3, NVP-AUY922
|
Binding affinity to Hsp90 nucleotide binding domain in human BT474 cells
Binding affinity to Hsp90 nucleotide binding domain in human BT474 cells
|
[PMID: 20608738] |
| BT-474 | IC50 |
14 nM
Compound: AUY922
|
Antiproliferative activity against human BT474 cells after 72 hrs by SRB assay
Antiproliferative activity against human BT474 cells after 72 hrs by SRB assay
|
[PMID: 29698859] |
| CAPAN-1 | IC50 |
657 nM
Compound: NVP-AUY922
|
Antiproliferative activity against human Capan1 cells assessed as reduction in cell viability after 72 hrs by SRB assay
Antiproliferative activity against human Capan1 cells assessed as reduction in cell viability after 72 hrs by SRB assay
|
[PMID: 32352777] |
| DU-145 | GI50 |
0.005 μM
Compound: 40f, VER-52296, NVP-AUY922
|
Growth inhibition of human DU145 cells by SRB assay
Growth inhibition of human DU145 cells by SRB assay
|
[PMID: 18020435] |
| DU-145 | IC50 |
0.0047 μM
Compound: NVP-AUY922
|
Antiproliferative activity against human DU145 cells assessed as cell growth inhibition
Antiproliferative activity against human DU145 cells assessed as cell growth inhibition
|
[PMID: 26112442] |
| DU-145 | IC50 |
21 nM
Compound: AUY922
|
Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay
Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay
|
[PMID: 29698859] |
| EBC-1 | IC50 |
13 nM
Compound: AUY922
|
Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
|
[PMID: 29698859] |
| Fibroblast | CC50 |
0.008 μM
Compound: 2, AUY-922
|
Cytotoxicity against Huntington's disease patient derived fibroblasts after 48 hrs by CellTiter Glo assay
Cytotoxicity against Huntington's disease patient derived fibroblasts after 48 hrs by CellTiter Glo assay
|
[PMID: 24673104] |
| HCC827 | IC50 |
7 nM
Compound: 7; NVP-AUY922
|
Cytotoxicity against gefitinib-resistant human HCC827 cells assessed as inhibition of cell proliferation by MTS assay
Cytotoxicity against gefitinib-resistant human HCC827 cells assessed as inhibition of cell proliferation by MTS assay
|
[PMID: 26844689] |
| HCT-116 | GI50 |
0.016 μM
Compound: 40f, VER-52296, NVP-AUY922
|
Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
|
[PMID: 18020435] |
| HCT-116 | GI50 |
16 nM
Compound: 45, VER-52296/NVP-AUY922
|
Antiproliferative against human HCT116 cells
Antiproliferative against human HCT116 cells
|
[PMID: 19017562] |
| HCT-116 | GI50 |
16 nM
Compound: 7; NVP-AUY922
|
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 24 hrs by SRB assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 24 hrs by SRB assay
|
[PMID: 38215028] |
| HCT-116 | IC50 |
0.02 μM
Compound: NVP
|
Cytotoxicity against human HCT116 cells assessed as cell growth inhibition
Cytotoxicity against human HCT116 cells assessed as cell growth inhibition
|
[PMID: 32305165] |
| HCT-116 | IC50 |
121 nM
Compound: NVP-AUY922
|
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay
|
[PMID: 32352777] |
| HCT-116 | IC50 |
16 nM
Compound: AUY922
|
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
|
[PMID: 29698859] |
| HeLa | IC50 |
0.0077 μM
Compound: NVP-AUY922
|
Antiproliferative activity against human HeLa cells assessed as cell growth inhibition
Antiproliferative activity against human HeLa cells assessed as cell growth inhibition
|
[PMID: 26112442] |
| J82 | IC50 |
5.2 μM
Compound: AUY922
|
Antiproliferative activity against human J82 cells assessed as inhibition of cell proliferation by CCK8 assay
Antiproliferative activity against human J82 cells assessed as inhibition of cell proliferation by CCK8 assay
|
[PMID: 35987020] |
| K562 | IC50 |
0.0087 μM
Compound: NVP-AUY922
|
Antiproliferative activity against human K562 cells assessed as cell growth inhibition
Antiproliferative activity against human K562 cells assessed as cell growth inhibition
|
[PMID: 26112442] |
| L02 | IC50 |
1364 nM
Compound: NVP-AUY922
|
Cytotoxicity agains human HL7702 cells assessed as reduction in cell viability after 72 hrs by SRB assay
Cytotoxicity agains human HL7702 cells assessed as reduction in cell viability after 72 hrs by SRB assay
|
[PMID: 32352777] |
| MCF7 | EC50 |
7 nM
Compound: 5, NVP-AUY922
|
Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2
Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2
|
[PMID: 22938030] |
| MCF7 | IC50 |
0.0064 μM
Compound: NVP-AUY922
|
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition
|
[PMID: 26112442] |
| MCF7 | IC50 |
7 nM
Compound: 7, NVP-AUY922
|
Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells
Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells
|
[PMID: 20055425] |
| MDA-MB-231 | IC50 |
21 nM
Compound: AUY922
|
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
|
[PMID: 29698859] |
| MIA PaCa-2 | IC50 |
38 nM
Compound: NVP-AUY922
|
Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability after 72 hrs by SRB assay
Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability after 72 hrs by SRB assay
|
[PMID: 32352777] |
| NCI-H1975 | GI50 |
0.02 μM
Compound: 1; AUY-922
|
Antiproliferative activity against human NCI-H1975 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H1975 cells measured after 48 hrs by SRB assay
|
[PMID: 32683166] |
| NCI-H3122 | IC50 |
0.014 μM
Compound: 3; AUY922
|
Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay
Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay
|
[PMID: 27688186] |
| NCI-H3122 | IC50 |
12.4 nM
Compound: AUY922
|
Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay
Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay
|
[PMID: 29698859] |
| NCI-H460 | GI50 |
0.03 μM
Compound: 1; AUY-922
|
Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay
|
[PMID: 32683166] |
| NCI-H460 | IC50 |
0.0024 μM
Compound: 10, VER-52296/NVP-AUY922
|
Cytotoxicity against human NCI-H460 after 72 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H460 after 72 hrs by sulforhodamine B assay
|
[PMID: 22066525] |
| NCI-H460 | IC50 |
0.0024 μM
Compound: 5, NVP-AUY922
|
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay
|
[PMID: 24565573] |
| NCI-H460 | IC50 |
2.4 nM
Compound: NVP-AUY922
|
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 72 hrs by SRB assay
|
[PMID: 24588105] |
| NCI-H460 | IC50 |
23 nM
Compound: AUY922
|
Antiproliferative activity against human NCI-H460 cells after 72 hrs by SRB assay
Antiproliferative activity against human NCI-H460 cells after 72 hrs by SRB assay
|
[PMID: 29698859] |
| NCI-N87 | IC50 |
83 nM
Compound: AUY922
|
Antiproliferative activity against human NCI-N87 cells after 72 hrs by SRB assay
Antiproliferative activity against human NCI-N87 cells after 72 hrs by SRB assay
|
[PMID: 29698859] |
| PC-3M | GI50 |
0.006 μM
Compound: 40f, VER-52296, NVP-AUY922
|
Growth inhibition of human PC3M cells by SRB assay
Growth inhibition of human PC3M cells by SRB assay
|
[PMID: 18020435] |
| SF-268 | GI50 |
0.006 μM
Compound: 40f, VER-52296, NVP-AUY922
|
Growth inhibition of human SF268 cells by SRB assay
Growth inhibition of human SF268 cells by SRB assay
|
[PMID: 18020435] |
| Sf9 | IC50 |
8 nM
Compound: NVP-AUY922
|
Displacement of GM-BODIPY from human full length HSP90 alpha expressed in baculovirus-infected Sf9 cells after 16 hrs by fluorescence polarization assay
Displacement of GM-BODIPY from human full length HSP90 alpha expressed in baculovirus-infected Sf9 cells after 16 hrs by fluorescence polarization assay
|
[PMID: 24751441] |
| SK-MEL-28 | GI50 |
0.005 μM
Compound: 40f, VER-52296, NVP-AUY922
|
Growth inhibition of human SKMel28 cells by SRB assay
Growth inhibition of human SKMel28 cells by SRB assay
|
[PMID: 18020435] |
| SW780 | IC50 |
3.95 μM
Compound: AUY922
|
Antiproliferative activity against human SW780 cells assessed as inhibition of cell proliferation by CCK8 assay
Antiproliferative activity against human SW780 cells assessed as inhibition of cell proliferation by CCK8 assay
|
[PMID: 35987020] |
| T-24 | IC50 |
4.93 μM
Compound: AUY922
|
Antiproliferative activity against human T24 cells assessed as inhibition of cell proliferation by CCK8 assay
Antiproliferative activity against human T24 cells assessed as inhibition of cell proliferation by CCK8 assay
|
[PMID: 35987020] |
| U-87MG ATCC | GI50 |
0.008 μM
Compound: 40f, VER-52296, NVP-AUY922
|
Growth inhibition of human U87MG cells by SRB assay
Growth inhibition of human U87MG cells by SRB assay
|
[PMID: 18020435] |
| U-87MG ATCC | IC50 |
31 nM
Compound: AUY922
|
Antiproliferative activity against human U87MG cells after 72 hrs by SRB assay
Antiproliferative activity against human U87MG cells after 72 hrs by SRB assay
|
[PMID: 29698859] |
Luminespib is a potent and selective HSP90 inhibitor, with IC50s and Kis of 21 ± 16, 8.2 ± 0.7 nM against HSP90β and of 7.8 ± 1.8, 9.0 ± 5.0 nM for HSP90α. Luminespib shows weak activity against GRP94 and TRAP-1 wich IC50s of 535 ± 51 nM (Ki, 108 nM) and 85 ± 8 nM (Ki, 53 nM), respectively. Luminespib exhibits inhibitory effect on proliferation of various human tumor cell lines (2.3-49.6 nM), induces cell cycle arrest and apoptosis and depletes client proteins in human cancer cells (80 nM)[1]. Luminespib (100 nM) significantly reduces CD40L fibroblast-induced changes in immunophenotype and STAT3 signaling but with no effect on the viability of chronic lymphocytic leukemia (CLL) cells. Luminespib (500 nM) in combination with NSC 118218 more effectively induces apoptosis in cells in co-culture than either drug alone, and overcomes fibroblast-derived resistance to Hsp90 inhibitor[2]. Luminespib shows great inhibition of pancreatic cancer cells with IC50 of at 10 nM. Luminespib (10 nM) reduces the expression and the epidermal growth factor (EGF)-mediated activation of EGFR and substantially disrupts EGF signaling in terms of diminishing downstream phosphorylation of ERKThr202/Tyr204. Luminespib (10 nM) significantly blocks pancreatic cancer cell migration and invasion both in the absence and presence of EGF[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 747412-49-3
-
Appearance Solid
-
Molecular Weight 465.54
-
Formula C26H31N3O5
-
Color Off-white to light yellow
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SMILES
O=C(C1=NOC(C2=CC(C(C)C)=C(O)C=C2O)=C1C3=CC=C(CN4CCOCC4)C=C3)NCC
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Synonyms
VER-52296; AUY922; NVP-AUY922
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (26)
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Journal Impact Factor
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Most Recent
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Blood
Targeting HSP90 dimerization via the C terminus is effective in imatinib-resistant CML and lacks the heat shock response. [Abstract]2018 Jul 19;132(3):307-320. PMID: 29724897
Luminespib purchased from MedChemExpress. Usage Cited in: Blood. 2018 Jul 19;132(3):307-320. [Abstract]
K562, KCL22 and HL60 are treated with the indicated (cytotoxic) concentration of Amidopyrine (AX) and AUY922 for 48h and later protein lysates are subjected to immunoblot analysis.
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
2017 Sep 4;8(1):422. PMID: 28871086 -
Leukemia
Targeting nuclear β-catenin as therapy for post-myeloproliferative neoplasm secondary AML. [Abstract]2019 Jun;33(6):1373-1386. PMID: 30575820 -
J Biomed Sci
2021 Jul 23;28(1):55. PMID: 34301262 -
Pharmacol Res
Destabilization of ROR1 enhances activity of Ibrutinib against chronic lymphocytic leukemia in vivo. [Abstract]2020 Jan;151:104512. PMID: 31726100 -
Clin Cancer Res
Colorectal Cancer Consensus Molecular Subtypes Translated to Preclinical Models Uncover Potentially Targetable Cancer Cell Dependencies. [Abstract]2018 Feb 15;24(4):794-806. PMID: 29242316
Luminespib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2018 Feb 15;24(4):794-806. [Abstract]
HSP90 inhibition with Luminespib or Ganetespib treatment at 50 and 100 nM for 24 hours in three CMS4 cell lines with response to HSP90 inhibition (CACO2, LIM2099 and SW480) confirmed up-regulation of HSP70 and HSP40 at the protein level in treated versus untreated control cells (western blotting).
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Cancer Lett
HSP90 inhibitor AUY922 suppresses tumor growth and modulates immune response through YAP1-TEAD pathway inhibition in gastric cancer. [Abstract]2024 Nov 25:217354. PMID: 39603381 -
NPJ Precis Oncol
Functional screening identifies kinesin spindle protein inhibitor filanesib as a potential treatment option for hepatoblastoma. [Abstract]2025 Apr 25;9(1):122. PMID: 40281281 -
Cell Rep
Gut microbiota-bile acid crosstalk contributes to calcium oxalate nephropathy through Hsp90α-mediated ferroptosis. [Abstract]2025 Jun 30;44(7):115936. PMID: 40591459 -
Cancer Cell Int
Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]2021 Jun 5;21(1):291. PMID: 34090418 -
Eur J Med Chem
HSP90/LSD1 dual inhibitors against prostate cancer as well as patient-derived colorectal organoids. [Abstract]2024 Aug 28:278:116801. PMID: 39241481 -
Biochem Pharmacol
2026 May:247:117785. PMID: 41679664 -
J Chem Theory Comput
Estimation of Drug-Target Residence Times by τ-Random Acceleration Molecular Dynamics Simulations. [Abstract]2018 Jul 10;14(7):3859-3869. PMID: 29768913 -
Int J Mol Sci
Effects of a Unique Combination of the Whole-Body Low Dose Radiotherapy with Inactivation of Two Immune Checkpoints and/or a Heat Shock Protein on the Transplantable Lung Cancer in Mice. [Abstract]2021 Jun 11;22(12):6309. PMID: 34208396 -
Nanomedicine
Nanotechnology-based reformulation of AUY922 mitigates retinal toxicity and retains potent anti-tumor activity. [Abstract]2026 May 13:102957. PMID: 42134612 -
Cancers (Basel)
2021 Feb 23;13(4):927. PMID: 33672199 -
J Biol Chem
Functional Maturation of Cytochromes P4503A4 and 2D6 Relies on GAPDH- and Hsp90-Dependent Heme Allocation. [Abstract]2024 Feb;300(2):105633. PMID: 38199567 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Viruses
Deep Transfer Learning Approach for Automatic Recognition of Drug Toxicity and Inhibition of SARS-CoV-2. [Abstract]2021 Apr 2;13(4):610. PMID: 33918368 -
Am J Cancer Res
The small-molecule drug homoharringtonine targets HSF1 to suppress pancreatic cancer progression. [Abstract]2024 May 15;14(5):2072-2087. PMID: 38859866 -
SLAS Discov
Medium-Throughput Detection of Hsp90/Cdc37 Protein-Protein Interaction Inhibitors Using a Split Renilla Luciferase-Based Assay. [Abstract]2020 Feb;25(2):195-206. PMID: 31662027 -
Stem Cell Res
2014 Sep;13(2):284-99. PMID: 25171775
Luminespib purchased from MedChemExpress. Usage Cited in: Stem Cell Res. 2014 Sep;13(2):284-99. [Abstract]
HSP90 inhibition affects ciliation. 24 h treatment with 100 nM AUY922 significantly affects ciliation, under 20% (left) O2 tension but not 5% O2 tension (right).
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Cold Spring Harb Mol Case Stud
2020 Jun 12;6(3):a004853. PMID: 32532875
Solvent & Solubility
DMSO : ≥ 62 mg/mL (133.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cell lines are grown in DMEM/10% FCS, 2 mM glutamine, and nonessential amino acids in a humidified atmosphere of 5% CO2 in air. All lines are free of Mycoplasma. Cell proliferation is determined using the SRB assay for tumor cells and prostate epithelial cells, the WST-1 assay for MCF10A and HB119, or an alkaline phosphatase assay for HUVEC and HDMEC. GI50 is the compound concentration inhibiting cell proliferation by 50% compared with vehicle controls. Active caspase-3/7 is measured using a homogenous caspase assay kit[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
For efficacy studies, human tumor xenografts are established s.c. in athymic mice. WM266.4 cells are also injected i.v. to generate experimental lung metastases and PC3LN3 prostate carcinoma cells are implanted into the prostates of male mice. Dosing by i.p. with Luminespib commences when tumors are well established. Tumor growth is monitored and at study end samples are harvested for analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Eccles, Suzanne A., et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Research (2008), 68(8), 2850-2860. [Content Brief]
[2]. Best OG, et al. Heat shock protein-90 inhibitor, NVP-AUY922, is effective in combination with NSC 118218 against chronic lymphocytic leukemia cells cultured on CD40L-stromal layer and inhibits their activated/proliferative phenotype. Leuk Lymphoma. 2012 Jul 9. [Content Brief]
[3]. Moser C, et al. Stoeltzing O.Targeting HSP90 by the novel inhibitor NVP-AUY922 reduces growth and angiogenesis of pancreatic cancer. Anticancer Res. 2012 Jul;32(7):2551-61. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1480 mL | 10.7402 mL | 21.4804 mL | 53.7011 mL |
| 5 mM | 0.4296 mL | 2.1480 mL | 4.2961 mL | 10.7402 mL | |
| 10 mM | 0.2148 mL | 1.0740 mL | 2.1480 mL | 5.3701 mL | |
| 15 mM | 0.1432 mL | 0.7160 mL | 1.4320 mL | 3.5801 mL | |
| 20 mM | 0.1074 mL | 0.5370 mL | 1.0740 mL | 2.6851 mL | |
| 25 mM | 0.0859 mL | 0.4296 mL | 0.8592 mL | 2.1480 mL | |
| 30 mM | 0.0716 mL | 0.3580 mL | 0.7160 mL | 1.7900 mL | |
| 40 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3425 mL | |
| 50 mM | 0.0430 mL | 0.2148 mL | 0.4296 mL | 1.0740 mL | |
| 60 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8950 mL | |
| 80 mM | 0.0269 mL | 0.1343 mL | 0.2685 mL | 0.6713 mL | |
| 100 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5370 mL |