A-674563 Inhibitor CAS No. 552325-73-2

Cat. No.	Name	Size	Price
KI1156	A-674563	2 mg	$272
	A-674563	5 mg	$464
	A-674563	10 mg	$832
	A-674563	50 mg	$2680
	A-674563	100 mg	$4436

Chemical Characteristic

Product Name	A-674563
CAS No.	552325-73-2
Molecular Weight	358.44
Formula	C₂₂H₂₂N₄O
Chemical Name	(alphaS)-alpha-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]benzeneethanamine
Smiles	c1(ccccc1)C[C@H](N)COc1cncc(c1)c1cc2c(n[nH]c2cc1)C
Chemical Structure

Biological activities

A-674563 is a potent serine/threonine kinase Akt (PKB) inhibitor. A-674563 potently inhibits Akt1, PKA and CDK2 with Ki of 11, 16 and 46 nM, respectively. A-674563 also inhibits PKCγ, ERK2, GSK3β and RSK2 with Ki of 360, 260, 110 and 580 nM, respectively. In MiaPaCa-2 cells in vitro, A-674563 (0-30 µM) reduces the phosphorylation of GSK3α/β, TSC2, mTOR, and ribosomal protein S6 in a dose-dependent fashion. In the PC-3 prostate cancer xenograft model, when given in combination, A-674563 (40 mg/kg) increases the anti-tumor efficacy of paclitaxel. In a glucose challenge tests in vivo, A-674563 administration (20 and 100 mg/kg) significantly increases plasma insulin.^[1] Furthermore, A-674563 inhibits hERG ion channels in vitro and causes acute hypotension in vivo.^[2] In vivo, A-674563 also is considered to have drastically improved PK profile with oral bioavailability of 67% in mouse, but is 70-fold less active than A-443654.^[3]

Protocols

In vivo: A-674563 is dissolved in DMSO.^[1]

References

[1] Luo Y, et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther. 2005, 4(6): 977-986. [2] Collins I, et al. Targeted small-molecule inhibitors of protein kinase B as anticancer agents. Anticancer Agents Med Chem. 2009, 9(1): 32-50. [3] Li Q, et al. Recent progress in the discovery of Akt inhibitors as anticancer agents. Expert Opinion on Therapeutic Patents. 2007, 17(9): 1077-1130.

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