CCT128930 - 10mM in DMSO , CAS No.885499-61-6

CAS: 885499-61-6 Cat. No.: C409110 Peso molecular: 341.84

GRADE & PURITY 10mM in DMSO

Synonyms

4-(4-chlorobenzyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

CCT128930 is a potent, ATP-competitive and selective inhibitor ofAkt2withIC50of 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, andautophagyindependent o
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- U87MG human glioblastoma cells and Akt pathway blockade.

In vivo

CCT128930 at 25 mg/kg i.p. shows a marked antitumor effect in established PTEN- 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 AUC_0-∞ of 4.6 μM h. CCT128930 administrated via i.p. leads to the peak plasma drug concentration of 1.3 μM and the corresponding AUC_0-∞ of 1.3 μM·h. Oral CCT128930 administration leads to the peak plasma concentration of only 0.43 μM and a correspondingly low AUC_0-∞ of 0.4 μM·h.
Cell Data

cell lines：

Concentrations：0-18.9 μM

Incubation Time：48 hours

Powder Purity:≥99%

Specifications

Sinónimos

4-(4-chlorobenzyl)-1-(7H-pyrrolo[2, 3-d]pyrimidin-4-yl)piperidin-4-amine

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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 indepen

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Nombres e identificadores

• Isómeros SMILES: C1CN(CCC1(CC2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4
• Peso molecular: 341.84
• Reaxy-Rn: 12598617
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12598617&ln=

Objetivos asociados (humanos)

CYP2D6 Tclin Cytochrome P450 2D6 (2 Activities)

Discover Target: CYP2D6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase (2 Activities)

Discover Target: AKT2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase (2 Activities)

Discover Target: AKT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 56 mg/mL (198.88 mM); Water: 19 mg/mL (67.47 mM); Ethanol: 4 mg/mL (14.2 mM)