Home Cytoskeletal Signaling HSP inhibitor VER-49009

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VER-49009 HSP inhibitor

Cat.No.S7458

VER-49009 (CCT0129397) is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
VER-49009 HSP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 387.82

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Quality Control

Batch: S745801 DMSO]77 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.48%
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99.48

Solubility

In vitro
Batch:

DMSO : 77 mg/mL (198.54 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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In vivo Formulation Calculator (Clear solution)

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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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 387.82 Formula

C19H18ClN3O4

 Storage (From the date of receipt)
CAS No. 940289-57-6 Download SDF Storage of Stock Solutions

Synonyms CCT0129397 Smiles CCNC(=O)C1=C(C(=NN1)C2=CC(=C(C=C2O)O)Cl)C3=CC=C(C=C3)OC

Mechanism of Action

Targets/IC50/Ki
HSP90β
47 nM
In vitro
VER-49009 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 167 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. This compound causes induction of HSP72 and HSP27 with depletion of client proteins, including C-RAF, B-RAF, and survivin, and PRMT5, which further result in cell cycle arrest and apoptosis. It inhibits the cell proliferation, and induces G2 phase arrest in hepatic stellate cell line CFSC cells, which may suggest a rational approach in the prevention of liver fibrosis.
Kinase Assay
Fluorescence Polarization Assay
Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe.
In vivo
In athymic mice, VER-49009 (20 mg/kg, i.v.) shows rapid clearance with values of 0.187 L/h. In an orthotopic human ovarian carcinoma model, this compound (4 mg/kg, i.p.) also induces the depletion of the sensitive HSP90 client protein ERBB2.
References

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