Rabusertib
Based on 24 publication(s) in Google Scholar
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.
- Purity: 99.98%
- CAS No.: 911222-45-2
- Formula: C18H22BrN5O3
- Molecular Weight:436.30
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Rabusertib
More- Sci Transl Med. 2021 Jan 20;13(577):eaba7401. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Nucleic Acids Res. 2021 Apr 6;49(6):3322-3337. [Abstract]
- J Immunother Cancer. 2026 Mar 25;14(3):e012426. [Abstract]
- Cancer Lett. 2026 Feb 4;642:218300.
- Cancer Lett. 2026 Apr 1:642:218300. [Abstract]
- Cell Death Dis. 2026 Mar 26;17(1):375. [Abstract]
- Proc Natl Acad Sci U S A. 2026 Feb 10;123(6):e2524246123. [Abstract]
- Dev Cell. 2022 Mar 14;57(5):638-653.e5. [Abstract]
- Int J Biol Macromol. 2026 Mar:351:151067. [Abstract]
- Cell Syst. 2020 Jan 22;10(1):66-81.e11. [Abstract]
- Oncogene. 2026 Jun 10. [Abstract]
- Breast Cancer Res. 2023 May 5;25(1):51. [Abstract]
- Cell Prolif. 2020 Oct;53(10):e12895. [Abstract]
- Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]
- Eur J Pharmacol. 2025 Sep 15:1003:177942. [Abstract]
- Cancer Biol Ther. 2022 Dec 31;23(1):69-82. [Abstract]
- Cancers (Basel). 2023 Jan 30;15(3):850. [Abstract]
- bioRxiv. 2026 Apr 29.
- University of Califomia San Francisco. 2026.
- bioRxiv. 2025 Nov 7.
- bioRxiv. 2025 April 26.
- bioRxiv. 2025 February 22.
- Research Square Preprint. 2024 Nov 06.
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
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WB
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
28.1 μM
Compound: LY2603618
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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
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[PMID: 30986571] |
| JeKo-1 | IC50 |
0.92 μM
Compound: LY2603618
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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
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[PMID: 30986571] |
| MV4-11 | IC50 |
0.869 μM
Compound: LY2603618
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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
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[PMID: 30986571] |
| Ramos | IC50 |
0.539 μM
Compound: LY2603618
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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
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[PMID: 30986571] |
| RPMI-8226 | IC50 |
4.381 μM
Compound: LY2603618
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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
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[PMID: 30986571] |
| Z-138 | IC50 |
0.368 μM
Compound: LY2603618
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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
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[PMID: 30986571] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 911222-45-2
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Appearance Solid
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Molecular Weight 436.30
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Formula C18H22BrN5O3
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Color Off-white to yellow
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SMILES
BrC(C=C1NC(NC2=NC=C(N=C2)C)=O)=C(C=C1OC[C@H]3OCCNC3)C
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Synonyms
LY2603618; IC-83
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (24)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
Small-molecule screen reveals synergy of cell cycle checkpoint kinase inhibitors with DNA-damaging chemotherapies in medulloblastoma. [Abstract]2021 Jan 20;13(577):eaba7401. PMID: 33472956
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.
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Nucleic Acids Res
2021 Apr 6;49(6):3322-3337. PMID: 33704464 -
J Immunother Cancer
Telmisartan increases olaparib efficacy in homologous recombination proficient tumors by augmenting type I interferon production. [Abstract]2026 Mar 25;14(3):e012426. PMID: 41881499 -
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Cancer Lett
2026 Apr 1:642:218300. PMID: 41651400 -
Cell Death Dis
2026 Mar 26;17(1):375. PMID: 41888112
Rabusertib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 Mar 26;17(1):375. [Abstract]
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. [Abstract]
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.
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Proc Natl Acad Sci U S A
2026 Feb 10;123(6):e2524246123. PMID: 41628322 -
Dev Cell
2022 Mar 14;57(5):638-653.e5. PMID: 35245445 -
Int J Biol Macromol
Inhibition of replication factor C4-induced DNA damage repair reverses the chemoresistance of glioblastoma to temozolomide and reveals the synthetic lethal effect of combined targeting of checkpoint kinase 1. [Abstract]2026 Mar:351:151067. PMID: 41747987 -
Cell Syst
Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]2020 Jan 22;10(1):66-81.e11. PMID: 31812693
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-GRmax 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).
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Oncogene
DNA replication stress and translational repression converge to drive CDK1- and caspase-dependent apoptosis in Ewing sarcoma. [Abstract]2026 Jun 10. PMID: 42270776 -
Breast Cancer Res
Systematic screening identifies ABCG2 as critical factor underlying synergy of kinase inhibitors with transcriptional CDK inhibitors. [Abstract]2023 May 5;25(1):51. PMID: 37147730 -
Cell Prolif
CHK1 monitors spindle assembly checkpoint and DNA damage repair during the first cleavage of mouse early embryos. [Abstract]2020 Oct;53(10):e12895. PMID: 32914523 -
Mol Cancer Ther
AMT-562, a Novel HER3-targeting Antibody-Drug Conjugate, Demonstrates a Potential to Broaden Therapeutic Opportunities for HER3-expressing Tumors. [Abstract]2023 Sep 5;22(9):1013-1027. PMID: 37302522 -
Eur J Pharmacol
VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]2025 Sep 15:1003:177942. PMID: 40651787 -
Cancer Biol Ther
Repeated treatments of Capan-1 cells with PARP1 and Chk1 inhibitors promote drug resistance, migration and invasion. [Abstract]2022 Dec 31;23(1):69-82. PMID: 35000525 -
Cancers (Basel)
Inhibition of Checkpoint Kinase 1 (CHK1) Upregulates Interferon Regulatory Factor 1 (IRF1) to Promote Apoptosis and Activate Anti-Tumor Immunity via MICA in Hepatocellular Carcinoma (HCC). [Abstract]2023 Jan 30;15(3):850. PMID: 36765808
Rabusertib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2023 Jan 30;15(3):850. [Abstract]
Prexasertib (5 µM; 24 h) decreases CHK1 expression in HepG2 and Huh-7 cells and increases γ-H2AX level.
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (22.92 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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) has not independently confirmed the accuracy of these methods. They are for reference only.
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) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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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]
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.
| 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 |
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