Elimusertib

SKU: orb1299925

Description

Elimusertib

Research Area

Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 1876467-74-1
• MW: 375.43
• Purity: 99.98% (May vary between batches)
• Formula: C₂₀H₂₁N₇O
• SMILES: C[C@@H]1COCCN1c1cc(-c2ccnn2C)c2ccnc(-c3cc[nH]n3)c2n1
• Target: ATM/ATR
• Solubility: DMSO:22.5 mg/mL (59.93 mM)

Bioactivity

• Target IC50:
  ATR:7 nM (IC50)
• In Vivo:
  The novel selective ATR kinase inhibitor Elimusertib on tumor cell growth and viability.Potent antiproliferative activity was demonstrated in a broad spectrum of human tumor cell lines.Elimusertib exhibited strong monotherapy efficacy in cancer xenograft models that carry DNA damage repair deficiencies.The combination of Elimusertib with DNA damage-inducing chemotherapy or external beam radiotherapy (EBRT) showed synergistic antitumor activity.Combination treatment with Elimusertib and DDR inhibitors achieved strong synergistic antiproliferative activity in vitro, and combined inhibition of ATR and PARP signaling using olaparib demonstrated synergistic antitumor activity in vivo Furthermore, the combination of Elimusertib with the novel, nonsteroidal androgen receptor antagonist darolutamide resulted in significantly improved antitumor efficacy compared with respective single-agent treatments in hormone-dependent prostate cancer,and addition of EBRT resulted in even further enhanced antitumor efficacy.
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Storage & Handling

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

Alternative Names

Inhibitor, inhibit, lymphomas, genomic, instability, Elimusertib, ATM, ATM and RAD3 related, ATM/ATR, Ataxia telangiectasia mutated, ATR, BAY1895344, BAY-1895344, BAY 1895344, DNA, damage, tumors, response, replication, repair, stress, solid

Compound Identifiers

PubChem CID

118869362