Elimusertib hydrochloride(Synonyms: BAY 1895344 hydrochloride)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Elimusertib hydrochloride (Synonyms: BAY 1895344 hydrochloride) 纯度: 99.84%

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 hydrochloride(Synonyms: BAY 1895344 hydrochloride)

Elimusertib hydrochloride Chemical Structure

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10 mM * 1 mL in DMSO ¥1210 In-stock
2 mg ¥550 In-stock
5 mg ¥1100 In-stock
10 mg ¥1760 In-stock
25 mg ¥3200 In-stock
50 mg ¥5200 In-stock
100 mg ¥8700 In-stock
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生物活性

Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC50 of 7 nM. Elimusertib hydrochloride has anti-tumor activity[1][2]. Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas[3].

IC50 & Target[1]

ATR

7 nM (IC50)

体外研究
(In Vitro)

Elimusertib hydrochloride potently inhibits the proliferation of a broad spectrum of human tumor cell lines with a median IC50 of 78 nM[1].
Elimusertib hydrochloride potently suppresses hydroxyurea-induced H2AX phosphorylation (IC50: 36 nM)[1].
Elimusertib hydrochloride shows good selectivity against mTOR (ratio of IC50 values: mTOR/ATR 61)[3].
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)[3].
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)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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[2].
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[3].
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[3].
Elimusertib hydrochloride exhibits moderate oral bioavailability (rat 87%, dog 51%) following oral administration (rat and dog 0.6-1 mg/kg)[3].
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)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C.B-17 SCID mice, SU-DHL-8 GCB-DLBCL xenograft model[3]
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[3]
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[3]
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).

Clinical Trial

分子量

411.89

Formula

C20H22ClN7O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4278 mL 12.1392 mL 24.2783 mL
5 mM 0.4856 mL 2.4278 mL 4.8557 mL
10 mM 0.2428 mL 1.2139 mL 2.4278 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (242.78 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.05 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.05 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.05 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.05 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.05 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.05 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [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 Research. July 2017 Volume 77, Issue 13 Supplement.

    [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 2017 Volume 77, Issue 13 Supplement

    [3]. Ulrich Lücking, et al. Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models. J Med Chem. 2020 Jul 9;63(13):7293-7325.

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