Elimusertib - CAS:1876467-74-1

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Elimusertib (Synonyms:BAY 1895344)

目录号 : KM6207 CAS No. : 1876467-74-1 纯度 : 98%

Data Sheet 产品使用指南

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。

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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

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

体外研究

Elimusertib potently inhibits the proliferation of a broad spectrum of human tumor cell lines with a median IC₅₀ of 78 nM.
Elimusertib potently suppresses hydroxyurea-induced H2AX phosphorylation (IC₅₀: 36 nM).
Elimusertib shows good selectivity against mTOR (ratio of IC₅₀ values: mTOR/ATR 61).
Elimusertib reveals high selectivity against other related kinases, such as DNA-PK (IC₅₀: 332 nM), ATM (IC₅₀: 1420 nM), and PI3K (IC₅₀: 3270 nM).
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).

体内研究

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

Animal Model:	Female C.B-17 SCID mice, SU-DHL-8 GCB-DLBCL xenograft model
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
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%), T_1/2 (1.3 h).

Animal Model:	Female beagle dogs
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%), T_1/2 (1.0 h).

分子式

C₂₀H₂₂ClN₇O

分子量

375.43

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。-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： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2.

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。