1883545-51-4
1883545-51-4 structure
- Name: AZD 5582 dihydrochloride
- Chemical Name: AZD5582 dihydrochloride
- CAS Number: 1883545-51-4
- Molecular Formula: C58H80Cl2N8O8
- Molecular Weight: 1088.21
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2020-08-07 19:32:33
- Modify Date: 2024-01-12 12:44:01
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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[1].
| Name | AZD5582 dihydrochloride |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| Target |
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]. 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]. 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 |
| References |
| Molecular Formula | C58H80Cl2N8O8 |
|---|---|
| Molecular Weight | 1088.21 |