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Elimusertib
本产品不向个人销售,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

产品名称
BAY 1895344
产品介绍
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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM2.6636 mL13.3181 mL26.6361 mL
5 mM0.5327 mL2.6636 mL5.3272 mL
10 mM0.2664 mL1.3318 mL2.6636 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℃, 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% DMSO    90% (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% DMSO    40%PEG300   5%Tween-80   45% 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。