WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 556343
CAS#: 2070009-66-2 (HCl)
Description: A-674563 is a potent and selective Akt1 inhibitor with Ki of 11 nM. A-674563 suppressed the activation of the NLRP3 inflammasome in cardiomyocytes following β-adrenoceptor activation, suggesting that AKT1 is a critical regulator molecule upstream of the NLRP3 inflammasome. A-674563 suppresses CDK2 activity, inhibits human NSCLC cell growth more effectively than the pan-AKT inhibitor, MK-2206
MedKoo Cat#: 556343
Name: A-674563 HCl
CAS#: 2070009-66-2 (HCl)
Chemical Formula: C22H23ClN4O
Exact Mass:
Molecular Weight: 394.903
Elemental Analysis: C, 66.91; H, 5.87; Cl, 8.98; N, 14.19; O, 4.05
Related CAS #: 2070009-66-2 (HCl) 552325-73-2 (free base)
Synonym: A-674563 HCl; A-674563 hydrochloride; A-674563; A674563; A 674563;
IUPAC/Chemical Name: (S)-1-((5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl)oxy)-3-phenylpropan-2-amine hydrochloride
InChi Key: HLNHYVLLEFHBJD-FYZYNONXSA-N
InChi Code: InChI=1S/C22H22N4O.ClH/c1-15-21-11-17(7-8-22(21)26-25-15)18-10-20(13-24-12-18)27-14-19(23)9-16-5-3-2-4-6-16;/h2-8,10-13,19H,9,14,23H2,1H3,(H,25,26);1H/t19-;/m0./s1
SMILES Code: N[C@@H](CC1=CC=CC=C1)COC2=CC(C3=CC4=C(C=C3)NN=C4C)=CN=C2.[H]Cl
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 394.903 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Wang R, Wang Y, Wu J, Guo Y, Xiao H, Zhang Y, Ma K. Resveratrol Targets AKT1 to Inhibit Inflammasome Activation in Cardiomyocytes Under Acute Sympathetic Stress. Front Pharmacol. 2022 Feb 17;13:818127. doi: 10.3389/fphar.2022.818127. PMID: 35250567; PMCID: PMC8891986.
2: He Y, Luo Y, Huang L, Zhang D, Wang X, Ji J, Liang S. New frontiers against sorafenib resistance in renal cell carcinoma: From molecular mechanisms to predictive biomarkers. Pharmacol Res. 2021 Aug;170:105732. doi: 10.1016/j.phrs.2021.105732. Epub 2021 Jun 15. PMID: 34139345.
3: Chen Y, Zhang H, Li F, Wang X. Inhibition of CX3C receptor 1-mediated autophagy in macrophages alleviates pulmonary fibrosis in hyperoxic lung injury. Life Sci. 2020 Oct 15;259:118286. doi: 10.1016/j.lfs.2020.118286. Epub 2020 Aug 15. PMID: 32810508.
4: Goßmann M, Linder P, Thomas U, Juhasz K, Lemme M, George M, Fertig N, Dragicevic E, Stoelzle-Feix S. Integration of mechanical conditioning into a high throughput contractility assay for cardiac safety assessment. J Pharmacol Toxicol Methods. 2020 Sep;105:106892. doi: 10.1016/j.vascn.2020.106892. Epub 2020 Jul 3. PMID: 32629160.
5: Ding HR, Wang JL, Tang ZT, Wang Y, Zhou G, Liu Y, Ren HZ, Shi XL. Mesenchymal Stem Cells Improve Glycometabolism and Liver Regeneration in the Treatment of Post-hepatectomy Liver Failure. Front Physiol. 2019 Apr 10;10:412. doi: 10.3389/fphys.2019.00412. PMID: 31024348; PMCID: PMC6468048.
6: Chorner PM, Moorehead RA. A-674563, a putative AKT1 inhibitor that also suppresses CDK2 activity, inhibits human NSCLC cell growth more effectively than the pan-AKT inhibitor, MK-2206. PLoS One. 2018 Feb 22;13(2):e0193344. doi: 10.1371/journal.pone.0193344. PMID: 29470540; PMCID: PMC5823456.
7: Dai B, Yan T, Zhang A. ROR2 receptor promotes the migration of osteosarcoma cells in response to Wnt5a. Cancer Cell Int. 2017 Nov 29;17:112. doi: 10.1186/s12935-017-0482-y. PMID: 29213214; PMCID: PMC5707918.
8: Kobayashi T, Fujita K, Kamatani T, Matsuda S, Tsumaki N. A-674563 increases chondrocyte marker expression in cultured chondrocytes by inhibiting Sox9 degradation. Biochem Biophys Res Commun. 2018 Jan 1;495(1):1468-1475. doi: 10.1016/j.bbrc.2017.11.180. Epub 2017 Dec 5. PMID: 29196261.
9: Chen O, Cao Z, Li H, Ye Z, Zhang R, Zhang N, Huang J, Zhang T, Wang L, Han L, Liu W, Sun X. High-concentration hydrogen protects mouse heart against ischemia/reperfusion injury through activation of thePI3K/Akt1 pathway. Sci Rep. 2017 Nov 1;7(1):14871. doi: 10.1038/s41598-017-14072-x. PMID: 29093541; PMCID: PMC5665927.
10: Zou Y, Fan G, Wang X. Pre-clinical assessment of A-674563 as an anti- melanoma agent. Biochem Biophys Res Commun. 2016 Aug 12;477(1):1-8. doi: 10.1016/j.bbrc.2016.03.020. Epub 2016 Mar 10. PMID: 26970307.
11: Xu L, Zhang Y, Gao M, Wang G, Fu Y. Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells. Biochem Biophys Res Commun. 2016 Apr 15;472(4):662-8. doi: 10.1016/j.bbrc.2016.02.094. Epub 2016 Feb 23. PMID: 26920060.
12: Franks SE, Briah R, Jones RA, Moorehead RA. Unique roles of Akt1 and Akt2 in IGF-IR mediated lung tumorigenesis. Oncotarget. 2016 Jan 19;7(3):3297-316. doi: 10.18632/oncotarget.6489. PMID: 26654940; PMCID: PMC4823107.
13: Kim H, Prasain N, Vemula S, Ferkowicz MJ, Yoshimoto M, Voytik-Harbin SL, Yoder MC. Human platelet lysate improves human cord blood derived ECFC survival and vasculogenesis in three dimensional (3D) collagen matrices. Microvasc Res. 2015 Sep;101:72-81. doi: 10.1016/j.mvr.2015.06.006. Epub 2015 Jun 27. PMID: 26122935; PMCID: PMC4537830.
14: Tei H, Miyake H, Fujisawa M. Enhanced sensitivity to sorafenib by inhibition of Akt1 expression in human renal cell carcinoma ACHN cells both in vitro and in vivo. Hum Cell. 2015 Jul;28(3):114-21. doi: 10.1007/s13577-015-0112-8. Epub 2015 Apr 11. PMID: 25862630.
