CCT128930(CCT 128930

CCT128930(CCT 128930 - Names and Identifiers

Name	4-(4-chlorobenzyl)-1-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidin-4-aMine
Synonyms	CS-447 CCT128930 CCT 128930 CCT128930(CCT 128930 4-(4-chlorobenzyl)-1-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)piperidin-4-aMine 4-[(4-Chlorophenyl)methyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinamine 4-PiperidinaMine, 4-[(4-chlorophenyl)Methyl]-1-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)- 4-Piperidinamine, 4-[(4-chlorophenyl)methyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-
CAS	885499-61-6

CCT128930(CCT 128930 - Physico-chemical Properties

Molecular Formula	C18H20ClN5
Molar Mass	341.84
Density	1.39
Boling Point	547.902 °C at 760 mmHg
pKa	13.93±0.50(Predicted)
Storage Condition	-20℃
In vitro study	CCT128930 is 28 times more selective for AKT2 than for the closely related PKA kinase and 20 times more selective for p70S6K. CCT128930 acts on PTEN-deficient human tumor cell lines, including U87MG human malignant glioma cells, LNCaP human prostate cancer cells and PC3 human prostate cancer cells, with significant anti-proliferative activity, GI50 6.3 μm, respectively, 0.35 μm and 1.9 μm. Moreover, CCT128930 acts on PTEN-null U87MG human malignant glioma cells, stops the cell cycle at G1 phase, and blocks the AKT pathway.
In vivo study	CCT128930 administered PTEN-null U87MG human malignant glioma intraperitoneally at a dose of 25 mg/kg has a significant anti-tumor effect, with a T/C ratio of 48% on the 12th day of treatment. CCT128930 treated BT474 human breast cancer xenografts with HER2 positive and PIK3CA mutation at a dose of 40 mg/kg, which produced profound anti-tumor effects and completely arrested tumor growth. On the 22nd day of treatment, the T/C ratio was 29%. In Vivo, CCT128930 is administered intravenously to plasma, reaching a maximum concentration of 6.4 μm, with a relatively short half-life, high volume distribution, and rapid clearance. Treatment with CCT128930 intraperitoneal injection yielded a maximum plasma drug concentration of 1.3 μm, corresponding to an UC 0-∞ of 1.3 μm h. CCT128930 was orally treated with a maximum plasma concentration of only 0.43 μm, and the corresponding auc0-∞ was as low as 0.4 μm h.