552325-73-2 Usage
Uses
A-674563 inhibits Akt1, PKA and CDK2 with Ki of 11 nM, 16 nM and 46 nM, respectively.
Biological Activity
a-674563 is a potent and selective akt1 inhibitor with ic50 value of 14 nm. a-67453 also inhibited pka and cdk2 with ic50 value of 16 nm and 46 nm.akt, also known as protein kinase b, is a serine/threonine-specific protein kinase that plays a key role in multiple cellular processes such as glucose metabolism, apoptosis, cell proliferation, transcription and cell migration.in miapaca-2 cells treated with a-674563 for 48 hour, it slowed the tumor cell proliferation (ec50 = 0.4 μm). in sts cells, phosphorylation of gsk3 and mdm2 was prominently reduced by a-674563 treatment. [1] akt inhibition-induced g2 cells cycle arrest and apoptosis were also observed in a563-treated sts cells. [2]in scid mice carrying established pc-3 tumors, administration of a-674563 at 40 mg/kg per day for 21 days, combined with administration of paclitaxel at 15 mg/kg per day on days 20.24.28, increased the efficacy of paclitaxel compared with paclitaxel monotherapy. [1] a563 also significantly blocked ht1080 xenograft growth in nude mice. [2]
references
1. luo y, shoemaker ar, liu x et al. potent and selective inhibitors of akt kinases slow the progress of tumors in vivo. mol cancer ther. 2005 jun;4(6):977-86.2. zhu qs, ren w, korchin b et al. soft tissue sarcoma cells are highly sensitive to akt blockade: a role for p53-independent up-regulation of gadd45 alpha. cancer res. 2008 apr 15;68(8):2895-903.
Check Digit Verification of cas no
The CAS Registry Mumber 552325-73-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 5,5,2,3,2 and 5 respectively; the second part has 2 digits, 7 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 552325-73:
(8*5)+(7*5)+(6*2)+(5*3)+(4*2)+(3*5)+(2*7)+(1*3)=142
142 % 10 = 2
So 552325-73-2 is a valid CAS Registry Number.
InChI: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
