CCT128930

For research use only.

Catalog No.S2635

22 publications

CCT128930 Chemical Structure

CAS No. 885499-61-6

CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of CCT128930 triggers cell apoptosis in HepG2 cells.

Selleck's CCT128930 has been cited by 22 publications

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Biological Activity

Description CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of CCT128930 triggers cell apoptosis in HepG2 cells.
Targets
Akt2 [1]
(Cell-free assay)		 p70 S6K [1]
(Cell-free assay)		 PKA [1]
(Cell-free assay)
6 nM 120 nM 168 nM
In vitro

CCT128930 exhibits marked antiproliferative activity against PTEN-deficient human tumor cell lines including U87MG human glioblastoma cells, LNCaP human prostate cancer cells and PC3 human prostate cancer cells with GI50 of 6.3 μM, 0.35 μM and 1.9 μM, respectively. Furthermore, CCT128930 causes a G1 arrest in PTEN-null U87MG human glioblastoma cells and Akt pathway blockade. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87MG cells NVK5XFJzTnWwY4Tpc44h[XO|YYm= MnvwTY5pcWKrdHnvckBw\iCSS1KgbY4hcHWvYX6gWVg4VUdiY3XscJMh[XO|ZYPz[YQh[XNiR2PLN{1j\XSjIIDoc5NxcG:{eXzheIlwdiCkeTDFUGlUSSxiSVO1NF0xNjZ4IH7N MViyNFE2OTZ5Nx?=
PC3M cells M3;yT2Z2dmO2aX;uJIF{e2G7 NX3QUFlRUW6qaXLpeIlwdiCxZjDQT2IhcW5iaIXtZY4hWEN|TTDj[YxteyCjc4Pld5Nm\CCjczDHV2s{NWKndHGgdIhwe3Cqb4L5cIF1cW:wIHL5JGVNUVODLDDJR|UxRTBwMECzJO69VQ>? NXSxdGdDOjBzNUG2O|c>

... Click to View More Cell Line Experimental Data
In vivo CCT128930 at 25 mg/kg i.p. shows a marked antitumor effect in established PTEN-null U87MG human glioblastoma xenografts with a treated:control (T/C) ratio of 48% on day 12. In HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts, CCT128930 at 40 mg/kg also produces a profound antitumor effect with complete growth arrest and a T/C ratio of 29% on day 22. CCT128930 administrated via i.v. reaches a peak concentration of 6.4 μM in plasma and is eliminated with a relatively short half-life, high volume of distribution, and rapid clearance, giving an area under the curve AUC0-∞ of 4.6 μM h. CCT128930 administrated via i.p. leads to the peak plasma drug concentration of 1.3 μM and the corresponding AUC0-∞ of 1.3 μM·h. Oral CCT128930 administration leads to the peak plasma concentration of only 0.43 μM and a correspondingly low AUC0-∞ of 0.4 μM·h. [1]

Protocol

Kinase Assay:[1]
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Kinase assays:

Profiling against 50 different human kinases is carried out using 10 μM CCT128930 at an ATP concentration equivalent to the Km for each enzyme.
Cell Research:[1]
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  • Cell lines: U87MG, LNCaP and PC3 cells
  • Concentrations: 0-18.9 μM
  • Incubation Time: 48 hours
  • Method: Cells are seeded in 96-well plates and allowed to attach for 36 hours to ensure exponential growth prior to treatment. In vitro antiproliferative activity is determined using a 96-hour SRB assay. TCA-fixed cells are stained for 30 minutes with 0.4% (wt/vol) SRB dissolved in 1% acetic acid. At the end of the staining period, SRB is removed and cultures are quickly rinsed four times with 1% acetic acid to remove unbound dye. The acetic acid is poured directly into the culture wells from a beaker. This procedure permits rinsing to be performed quickly so that desorption of protein-bound dye does not occur. Residual wash solution is removed by sharply flicking plates over a sink, which ensures the complete removal of rinsing solution. Because of the strong capillary action in 96-well plates, draining by gravity alone often fails to remove the rinse solution when plates are simply inverted. After being rinsed, the cultures are air dried until no standing moisture is visible. Bound dye is solubilized with 10 mM unbuffered Tris base (pH 10.5) for 5 minutes on a gyratory shaker. OD is read in either a UVmax microtiter plate reader or a Beckman DU-70 spectrophotometer. For maximum sensitivity, OD is measured at 564 nm. Because readings are linear with dye concentrations only below 1.8 OD units, however, suboptimal wavelengths are generally used, so that all samples in an experiment remains within the linear OD range. With most cell lines, wavelengths of approximately 490-530 nm works well for this purpose.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: PTEN-null U87MG human glioblastoma cells are injected subcutaneously (s.c.) in the right flank of female CrTacNCr-Fox1nu mice. For HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts, cells are administered s.c. in medium supplemented with M
  • Dosages: ≤50 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 68 mg/mL (198.92 mM)
Water Insoluble
Ethanol '6 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+ 40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing. 		2 mg/ml

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 341.84
Formula

C18H20ClN5
CAS No. 885499-61-6
Storage powder
in solvent
Synonyms N/A
Smiles C1CN(CCC1(CC2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID