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Elimusertib

CAS No. : 1876467-74-1

MCE 站：Elimusertib

产品活性：Elimusertib (BAY-1895344) 是一种有效、可口服、选择性的 ATR 抑制剂，IC₅₀ 值为 7 nM，具有抗肿瘤活性。Elimusertib 可用于实体瘤和淋巴瘤的研究。

研究领域：Cell Cycle/DNA Damage  |  PI3K/Akt/mTOR

作用靶点：ATM/ATR

In Vitro: Elimusertib potently inhibits the proliferation of a broad spectrum of human tumor cell lines with a median IC₅₀ of 78 nM.
Elimusertib potently suppresses hydroxyurea-induced H2AX phosphorylation (IC₅₀: 36 nM).
Elimusertib shows good selectivity against mTOR (ratio of IC₅₀ values: mTOR/ATR 61).
Elimusertib reveals high selectivity against other related kinases, such as DNA-PK (IC₅₀: 332 nM), ATM (IC₅₀: 1420 nM), ａnd PI3K (IC₅₀: 3270 nM).
Elimusertib has potent antiproliferative activity against various cancer cell lines in vitro, 25 for example in the CRC cell lines HT-29 (IC₅₀: 160 nM) ａnd LoVo (IC₅₀: 71 nM), ａnd in the B-cell lymphoma cell line SU-DHL-8 (IC₅₀: 9 nM).

In Vivo: Elimusertib shows potent anti-tumor efficacy in monotherapy in a variety of xenograft models of ovarian ａnd colorectal cancer, ａnd causes complete tumor remission in mantle cell lymphoma models.
Elimusertib (50 mg/kg; p.o.; b.i.d.; 3 days on/4 days off; for 11 days) exhibits strong antitumor efficacy in the ATM-mutated SU-DHL-8 (ATM K1964E) human GCB-DLBCL cell line derived xenograft model in mice.
Elimusertib (20 mg/kg, ａnd 10 mg/kg from day 14; p.o.; daily; 2 days on/5 days off; for 42 days) in combination with Carboplatin (40 mg/kg; i.p.; daily; 1 day on/6 days off) results in synergistic antitumor activity in the platinum-resistant ATM protein low expressing CR5038 human CRC PDX model in NOD/SCID mice.
Elimusertib exhibits moderate oral bioavailability (rat 87%, dog 51%) following oral administration (rat ａnd dog 0.6-1 mg/kg).
Elimusertib exhibits terminal elimination half-lives (mouse 0.17 h, rat 1.3 and, dog 1.0 h) due to plasma clearance (3.5, 1.2, ａnd 0.79 L/h/kg respectively) following intravenous administration (mouse, rat ａnd dog 0.3-0.5 mg/kg).

相关产品：Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Ceralasertib  |  KU-55933  |  Elimusertib hydrochloride  |  AZD0156  |  KU-60019  |  AZD1390  |  VE-821  |  AZ20  |  CGK733  |  ATR inhibitor 2  |  AZ32  |  CP-466722  |  KU 59403  |  ETP-46464  |  Garci C  |  Ro 90-7501  |  NU6027  |  Antitumor agent-28  |  ATM Inhibitor-1  |  ATR inhibitor 1

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