AT9283

SKU: orb1304573

Description

AT9283

Research Area

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

Key Properties

• CAS Number: 896466-04-9
• MW: 381.43
• Purity: 99.91%
• Formula: C₁₉H₂₃N₇O₂
• SMILES: O=C(NC1CC1)Nc1c[nH]nc1-c1nc2cc(CN3CCOCC3)ccc2[nH]1
• Target: Bcr-Abl,JAK,Aurora Kinase,Apoptosis,FLT,Autophagy
• Solubility: DMSO:71 mg/mL (186.14 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:22 mg/mL (57.68 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.24 mM)

Bioactivity

• Target IC50:
  Abl (T315I):4 nM|Aurora A:3 nM|JAK3:1.1 nM|JAK2:1.2 nM|Aurora B:3 nM
• In Vivo:
  In HCT116 cells, AT9283 inhibits Aurora B kinase activity with an IC50 value of 30 nM, leading to a polyploid phenotype and concurrently suppressing colony formation. Moreover, AT9283 significantly inhibits a range of kinases, including Aurora A (IC50=3 nM), Aurora B (IC50=3 nM), JAK3 (IC50=1.1 nM), JAK2 (IC50=1.2 nM), and Abl (IC50=4 nM).
• In Vitro:
  In mice bearing HCT116 human colorectal carcinoma xenografts, AT9283 (15-20 mg/kg) was capable of inhibiting tumor growth.
• Cell Research:
  HCT 116 cells are cultured in DMEM + 10% FBS + GLUTAMAX I. Black 96-well flat-bottomed (clear) tissue culture treated plates are seeded in 200 μL of medium and incubated for approximately 16 hours at 37°C in a humidified atmosphere of 5% CO2 in air. Cells are treated with test compound at nine different concentrations (spanning 1 nM to 10 μM, plus DMSO vehicle control) and then incubated for 72 hours. Polyploidy morphological observations of the cells are then noted. The concentration of AT9283 required to produce a distinct polyploid phenotype is reported. Cells are seeded at a concentration of 75−100 cells/mL relevant culture media onto 6- or 24-well tissue culture plates and allowed to recover for 16 hours. Test compound (11 concentrations spanning 0.1 nM to 10 μM) or vehicle control (DMSO) is added to duplicate wells to give a final DMSO concentration of 0.1%. Following compound addition, colonies are allowed to grow between 10 and 14 days for optimum discrete colony counting. Colonies are fixed in 2 mL of Carnoys fixative (25% acetic acid, 75% MeOH) and stained in 2 mL of 0.4% w/v crystal violet. The numbers of colonies in each well is counted. IC50 values are calculated by sigmoidal dose-response (variable slope) IC50 curves using Prism Graphpad software. (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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, AT-9283, AT9283, AT 9283, Aurora B, Aurora A, Autophagy, Aurora Kinase, AuroraKinase, BcrAbl, Bcr-Abl, Abl1 (T315I), Cluster of differentiation antigen 135, CD135, inhibit, J 504568, Janus kinase, JAK3, JAK, J504568, J-504568, JAK2, Inhibitor, FLT3, Fms like tyrosine kinase 3

Compound Identifiers

PubChem CID

135398495