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BAY 80-6946

产品编号: DC9591 Featured
BAY 80-6946
结构式
1032568-63-0
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中国地区超过5000个高品质化合物库存
应用领域
Copanlisib (BAY 80-6946) 是一种有效的，选择性的和 ATP 竞争性的泛 I 类 PI3K 抑制剂，对 PI3Kα，PI3Kδ，PI3Kβ 和 PI3Kγ 的 IC50 分别为 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。除 mTOR 外，Copanlisib 对其他脂质和蛋白激酶的选择性超过 2000 倍。Copanlisib 具有优异的抗肿瘤活性。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 1032568-63-0
名称:
别名: BAY80-6946; Copanlisib
SMILES: COC1=C(C=CC2=C1N=C(N3C2=NCC3)NC(=O)C4=CN=C(N=C4)N)OCCCN5CCOCC5
分子式: C23H28N8O4
分子量: 480.5196
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: BAY 80-6946(Copanlisib) is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM. in vitro: BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. BAY 86-9766 inhibits proliferation with IC50 of 147 nM in HuCCT-1 (KRASG12D ) and 137 nM in EGI-1 (KRASG12D ) cell lines. in vivo: BAY 80-6946 is generally well tolerated through the MTD (maximum tolerated dose) of 0.8 mg/kg. PK (pharmacokinetics) results support weekly dosing. Grade 2/3 hyperglycemia in the first 24 hrs after receiving a dose is common at the MTD. PK, clinical SD and FDG-PET data are consistent with effective exposure and PI3K pathway inhibition.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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