Name: VER-155008
Brand: Selleck Chemicals
SKU: S7751
Availability: InStock
Rating: 5 (53 reviews)

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	Akt Wnt/beta-catenin PKC ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK Kinesin
Other HSP Inhibitors	Tanespimycin (17-AAG) Elesclomol (STA-4783) Luminespib (NVP-AUY922) Ganetespib (STA-9090) Alvespimycin (17-DMAG) Hydrochloride Onalespib (AT13387) BIIB021 Zelavespib (PU-H71) HSP990 (NVP-HSP990) NVP-BEP800

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
BL21 DE3	Function assay	10 mins	Inhibition of GRP78 (26 to 636 residues) (unknown origin) expressed in Escherichia coli BL21 DE3 cells pre-incubated for 10 mins before FITC-NRLLLTG fluorescent peptide addition in presence of 10 uM ADP followed by further incubation for 2 hrs by fluoresc, IC50=0.8μM	31129054
HCT116	Cytotoxicity assay		Cytotoxicity against human HCT116 cells by SRB assay, GI50=5μM	19256508
HCT116	Antiproliferative assay		Antiproliferative activity against human HCT116 cells, GI50=5μM	21526763
BT474	Function assay		Binding affinity to Hsp70 nucleotide binding domain in human BT474 cells, IC50=10.4μM	20608738
HCT116	Function assay	24 hrs	Inhibition of HSP70 in human HCT116 cells assessed as reduction of He2 protein levels after 24 hrs by Western blot	19256508
HCT116	Function assay	24 hrs	Inhibition of HSP70 in human HCT116 cells assessed as reduction of Raf1 protein levels after 24 hrs by Western blot	19256508
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (179.72 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (8.99mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (4.49mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	556.4	Formula	C₂₅H₂₃Cl₂N₇O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1134156-31-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	HSP70 (Cell-free assay) 0.5 μM HSC70 (Cell-free assay) 2.6 μM GRP78 (Cell-free assay) 2.6 μM
In vitro	VER-155008 inhibits the proliferation of human breast and colon cancer cell lines BT474, MB-468, HCT116, and HT29 with GI50s in the range 5.3-14.4 μM, and induces Hsp90 client protein degradation in both HCT116 and BT474 cells. In the 8505C and FRO cells, this compound reduces the cell viability and elevates the percentage of dead cells in a time- and dose- dependent manner. It causes a dose-dependent inhibition of cytokine-dependent AML cell proliferation. This chemical shows an effective inhibition of cell proliferation in A549 and H1975 cells.
Kinase Assay	Hsc70, Hsp70 and Grp78 ﬂuorescence polarisation (FP) assay
Kinase Assay	The FP assay for Hsp70 is conducted in aqueous buffer consisting of 100 mM Tris pH 7.4, 150 mM KCl and 5 mM CaCl2, in a final assay volume of 100 µl, using 96 well black polystyrene high bind plates with a Fusion plate reader. N⁶-(6-amino)hexyl-ATP-5-FAM and the in-house protein preparation of GST-HSP70 3-382 have final concentrations in the assay of 20 nM and 400 nM, respectively. Compounds are tested as 10-point IC50s, with a final DMSO concentration of 5%. Assay mixtures are incubated for 3 h prior to reading on the Fusion (ex 485 nm; em 535 nm). The data is fitted using a 4 parameter logistical data model by XLFit 4. The FP assay for Hsc70 and Grp78 is carried out as described for Hsp70 using the same N6 -(6-amino)hexyl-ATP-5-FAM as the FP probe with the following modiﬁcations. For Hsc70, the protein and probe concentrations are 0.3 μM and 20 nM, respectively with a 30 min incubation at 22℃ while for Grp78, the protein and probe concentrations are 2 μM and 10 nM, respectively with a 2 h incubation at 22℃. The K^D for the FAM-ATP probe was 0.24 μM for Hsc70 and 2 μM for Grp78.
In vivo	In HCT116 tumor bearing mice, VER-155008 (25 or 40 mg/kg, i.v.) demonstrates rapid metabolism and clearance, along with tumor levels below the predicted pharmacologically active level.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20012863/ [2] https://pubmed.ncbi.nlm.nih.gov/25450359/ [3] https://pubmed.ncbi.nlm.nih.gov/23586877/ [4] https://pubmed.ncbi.nlm.nih.gov/24676905/ [5] https://pubmed.ncbi.nlm.nih.gov/19256508/