Rabusertib (Synonyms: LY2603618; IC-83)

Name: Rabusertib
Brand: MedChemExpress
SKU: HY-14720
Rating: 5.0 (13 reviews)

Cat. No.: HY-14720 Purity: 99.99%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

Rabusertib Chemical Structure

CAS No. : 911222-45-2

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Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 53	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 53	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 48	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 73	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 146	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 330	In-stock	Estimated Time of Arrival: December 31
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Based on 13 publication(s) in Google Scholar

12 Publications Citing Use of MCE Rabusertib

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

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Chk1 Chk2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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]

In Vitro

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.

In Vivo

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.

Clinical Trial

Molecular Weight

436.30

Formula

C₁₈H₂₂BrN₅O₃

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.

Purity & Documentation

Purity: 99.99%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (250 KB) HNMR (527 KB) RP-HPLC (258 KB) LCMS (130 KB)

Handling Instructions (2659 KB)

References

[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]

Cell Assay ^[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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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

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)

Customer Review

Rabusertib Related Antibodies

12 Publications Citing Use of MCE Rabusertib

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Complete Stock Solution Preparation Table

Rabusertib Related Classifications

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