Gartisertib

SKU: orb1710367

Description

Gartisertib

Research Area

Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 1613191-99-3
• MW: 541.55
• Formula: C₂₅H₂₉F₂N₉O₃
• SMILES: Nc1nn2cc(F)cnc2c1C(=O)Nc1cncc(F)c1N1CCC(CC1)C(=O)N1CCN(CC1)C1COC1
• Target: ATM/ATR
• Solubility: DMSO:16 mg/mL (29.54 mM);10% DMSO+90% Saline:1.5 mg/mL (2.77 mM)

Bioactivity

• Target IC50:
  ATR:8 nM
• In Vivo:
  Gartisertib (10 mg/kg or 20 mg/kg) plus cisplatin inhibited tumor growth in metastatic clear cell renal cell carcinoma (ccRCC) xenografts, demonstrating therapeutic synergies.
  Read more...
• In Vitro:
  Gartisertib was four times more potent in all glioblastoma cell lines than the widely used ATR inhibitor berzosertib (Gartisertib median IC50 = 0.56 μM, berzosertib median IC50 = 2.21 μM). In addition, Gartisertib observed a higher IC50 (7.22 μM) in human astrocytes, indicating a lower potential toxicity of Gartisertib to normal brain cells. The combination of Gartisertib (1 μM) with TMZ+RT significantly increased apoptosis and cell death in patient-derived glioblastoma cell lines.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Gartisertib, M 4344, M4344, ATM, ATR inhibitor 2, ATR, VRT1228692, VX 03, VX-803

Compound Identifiers

PubChem CID

86720912