1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP
  3. VER-49009

VER-49009 (Synonyms: CCT 129397)

Cat. No.: HY-15986 Purity: 99.26%
Handling Instructions

VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM.

For research use only. We do not sell to patients.

VER-49009 Chemical Structure

VER-49009 Chemical Structure

CAS No. : 558640-51-0

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Description

VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM.

IC50 & Target[1]

HSP90

25 nM (IC50)

In Vitro

VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM. VER-49009 binds to the ATPase of full length yeast Hsp90 protein, with an IC50 of 140 nM[1]. VER-49009 inhibits Hsp90, with a Kd of 78 nM. VER-49009 also shows antiproliferative activities against various human cancer cells, with a mean GI50 of 685 ± 119 nM. VER-49009 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI50 values of 444 ± 91.1 nM, and shows higher GI50s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. VER-49009 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression[2]. VER-49009 inhibits the proliferation (1, 2.5 μM), induces G2 phase arrest and reduces total Akt and phospho-Akt expression levels in CFSC cells (1-5 μM)[3].

In Vivo

VER-49009 (4 mg/kg, i.p.) results in clear depletion of ERBB2 at 3 and 8 h following the final dose, with client protein levels returning to normal by 24 h, in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors[2].

Molecular Weight

387.82

Formula

C₁₉H₁₈ClN₃O₄

CAS No.

558640-51-0

SMILES

O=C(C1=NNC(C2=CC(Cl)=C(O)C=C2O)=C1C3=CC=C(OC)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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (257.85 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5785 mL 12.8926 mL 25.7852 mL
5 mM 0.5157 mL 2.5785 mL 5.1570 mL
10 mM 0.2579 mL 1.2893 mL 2.5785 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (7.09 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (7.09 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[3]

Briefly, 5 × 103 cells/well are plated in 96-well culture plates. After an overnight incubation, the cells are treated with various concentrations of VER-49009 and VER-49009M (0, 1, 2.5, and 5 μM) for 24 h[3].

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

Animal Administration
[2]

In some studies, female NCr athymic mice are implanted i.p. with 10 million OVCAR3 ovarian carcinoma cells harvested from donor mice. This tumor mimics late-stage malignant disease. Once tumors are well established, mice are injected i.p. with 4 mg/kg VER-49009 or VER-50589 twice daily over 2 days (four doses total). Tumors are harvested at intervals after the last dose and snap frozen for pharmacodynamic analyses[1].

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

References
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Keywords:

VER-49009CCT 129397VER49009VER 49009CCT129397CCT-129397HSPHeat shock proteinsInhibitorinhibitorinhibit

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VER-49009
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