| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| E409275-1ml |
1ml |
现货  |
|
| 别名 | Elimusertib(BAY-1895344)盐酸盐 |
|---|---|
| 英文别名 | BAY-1895344 HCl | 2-[(3R)-3-methyl-4-morpholinyl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-3-yl)-1,7-Naphthyridine hydrochloride |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Elimusertib (BAY-1895344) hydrochloride |
| 生化机理 | Elimusertib（BAY-1895344）盐酸盐是一种强效、高选择性、口服型 ATR 抑制剂，IC50 为 7 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 丝氨酸蛋白激酶 ATR 抑制剂 |
| 产品介绍 |
Information Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally availableATRinhibitor with an IC50 of 7 nM. In vitro, BAY 1895344 is shown to be a very potent and highly selective ATR inhibitor (IC50 = 7 nM), which potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC50 = 78 nM). In cellular mechanistic assays BAY 1895344 potently inhibits hydroxyurea-induced H2AX phosphorylation (IC50 = 36 nM). In vivo BAY 1895344 reveals significantly improved aqueous solubility, bioavailability across species and no activity in the hERG patch-clamp assay. It also demonstrates very promising efficacy in monotherapy in DNA damage deficient tumor models as well as combination treatment with DNA damage inducing therapies. BAY 1895344 exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models of different indications that are characterized by DDR deficiencies, inducing stable disease in ovarian and colorectal cancer or even complete tumor remission in mantle cell lymphoma models. cell lines： Concentrations： Incubation Time： Powder Purity:≥98% |
| IC50 | ATR, IC50: 7 nM |
|---|
| Canonical SMILES | Cl.CC1COCCN1C2=CC(=C3C=CN=C(C4=CC=N[NH]4)C3=N2)C5=CC=N[N]5C |
|---|---|
| 分子量 | 411.89 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 56 mg/mL (201.22 mM); Water: 56 mg/mL (201.22 mM); Ethanol: Insoluble; |
|---|
| Concentration(Compounding value) | 9-11(mmol/L) |
|---|---|
| Record the entire process by video | Conform |
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