Rabusertib (Synonyms: LY2603618; IC-83)

Name: Rabusertib
Brand: MedChemExpress
SKU: HY-14720
Rating: 5.0 (21 reviews)

製品番号: HY-14720 純度: 99.98%: Data Sheet SDS COA 取扱説明書
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Technical Support

Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC₅₀ of 7 nM.

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CAS 番号 : 911222-45-2

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 52	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 52	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$48	在庫あり	Estimated Time of Arrival: December 31
10 mg	$80	在庫あり	Estimated Time of Arrival: December 31
25 mg	$170	在庫あり	Estimated Time of Arrival: December 31
50 mg	$270	在庫あり	Estimated Time of Arrival: December 31
100 mg	$400	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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カスタマーレビュー

Based on 21 publication(s) in Google Scholar

顧客検証

Bio/Physico-chemical Assay

Cell Proliferation/Viability Assay

Cell Imaging/Staining

: Rabusertib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 Mar 26;17(1):375.; pH3 (S10) levels were markedly reduced after 8 h of Rabusertib (20 μM) treatment, indicating a defect in mitotic entry similar to that observed upon CHK1 depletion.

: Rabusertib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 Mar 26;17(1):375.; Cell viability analysis (CellTiter-Glo assay) of parental 293A cells treated with increasing concentrations of the CHK1 inhibitor rabusertib for 24 hours to determine the working concentration.

: Rabusertib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2023 Jan 30;15(3):850.; Prexasertib (5 µM; 24 h) decreases CHK1 expression in HepG2 and Huh-7 cells and increases γ-H2AX level.

: Rabusertib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2021 Jan 20;13(577):eaba7401. [Abstract]; The three CHK1/2 inhibitors (AZD7762, MK8776 and Rabusertib (LY2606368)) and the CHK1-specific inhibitor (LY2603618) exhibited consistent synergistic action with the DNA-damaging agents.

: Rabusertib purchased from MedChemExpress. Usage Cited in: Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]; Quantification of nuclear intensity values in gated S-phase cells. Boxplots show median and 25th/75th percentiles. D:DMSO, A8:AZD8055, O:omipalisib, T2:Torin2, AZ:AZ20, R:Rabusertib.

: Rabusertib purchased from MedChemExpress. Usage Cited in: Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]; 72h dose-response curves. "Mixture" denotes equimolar concentrations of AZD8055/Rabusertib; "analogs" indicate Torin2 chemical analogs.

: Rabusertib purchased from MedChemExpress. Usage Cited in: Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]; Live-cell imaging of cells treated with sub-GR_max doses of AZD8055 and/or the Chk1 inhibitor Rabusertib. Doses for each cell line (AZD8055, Rabusertib): Hs 578T (0.1 μM, 0.5 μM); HCC70 (0.032 μM, 0.32 μM); HCC1806 (0.320 μM, 0.32 μM).

Checkpoint Kinase (Chk) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Chk1 Chk2 BUBR1

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC₅₀ of 7 nM.

IC₅₀ & Target^[1]

Chk1

7 nM (IC₅₀)

Chk2

12000 nM (IC₅₀)

PDK1

893 nM (IC₅₀)

CAMK2

1550 nM (IC₅₀)

VEGFR3

2128 nM (IC₅₀)

MET

2200 nM (IC₅₀)

JNK1

4930 nM (IC₅₀)

RSK2

5700 nM (IC₅₀)

NTRK1

12000 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	28.1 μM Compound: LY2603618	Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by automated patch clamp assay Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by automated patch clamp assay	[PMID: 30986571]
JeKo-1	IC₅₀	0.92 μM Compound: LY2603618	Inhibition of human JeKo1 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay Inhibition of human JeKo1 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay	[PMID: 30986571]
MV4-11	IC₅₀	0.869 μM Compound: LY2603618	Inhibition of human MV411 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay Inhibition of human MV411 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay	[PMID: 30986571]
Ramos	IC₅₀	0.539 μM Compound: LY2603618	Inhibition of human Ramos cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay Inhibition of human Ramos cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay	[PMID: 30986571]
RPMI-8226	IC₅₀	4.381 μM Compound: LY2603618	Inhibition of human RPMI8226 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay Inhibition of human RPMI8226 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay	[PMID: 30986571]
Z-138	IC₅₀	0.368 μM Compound: LY2603618	Inhibition of human Z138 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay Inhibition of human Z138 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay	[PMID: 30986571]

体外実験

Rabusertib (LY2603618) is a highly effective inhibitor of multiple aspects of Chk1 biology. Rabusertib (LY2603618) is tested against a panel of 51 diverse protein kinases in vitro. With an IC₅₀ of 7 nM for Chk1, Rabusertib (LY2603618) is approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated (PDK1, IC₅₀=893 nM, others >1000 nM). Rabusertib (LY2603618) effectively reduced Chk1 autophosphorylation with an EC₅₀ of 430 nM. Inhibition of Chk1 by Rabusertib (LY2603618) also effectively abrogated the G₂/M DNA damage checkpoint in cells treated with DNA damaging agents. Treatment of cells with Rabusertib (LY2603618) produced a cellular phenotype similar to that reported for depletion of Chk1 by RNAi. Inhibition of intracellular Chk1 by Rabusertib (LY2603618) results in impaired DNA synthesis, elevated H2A.X phosphorylation indicative of DNA damage and premature entry into mitosis^[1]. Treatments of the SK-N-BE(2) cells with variable concentrations of Rabusertib (LY2603618) results in dose-dependent inhibition of cell growth determined by MTT assays with an IC₅₀ of 10.81 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Mice bearing Calu-6 xenografts are treated with 150 mg/kg (IP) Gemcitabine and a single simultaneous 200 mg/kg oral dose of Rabusertib (LY2603618). 200 mg/kg of Rabusertib (LY2603618) is sufficient to inhibit 85 % of Chk1 autophosphorylation in vivo at 2 h. Rabusertib (LY2603618) effectively reduces Gemcitabine-induced phosphorylation on Tlk serine 695 as well, supporting the cited report with a selective chemical inhibitor of Chk1^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

分子量

436.30

分子式

C₁₈H₂₂BrN₅O₃

CAS 番号

911222-45-2

Appearance

Solid

Color

Off-white to yellow

SMILES

BrC(C=C1NC(NC2=NC=C(N=C2)C)=O)=C(C=C1OC[C@H]3OCCNC3)C

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 31.25 mg/mL (71.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2920 mL	11.4600 mL	22.9200 mL
5 mM	0.4584 mL	2.2920 mL	4.5840 mL
10 mM	0.2292 mL	1.1460 mL	2.2920 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (22.92 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.98%

Select Batch:

データシート (281 KB) SDS (393 KB)

COA (250 KB) HNMR (488 KB) RP-HPLC (247 KB) LCMS (130 KB)

取扱説明書 (2659 KB)

参考文献

[1]. King C, et al. Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor. Invest New Drugs. 2014 Apr;32(2):213-26. [Content Brief]

[2]. Wang G, et al. Panobinostat synergistically enhances the cytotoxic effects of cisplatin, doxorubicin or etoposide on high-risk neuroblastoma cells. PLoS One. 2013 Sep 30;8(9):e76662. [Content Brief]

細胞実験 ^[1]	Cells are plated at 2.5×10³ per well, on 96-well tissue culture plates and incubated for one cell doubling (18-24 h). Gemcitabine dilutions are set up by half-log steps across a final concentration range of 1-1000 nM. Rabusertib (LY2603618) is prepared by dilutions in DMSO to 5000× final concentration, and then diluted 1000-fold into medium to generate 5× stocks for addition to wells. Approximately 24 h after Gemcitabine addition, Rabusertib (LY2603618) is added. Each combination is done in triplicate. After a period of two cell doublings following Rabusertib (LY2603618) addition, MTS/PMS reagent is added to each well according to the manufacturer’s instructions. Absorbance is read on a Spectra Max 250 spectrophotometer at 490 nm and the data analyzed with GraphPad Prism 4.0. Dose-response curves are fit by non-linear regression, with bottom fits constrained to 0 % inhibition^[1]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[1]	Mice^[1] Female Harlan athymic nude mice (26-28 g) are used for these studies. Tumor growth is initiated by subcutaneous injection of 1×10⁶ Calu-6 cells in a 1:1 mixture of serum-free growth medium and Matrigel in the rear flank of each subject animal. When tumor volumes reach approximately 150 mm³ in size, the animals are randomized by tumor size and body weight, and placed into their respective treatment groups. Each animal receives 2 injections, one of either saline vehicle or 150 mg/kg Gemcitabine administered by intraperitoneal injection in a volume of 200 μL, and the other being the Captisol vehicle or LY2603618 administered orally in a volume of 200 μL. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. King C, et al. Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor. Invest New Drugs. 2014 Apr;32(2):213-26. [Content Brief] [2]. Wang G, et al. Panobinostat synergistically enhances the cytotoxic effects of cisplatin, doxorubicin or etoposide on high-risk neuroblastoma cells. PLoS One. 2013 Sep 30;8(9):e76662. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2920 mL	11.4600 mL	22.9200 mL	57.3000 mL
	5 mM	0.4584 mL	2.2920 mL	4.5840 mL	11.4600 mL
	10 mM	0.2292 mL	1.1460 mL	2.2920 mL	5.7300 mL
	15 mM	0.1528 mL	0.7640 mL	1.5280 mL	3.8200 mL
	20 mM	0.1146 mL	0.5730 mL	1.1460 mL	2.8650 mL
	25 mM	0.0917 mL	0.4584 mL	0.9168 mL	2.2920 mL
	30 mM	0.0764 mL	0.3820 mL	0.7640 mL	1.9100 mL
	40 mM	0.0573 mL	0.2865 mL	0.5730 mL	1.4325 mL
	50 mM	0.0458 mL	0.2292 mL	0.4584 mL	1.1460 mL
	60 mM	0.0382 mL	0.1910 mL	0.3820 mL	0.9550 mL

Rabusertib Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rabusertib911222-45-2LY2603618 IC-83LY 2603618LY-2603618IC83IC 83IC-83Checkpoint Kinase (Chk)AutophagyInhibitorinhibitorinhibit

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Rabusertib (Synonyms: LY2603618; IC-83)

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Molarity Calculator

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Complete Stock Solution Preparation Table

Rabusertib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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Rabusertib (Synonyms: LY2603618; IC-83)

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Rabusertib 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Checkpoint Kinase (Chk) アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Rabusertib 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Rabusertib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

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