AZD5582 dihydrochloride

Name: AZD5582 dihydrochloride
Brand: MedChemExpress
SKU: HY-110346
Rating: 5.0 (11 reviews)

Cat. No.: HY-110346 Purity: 98.67%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC₅₀s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.

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

AZD5582 dihydrochloride Chemical Structure

CAS No. : 1883545-51-4

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 310	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1050	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1680	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of AZD5582 dihydrochloride:

AZD5582 In-stock

10 Publications Citing Use of MCE AZD5582 dihydrochloride

: AZD5582 dihydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2023 Feb 8;CIR-22-0494. [Abstract]; AZD5582 (0.1-1 μM; 24 h) decreases the expression of cIAP1, cIAP2 and XIAP in GM-CSF DCs.

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•Related Screening Libraries:

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View All IAP Isoform Specific Products:

View All Isoforms

cIAP cIAP-1 cIAP-2 XIAP

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

cIAP1

15 nM (IC₅₀)

cIAP2

21 nM (IC₅₀)

XIAP

15 nM (IC₅₀)

In Vitro

AZD5582 (20 nM; 48 hours) inhibits cell viability by cooperation with IFNγ or viral double-stranded RNA (dsRNA) in H1975 NSCLC cells^[2].
AZD5582 (20 nM; 17 or 25 hours) downregulates cIAP-1, activates RIPK1 (upstream regulator of caspase-8), and triggers the activation of extrinsic (caspase-8) and intrinsic (caspase-9) apoptosis pathways, causing the cleavage of caspase-3 and caspase-7^[2].
AZD5582 (20 nM; 48 hours) involves in apoptosis due to induction of cell death and active caspase-3/8 activities by AZD5582 and IFNγ co-treatment in HCC827 NSCLC cells^[2].

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

Cell Viability Assay^[2]

Cell Line:	H1975 NSCLC cell line
Concentration:	20 nM
Incubation Time:	48 hours
Result:	Cooperated with IFNγ or viral double-stranded RNA (dsRNA) to inhibit cell viability even cell death.

Apoptosis Analysis^[2]

Cell Line:	HCC827 NSCLC cell line
Concentration:	20 nM
Incubation Time:	48 hours
Result:	Had an inhibitory effect on cell viability by cooperating with IFNγ.

Western Blot Analysis^[2]

Cell Line:	H1975 NSCLC cell line
Concentration:	20 nM
Incubation Time:	17 or 25 hours
Result:	Down-regulated cIAP-1, activated RIPK1 (upstream regulator of caspase-8), triggered the cleavage (activation) of caspase-3,7,8 and 9.

In Vivo

AZD5582 (intravenous injection; 0.1-3.0 mg/kg; once a week; 2 weeks) causes degradation of cIAP1 and caspase 3 cleavage in tumor cells, and after a two-week treatment, the tumors largely resolved; when the mice are given a medium dose (0.5 mg/kg) of AZD5582, cIAP1 degrades after administration, but it takes a while time to reach apoptosis-inducing effect^[1].

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

Animal Model:	MDA-MB-231 xenograft-bearing mice^[1]
Dosage:	0.1 mg/kg, 0.5 mg/kg, 3.0 mg/kg
Administration:	Intravenous injection; once a week; 2 weeks
Result:	Resulted in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg

Molecular Weight

1088.21

Formula

C₅₈H₈₀Cl₂N₈O₈

CAS No.

1883545-51-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

CN[C@@H](C)C(N[C@H](C(N1[C@H](C(N[C@H]2C3=CC=CC=C3C[C@H]2OCC#CC#CCO[C@H]4[C@@H](NC([C@@H]5CCCN5C([C@@H](NC([C@H](C)NC)=O)C6CCCCC6)=O)=O)C(C=CC=C7)=C7C4)=O)CCC1)=O)C8CCCCC8)=O.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (45.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.9189 mL	4.5947 mL	9.1894 mL
5 mM	0.1838 mL	0.9189 mL	1.8379 mL
10 mM	0.0919 mL	0.4595 mL	0.9189 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.67%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (249 KB) HNMR (269 KB) RP-HPLC (340 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Hennessy EJ, et al. Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582). J Med Chem. 2013 Dec 27;56(24):9897-919. [Content Brief]

[2]. Qin Hao, et al. IF-γ and Smac mimetics synergize to induce apoptosis of lung cancer cells in a TNFα-independent manner,Cancer Cell Int. 2018; 18: 84. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	0.9189 mL	4.5947 mL	9.1894 mL	22.9735 mL
	5 mM	0.1838 mL	0.9189 mL	1.8379 mL	4.5947 mL
	10 mM	0.0919 mL	0.4595 mL	0.9189 mL	2.2974 mL
	15 mM	0.0613 mL	0.3063 mL	0.6126 mL	1.5316 mL
	20 mM	0.0459 mL	0.2297 mL	0.4595 mL	1.1487 mL
	25 mM	0.0368 mL	0.1838 mL	0.3676 mL	0.9189 mL
	30 mM	0.0306 mL	0.1532 mL	0.3063 mL	0.7658 mL
	40 mM	0.0230 mL	0.1149 mL	0.2297 mL	0.5743 mL