1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Autophagy Apoptosis
  2. HSP Autophagy Apoptosis
  3. Luminespib

Luminespib  (Synonyms: VER-52296; AUY922; NVP-AUY922)

Cat. No.: HY-10215 Purity: 99.74%
COA Handling Instructions

Luminespib (VER-52296) est un inhibiteur puissant de HSP90 avec des IC50s de 7,8 et 21 nM pour HSP90α et HSP90β, respectivement.

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.

Luminespib Chemical Structure

Luminespib Chemical Structure

CAS No. : 747412-49-3

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 92 In-stock
25 mg USD 185 In-stock
100 mg USD 462 In-stock
200 mg USD 792 In-stock
500 mg USD 1452 In-stock
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 19 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

    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).

    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).

    View All HSP Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively[1].

    IC50 & Target

    HSP90α

    7.8 nM (IC50)

    HSP90β

    21 nM (IC50)

    GRP94

    535 nM (IC50)

    TRAP-1

    85 nM (IC50)

    In Vitro

    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.

    In Vivo

    Luminespib (50, 75 mg/kg, i.p.) significantly inhibits tumor growth rate, reducing the mean weights of tumors on day 11 in human tumor xenografts[2]. Luminespib (50 mg/kg/week, 3×25 mg/kg/week) significantly reduces tumor growth rates and lowers tumor weights in the L3.6pl pancreatic cancer cell-bearing mice model[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    465.54

    Formula

    C26H31N3O5

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to gray

    SMILES

    O=C(C1=NOC(C2=CC(C(C)C)=C(O)C=C2O)=C1C3=CC=C(CN4CCOCC4)C=C3)NCC

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1480 mL 10.7402 mL 21.4804 mL
    5 mM 0.4296 mL 2.1480 mL 4.2961 mL
    View the 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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.81%

    References
    Cell Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. 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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email Address *

    Phone Number *

     

    Organization Name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Luminespib
    Cat. No.:
    HY-10215
    Quantity:
    MCE Japan Authorized Agent: