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VER 155008

Cat. No. M3116
VER 155008 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 85  USD85 In stock
5mg USD 68  USD68 In stock
10mg USD 90  USD90 In stock
50mg USD 300  USD300 In stock
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Quality Control & Documentation
Biological Activity

VER-155008 is a potent inhibitor of the HSP70 family, with IC50 of 0.5 μM and 2.6 μM for HSP70 and Grp78, respectively, exhibits >100-fold selectivity over HSP90.

Protocol (for reference only)
Cell Experiment
Cell lines BT474, MB-468, HCT116, and HT29 cells
Preparation method Growing all cell lines in DMEM/10% FCS with GlutaMAX-I in a humidified atmosphere of 5% CO2 in air.Using the sulforhodamine B (SRB) assay to dtermine cell proliferation .
Concentrations 50 μM
Incubation time 72 h
Animal Experiment
Animal models HCT116 tumor bearing
Formulation 10% DMSO/5% Tween 80/85% Saline (v/v/v)
Dosages 40 mg/kg
Administration i.v.
Chemical Information
Molecular Weight 556.4
Formula C25H23Cl2N7O4
CAS Number 1134156-31-2
Solubility (25°C) DMSO: 35 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kosuke Sakai, et al. Functional inhibition of heat shock protein 70 by VER-155008 suppresses pleural mesothelioma cell proliferation via an autophagy mechanism

[2] Lingjuan Huang, et al. Blockade of HSP70 by VER-155008 synergistically enhances bortezomib-induced cytotoxicity in multiple myeloma

[3] Phuc H Pham, et al. VER-155008 induced Hsp70 proteins expression in fish cell cultures while impeding replication of two RNA viruses

[4] Xichuan Tang, et al. Gold nanorods together with HSP inhibitor-VER-155008 micelles for colon cancer mild-temperature photothermal therapy

[5] Wei Wen, et al. VER-155008, a small molecule inhibitor of HSP70 with potent anti-cancer activity on lung cancer cell lines

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  Catalog
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Keywords: VER 155008 supplier, HSP, inhibitors, activators


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