A-674563 HCl | CAS#2070009-66-2 | AKT1 inhibitor

A-674563 HCl
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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

Chemical Structure

A-674563 HCl

CAS# 2070009-66-2 (HCl)

Instruction

Theoretical Analysis

MedKoo Cat#: 556343
Name: A-674563 HCl
CAS#: 2070009-66-2 (HCl)
Chemical Formula: C22H23ClN4O
Exact Mass: 0.00
Molecular Weight: 394.903
Elemental Analysis: C, 66.91; H, 5.87; Cl, 8.98; N, 14.19; O, 4.05

Price and Availability

Size	Price	Availability
50mg	USD 550	2 Weeks
100mg	USD 950	2 Weeks
200mg	USD 1450	2 Weeks
500mg	USD 2850	2 Weeks
1g	USD 4250	2 Weeks
2g	USD 7650	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 394.90 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:

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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.

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