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Elimusertib
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Elimusertib图片
CAS NO: 1876467-74-1
包装与价格：
包装 价格(元)
10 mM * 1 mL in DMSO 电议
5mg 电议
10mg 电议
25mg 电议
50mg 电议
100mg 电议
200mg 电议
500mg 电议

半岛bd体育手机客户端 名称
BAY 1895344
半岛bd体育手机客户端 介绍
Elimusertib (BAY-1895344) 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 可用于实体瘤和淋巴瘤的研究。
生物活性

Elimusertib (BAY-1895344) is a potent, orally active and selectiveATRinhibitor with anIC50of 7 nM. Elimusertib has anti-tumor activity[1][2]. Elimusertib can be used for the research of solid tumors and lymphomas[3].
IC50& Target

ATR

7 nM (IC50)
体外研究
(In Vitro)

Elimusertib potently inhibits the proliferation of a broad spectrum of human tumor cell lines with a median IC50of 78 nM[1].
Elimusertib potently suppresses hydroxyurea-induced H2AX phosphorylation (IC50: 36 nM)[1].
Elimusertib shows good selectivity against mTOR (ratio of IC50values: mTOR/ATR 61)[3].
Elimusertib 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 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].
体内研究
(In Vivo)

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

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

375.43
性状

Solid
Formula

C20H21N7O
CAS 号

1876467-74-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:

DMSO : 5.4 mg/mL(14.38 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.6636 mL 13.3181 mL 26.6361 mL
5 mM 0.5327 mL 2.6636 mL 5.3272 mL
10 mM 0.2664 mL 1.3318 mL 2.6636 mL
*

请根据半岛bd体育手机客户端 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半岛bd体育手机客户端 失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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： 0.5%CMC-Na/saline water

    Solubility: 4 mg/mL (10.65 mM); Suspended solution; Need ultrasonic and adjust pH to 3 with HCl

  • 2.

    请依序添加每种溶剂： 10% DMSO90% (20%SBE-β-CDin saline)

    Solubility: 1.09 mg/mL (2.90 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.09 mg/mL (2.90 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 10.9 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 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
  • 3.

    请依序添加每种溶剂： 10% DMSO40%PEG3005%Tween-8045% saline

    Solubility: 0.89 mg/mL (2.37 mM); Suspended solution; Need ultrasonic

    此方案可获得 0.89 mg/mL (2.37 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 8.9 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
* 以上所有助溶剂都可在本网站选购。
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