857531-00-1

Basic information

• Product Name: AT7867
• Synonyms: AT7867;Piperidine, 4-(4-chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]-;4-(4-Chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine;AT-7867(AT7867);4-(4-(1H-pyrazol-4-yl)phenyl)-4-(4-chlorophenyl)piperidine;4-(4-Chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine AT 7867;Piperidine, 4-(4-chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]- 4-(4-Chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine
• CAS NO: 857531-00-1
• Molecular Formula: C20H20ClN3
• Molecular Weight: 337.86
• EINECS: -0
• Product Categories: Inhibitors;Akt;mTOR;PI3K
• Mol File: 857531-00-1.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 530.2 °C at 760 mmHg
• Flash Point: 274.5 °C
• Appearance: /
• Density: 1.214
• Solubility: ≥16.9 mg/mL in DMSO; ≥4.38 mg/mL in EtOH with ultrasonic; ≥45 mg/mL in H2O
• CAS DataBase Reference: AT7867(CAS DataBase Reference)
• NIST Chemistry Reference: AT7867(857531-00-1)
• EPA Substance Registry System: AT7867(857531-00-1)

Safety Data

• Hazardous Substances Data: 857531-00-1(Hazardous Substances Data)

Usage

Description

AT7867 is a potent and orally bioavailable inhibitor of Akt isoforms Akt1, 2, and 3 (IC50s = 32, 17, and 47 nM, respectively). It also inhibits p70S6 kinase and PKA (IC50s = 85 and 20 nM, respectively), but is without effect against a panel of other kinases. AT7867 inhibits growth and induces apoptosis in a variety of cancer cell lines in vitro and suppresses tumor growth of PTEN-deficient xenografts in mice.

Uses

A potent Akt inhibitor with an IC50 of 17 nM. AT7867 also inhibits structurally related AGC kinases p70S6K and PKA with IC50s of 20 nM and 85 nM, respectively.

Enzyme inhibitor

This potent ATP-competitive inhibitor (FW = 337.85; CAS 857531-00-1; Solubility: 68 mg/mL DMSO, <1 mg/mL H2O), known systematically as 4- (4-(1H-pyrazol-4-yl)phenyl)-4-(4-chlorophenyl)piperidine, targets Akt1, Akt2 and Akt3 Protein Kinases B (or PKB), with IC50 values of 32 nM, 17 nM and 47 nM, respectively. AT7867 also inhibits the structurally related AGC kinases, p70S6K and PKA, with IC50 values of 20 nM and 85 nM, respectively.

references

grimshaw km, hunter lj, yap ta et al. at7867 is a potent and oral inhibitor of akt and p70 s6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. mol cancer ther. 2010 may;9(5):1100-10.

Relevant articles and documents

PHARMACEUTICAL COMPOUNDS

The invention provides compounds of the formula (I) having ROCK kinase and/or protein kinase p70S6K inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length