MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Elimusertib hydrochloride

CAS No. :

MCE 站：Elimusertib hydrochloride

产品活性：Elimusertib (BAY 1895344) hydrochloride 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 hydrochloride 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 hydrochloride potently inhibits the proliferation of a broad spectrum of human tumor cell lines with a median IC₅₀ of 78 nM.
Elimusertib hydrochloride potently suppresses hydroxyurea-induced H2AX phosphorylation (IC₅₀: 36 nM).
Elimusertib hydrochloride shows good selectivity against mTOR (ratio of IC₅₀ values: mTOR/ATR 61).
Elimusertib hydrochloride reveals high selectivity against other related kinases, such as DNA-PK (IC₅₀: 332 nM), ATM (IC₅₀: 1420 nM), and PI3K (IC₅₀: 3270 nM).
Elimusertib hydrochloride 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 hydrochloride 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 hydrochloride (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 hydrochloride (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 hydrochloride exhibits moderate oral bioavailability (rat 87%, dog 51%) following oral administration (rat and dog 0.6-1 mg/kg).
Elimusertib hydrochloride 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  |  AZ20  |  CGK733  |  AZ32  |  CP-466722  |  ETP-46464  |  Garcinone C  |  Ro 90-7501  |  NU6027

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。