WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H401012
CAS#: 552325-73-2
Description: A-674563 is a potent, orally available Akt1 inhibitor with an IC50 value of 11nM. Also displays activity against PKA and CDK2 with IC50 values of 16nM and 46nM respectively. A-674563 could contribute to culture conditions that expand chondrocytes without losing chondrocytic characters, and was significantly more effective at reducing NSCLC cell survival relative to the pan-AKT inhibitor MK-2206.
Hodoodo Cat#: H401012
Name: A-674563
CAS#: 552325-73-2
Chemical Formula: C22H22N4O
Exact Mass: 358.18
Molecular Weight: 358.436
Elemental Analysis: C, 73.72; H, 6.19; N, 15.63; O, 4.46
Synonym: A674563; A 674563; A-674563
IUPAC/Chemical Name: (S)-1-((5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl)oxy)-3-phenylpropan-2-amine
InChi Key: BPNUQXPIQBZCMR-IBGZPJMESA-N
InChi Code: InChI=1S/C22H22N4O/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)/t19-/m0/s1
SMILES Code: N[C@@H](CC1=CC=CC=C1)COC2=CC(C3=CC4=C(NN=C4C)C=C3)=CN=C2
Appearance: Solid powder
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: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
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
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 358.44 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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: 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.
2: 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.
3: 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.
4: 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.
5: 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.
6: 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.
7: 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.
8: 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.
9: 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.
10: 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.
11: 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.
12: 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.
13: 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.
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.