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Apoptozole HSP inhibitor

Name: Apoptozole
Brand: Selleck Chemicals
SKU: S8365
Availability: InStock
Rating: 5 (7 reviews)

Cat.No.S8365

Apoptozole (Apoptosis Activator VII) is an inhibitor of heat shock protein 70(HSP70) and Hsc70 with dissociation constants Kd of 0.14 μM and 0.21 μM, respectively. It induces caspase-dependent apoptosis.

Chemical Structure

Molecular Weight: 625.56

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Quality Control

Batch: S836501 DMSO]100 mg/mL]false]Ethanol]25 mg/mL]false]Water]Insoluble]false Purity: 99.84%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.84

Related Targets	Akt Wnt/beta-catenin PKC ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK Kinesin
Other HSP Inhibitors	Tanespimycin (17-AAG) Luminespib (NVP-AUY922) Elesclomol (STA-4783) Ganetespib (STA-9090) Alvespimycin (17-DMAG) Hydrochloride VER155008 BIIB021 Onalespib (AT13387) NVP-BEP800 KRIBB11

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (159.85 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : 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.
Clear solution	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.	2.500mg/ml (4.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (1.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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

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	625.56	Formula	C₃₃H₂₅F₆N₃O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1054543-47-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Apoptosis Activator VII			Smiles	COC1=CC=C(C=C1)C2=C(N(C(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)CC4=CC=C(C=C4)C(=O)N)C5=CC=C(C=C5)OC

Mechanism of Action

Targets/IC₅₀/Ki	HSP70 (Cell-free assay) 0.14 μM(Kd) HSC70 (Cell-free assay) 0.21 μM(Kd)
In vitro	Apoptozole induces caspase dependent apoptosis by blocking interaction of HSP70 with APAF-1, without affecting interactions of HSP70 with ASK1, JNK, BAX, and AIF. However, apoptozole may form aggregates under aqueous conditions that could interact with HSP70 proteins in a non-specific manner, potentially leading to false positives and inconsistent data.
In vivo	Apoptozole greatly retards tumor growth in mice xenografted with cancer cells without affecting mouse viability. The elimination half-life time (T_1/2) of Az in blood is found to be significantly longer than that of Dox (8.04 versus 1.60 hr) and the time needed to reach a maximum concentration (Tmax) of Az is shorter than that of Dox (1.00 versus 4.00 hr).
References	[1] https://pubmed.ncbi.nlm.nih.gov/18729127/ [2] https://pubmed.ncbi.nlm.nih.gov/25772468/ [3] https://pubmed.ncbi.nlm.nih.gov/26458144/

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