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AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA induces apoptosis.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $50 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $152 | In Stock | |
25 mg | $273 | In Stock | |
50 mg | $465 | In Stock | |
100 mg | $682 | In Stock | |
1 mL x 10 mM (in DMSO) | $147 | In Stock |
Description | AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA induces apoptosis. |
Targets&IC50 | CIAP2:21 nM, XIAP:15 nM, CIAP1:15 nM |
In vitro | AZD5582 TFA (20 nM; 48 h; H1975 NSCLC cell line) in collaboration with IFNγ or viral double-stranded RNA (dsRNA), suppresses cell viability and even induces cell death in H1975 NSCLC cells.[2] AZD5582 TFA (20 nM; 17 or 25 h) induces cIAP-1 downregulation, promotes RIPK1 activation (an upstream regulator of caspase-8), and initiates the activation of both extrinsic (caspase-8) and intrinsic (caspase-9) apoptotic pathways, resulting in the cleavage of caspase-3 and caspase-7.[2] AZD5582 TFA (20 nM; 48 h; H1975 NSCLC cell line) is involved in apoptosis due to induction of cell death and active caspase-3/8 activities by AZD5582 TFA and IFNγ co-treatment in HCC827 NSCLC cells.[2] |
In vivo | AZD5582 TFA (0.1-3.0 mg/kg; i.v.; once a week; 2 weeks; MDA-MB-231 xenograft-bearing mice) triggers cIAP1 degradation and caspase 3 cleavage within tumor cells. Following a two-week treatment, significant tumor resolution is observed. Upon administering a medium dose of 0.5 mg/kg AZD5582 TFA to mice, cIAP1 degradation occurs upon administration, although it takes some time for the apoptosis-inducing effects to manifest.[1] |
Alias | AZD5582 TFA(1258392-53-8 free base) |
Molecular Weight | 1129.31 |
Formula | C60H79F3N8O10 |
Smiles | O=C([C@H]1N(CCC1)C([C@H](C2CCCCC2)NC([C@H](C)NC)=O)=O)N[C@H]3C4=CC=CC=C4C[C@H]3OCC#CC#CCO[C@H]5[C@H](C6=CC=CC=C6C5)NC([C@H]7N(CCC7)C([C@H](C8CCCCC8)NC([C@H](C)NC)=O)=O)=O.OC(C(F)(F)F)=O |
Relative Density. | no data available |
Storage | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (44.27 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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