产品
编 号：F234782
分子式：C20H21N7O
分子量：375.43
分子式：C20H21N7O
分子量：375.43
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1876467-74-1
产品详情
生物活性：
Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity. Elimusertib can be used for the research of solid tumors and lymphomas.
体内研究：
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).Animal Model:Female C.B-17 SCID mice, SU-DHL-8 GCB-DLBCL xenograft model
Dosage:50 mg/kg
Administration:Oral administration, b.i.d., 3 days on/4 days off, for 11 days
Result:Inhibited tumor area.
Animal Model:Male Wistar rats
Dosage:0.3-0.5 mg/kg for i.v.; 0.6-1 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous injection and oral administration
Result:Oral bioavailability (87%), T1/2 (1.3 h).
Animal Model:Female beagle dogs
Dosage:0.3-0.5 mg/kg for i.v.; 0.6-1 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous injection and oral administration
Result:Oral bioavailability (51%), T1/2 (1.0 h).
体外研究：
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).
Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib has anti-tumor activity. Elimusertib can be used for the research of solid tumors and lymphomas.
体内研究：
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).Animal Model:Female C.B-17 SCID mice, SU-DHL-8 GCB-DLBCL xenograft model
Dosage:50 mg/kg
Administration:Oral administration, b.i.d., 3 days on/4 days off, for 11 days
Result:Inhibited tumor area.
Animal Model:Male Wistar rats
Dosage:0.3-0.5 mg/kg for i.v.; 0.6-1 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous injection and oral administration
Result:Oral bioavailability (87%), T1/2 (1.3 h).
Animal Model:Female beagle dogs
Dosage:0.3-0.5 mg/kg for i.v.; 0.6-1 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous injection and oral administration
Result:Oral bioavailability (51%), T1/2 (1.0 h).
体外研究：
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).
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