Afuresertib

SKU: orb1307134

Description

Afuresertib

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1047644-62-1
• MW: 427.32
• Purity: 99.77%
• Formula: C₁₈H₁₇Cl₂FN₄OS
• SMILES: Cn1ncc(Cl)c1-c1cc(sc1Cl)C(=O)N[C@H](CN)Cc1cccc(F)c1
• Target: PKC,ROCK,Akt
• Solubility: DMSO:50 mg/mL (117.01 mM);Ethanol:79 mg/mL (184.87 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.68 mM)

Bioactivity

• Target IC50:
  PKCη:210 nM|PKCθ:510 nM|Akt3:2.6 nM(Ki)|ROCK:100 nM|PKCβI:430 nM|Akt1:0.08 nM(Ki)|Akt2:2 nM(Ki)
• In Vivo:
  Ove All 65% of hematological cell lines were sensitive to Afuresertib with an EC50 < 1 μM. 21% of solid tumor cell lines tested had an EC50 < 1 μM for Afuresertib. Afuresertib inhibite the kinase activity o the E17K AKT1 mutant protein with an EC50 of 0.2 nM. Afuresertib showed Afuresertib showed a concentration dependent effect o the phosphorylation levels of multiple AKT substratees, including GSK3b, PRAS40, FOXO and cystatin 9.
• In Vitro:
  Ove All 65% of hematological cell lines were sensitive to Afuresertib with an EC50 < 1 μM. 21% of solid tumor cell lines tested had an EC50 < 1 μM for Afuresertib. Afuresertib inhibite the kinase activity o the E17K AKT1 mutant protein with an EC50 of 0.2 nM. Afuresertib showed Afuresertib showed a concentration dependent effect o the phosphorylation levels of multiple AKT substratees, including GSK3b, PRAS40, FOXO and cystatin 9.
• Cell Research:
  A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth Inhibition b the compounds at 0-30 μM. Cell growth is determined relative to untreated (DMSO) controls. EC50's are calculated from Inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Afuresertib, Akt, Akt3, Akt2, Akt1, inhibit, Inhibitor, GSK 2110183, GSK2110183, GSK-2110183, GSK2110183C, Rho-associated kinase, Rho-associated protein kinase, ROCK, ROK, Rho-kinase, PKB, PKC, Protein kinase C, Protein kinase B

Compound Identifiers

PubChem CID

46843057