AZD-5582
- CAS No.
- 1258392-53-8
- Chemical Name:
- AZD-5582
- Synonyms
- ZD5582;CS-2673;AZD-5582;AZD5582 ,S7362;AZD5582;AZD-5582;AZD 5582;3,3'-[2,4-Hexadiyne-1,6-diylbis[oxy[(1S,2R)-2,3-dihydro-1H-indene-2,1-diyl]]]bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-L-prolinamide];L-Prolinamide, 3,3'-[2,4-hexadiyne-1,6-diylbis[oxy[(1S,2R)-2,3-dihydro-1H-indene-2,1-diyl]]]bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-;(2S,2'S)-N,N'-((1S,1'S,2R,2'R)-(hexa-2,4-diyne-1,6-diylbis(oxy))bis(2,3-dihydro-1H-indene-2,1-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide);(2S,2'S)-N,N'-((1S,1'S,2R,2'R)-(hexa-2,4-diyne-1,6-diylbis(oxy))bis(2,3-dihydro-1H-indene-2,1-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide);(S,S,2S,2'S)-N,N'-((1S,1'S,2R,2'R)-(hexa-2,4-diyne-1,6-diylbis(oxy))bis(2,3-dihydro-1H-indene-2,1-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide)
- CBNumber:
- CB52731019
- Molecular Formula:
- C58H78N8O8
- Molecular Weight:
- 1015.29
- MDL Number:
- MFCD28411397
- MOL File:
- 1258392-53-8.mol
Boiling point | 1207.3±65.0 °C(Predicted) |
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Density | 1.26±0.1 g/cm3(Predicted) |
storage temp. | 4°C, protect from light, stored under nitrogen |
solubility | DMF: 30 mg/ml; DMSO: 15 mg/ml; Ethanol: 30 mg/ml |
form | A crystalline solid |
pka | 12.99±0.40(Predicted) |
color | White to yellow |
InChIKey | BRCXWBBDZROUEZ-WCMFYDHYSA-N |
UNSPSC Code | 12352200 |
NACRES | NA.77 |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS07 |
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Signal word | Warning |
Hazard statements | H302 |
Precautionary statements | P280-P305+P351+P338 |
AZD-5582 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML2900 | AZD5582 ≥98% (HPLC) | 1258392-53-8 | 5mg | $121 | 2025-07-31 | Buy |
Sigma-Aldrich | SML2900 | AZD5582 ≥98% (HPLC) | 1258392-53-8 | 25mg | $489 | 2025-07-31 | Buy |
TRC | A808300 | AZD5582 | 1258392-53-8 | 1mg | $165 | 2021-12-16 | Buy |
Activate Scientific | AS117573 | AZD5582 98+% | 1258392-53-8 | 5mg | $177 | 2021-12-16 | Buy |
Activate Scientific | AS117573 | AZD5582 98+% | 1258392-53-8 | 1mg | $88 | 2021-12-16 | Buy |
AZD-5582 Chemical Properties,Uses,Production
Uses
It is a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer.
Biological Activity
AZD5582 is a divalent AVPI motif-based Smac (DIABLO) mimetic (SMC) th at acts a potent apoptosis protein repe at (BIR) domain-targeting antagonist against inhibitor of apoptosis proteins (IAPs) cIAP1/2 (BIR3 IC50 = 15/21 nM against 2.5 nM AbuRPFK-5FAM) and XIAP (BIR2/3 IC50 = 21/15 nM). AZD5582 abolishes cellular XIAP-caspase-9 interaction (1 μM, 4 hrs), induces cIAP1/2 degradation (EC50 = 0.1 nM, 1 hr) and apoptosis (GI50 <60 pM, 48 hrs) in MDA-MB-231 breast cancer cultures. AZD5582 causes substantial tumor regression by inducing cIAP1 degradation and apoptosis in tumor cells in MDA-MB-231 xenograft-bearing mice in vivo (3.0 mg/kg/wk i.v.).
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 |
IC 50
cIAP1: 15 nM (IC50); cIAP2: 21 nM (IC50); XIAP: 15 nM (IC50)
AZD-5582 Preparation Products And Raw materials
Raw materials
Preparation Products
AZD-5582 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32433 | 58 |
Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30229 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
HANGZHOU LEAP CHEM CO., LTD. | +86-571-87711850 | market18@leapchem.com | China | 24727 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39031 | 58 |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |