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。

Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC 50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity. Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas.

Solid

ATR 7 nM (IC50)

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).

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

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Ulrich T. Luecking, et al. Abstract 983: Identification of potent, highly selective and orally available ATR inhibitor BAY 1895344 with favorable PK properties and promising efficacy in monotherapy and combination in preclinical tumor models. Cancer Resea
[2]. Antje Margret Wengner, et al. Abstract 836: ATR inhibitor BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride in preclinical tumor models. Cancer Research. July

In Vitro: DMSO : 50 mg/mL (121.39 mM; Need ultrasonic)H₂O : 50 mg/mL (121.39 mM; Need ultrasonic)配制储备液