AZD5582 |
| Catalog No.GC19050 |
AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1258392-53-8
Sample solution is provided at 25 µL, 10mM.
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AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively). IC50 value: 15/21/15 nM (cIAP1/cIAP2/XIAP) [1]Target: IAPs inhibitorAZD5582 causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro. When administered intravenously to MDA-MB-231 xenograft-bearing mice, AZD5582 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Antiproliferative effects are observed with AZD5582 in only a small subset of the over 200 cancer cell lines examined, consistent with other published IAP inhibitors [1]. AZD5582 significantly enhanced apoptosis induced by the death receptor (DR) agonist tumour necrosis factor-related apoptosis-inducing ligand (TRAIL). Importantly, killing by TRAIL plus AZD5582 was independent of adverse prognostic features including TP53 deletion which is strongly associated with chemoresistance in CLL [2].
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.
[2]. Zhuang J, et al. Selective IAP inhibition results in sensitization of unstimulated but not CD40-stimulated chronic lymphocytic leukaemia cells to TRAIL-induced apoptosis. Pharmacol Res Perspect. 2014 Dec;2(6):e00081.
| Cas No. | 1258392-53-8 | SDF | |
| Canonical 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 | ||
| Formula | C58H78N8O8 | M.Wt | 1015.29 |
| Solubility | DMSO : ≥ 66.25 mg/mL (65.25 mM) | Storage | 4°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.9849 mL | 4.9247 mL | 9.8494 mL |
| 5 mM | 0.197 mL | 0.9849 mL | 1.9699 mL |
| 10 mM | 0.0985 mL | 0.4925 mL | 0.9849 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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