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

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

Cat. No.: HY-10215 Purity: 99.14%
Handling Instructions

NVP-AUY922 is a potent HSP90 inhibitor with IC50s of 7.8 nM/21 nM for HSP90α/β, respectively, and has weaker potency against the HSP90 family members GRP94 and TRAP-1 (IC50, 535 nM, 85 nM, respectively).

For research use only. We do not sell to patients.
NVP-AUY922 Chemical Structure

NVP-AUY922 Chemical Structure

CAS No. : 747412-49-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
5 mg USD 60 In-stock
10 mg USD 84 In-stock
25 mg USD 168 In-stock
100 mg USD 420 In-stock
200 mg USD 720 In-stock
500 mg USD 1320 In-stock
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Customer Review

    NVP-AUY922 purchased from MCE. Usage Cited in: Stem Cell Res. 2014 Sep;13(2):284-99.

    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).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    NVP-AUY922 is a potent HSP90 inhibitor with IC50s of 7.8 nM/21 nM for HSP90α/β, respectively, and has weaker potency against the HSP90 family members GRP94 and TRAP-1 (IC50, 535 nM, 85 nM, respectively).

    IC50 & Target

    IC50: 7.8 nM (HSP90α), 21 nM (HSP90β), 535 nM (GRP94), 85 nM (TRAP-1)[1]

    In Vitro

    NVP-AUY922 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. NVP-AUY922 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. NVP-AUY922 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]. NVP-AUY922 (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. NVP-AUY922 (500 nM) in combination with fludarabine more effectively induces apoptosis in cells in co-culture than either drug alone, and overcomes fibroblast-derived resistance to Hsp90 inhibitor[2]. NVP-AUY922 shows great inhibition of pancreatic cancer cells with IC50 of at 10 nM. NVP-AUY922 (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. NVP-AUY922 (10 nM) significantly blocks pancreatic cancer cell migration and invasion both in the absence and presence of EGF[3].

    In Vivo

    NVP-AUY922 (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]. NVP-AUY922 (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].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.2148 mL 1.0740 mL 2.1480 mL
    Please refer to the solubility information to select the appropriate solvent.
    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]

    NVP-AUY922 is dissolved in DMSO and diluted in sterile saline/Tween 20[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 NVP-AUY922 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
    Molecular Weight

    465.54

    Formula

    C₂₆H₃₁N₃O₅

    CAS No.

    747412-49-3

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 62 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    NVP-AUY922
    Cat. No.:
    HY-10215
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