Rabusertib (LY2603618)

For research use only.

Catalog No.S2626 Synonyms: IC-83

37 publications

Rabusertib (LY2603618) Chemical Structure

Molecular Weight(MW): 436.3

Rabusertib (LY2603618) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated.

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Selleck's Rabusertib (LY2603618) has been cited by 37 publications

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Biological Activity

Description Rabusertib (LY2603618) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated.
Chk1 [1]
(Cell-free assay)
7 nM
In vitro

Chk1 is an ATP-dependent serine-threonine kinase and a key component in the DNA replication-monitoring checkpoint system activated by double-stranded breaks (DSBs). Chk1 contributes to all currently defined cell cycle checkpoints, including G1/S, intra-S-phase, G2/M, and the mitotic spindle checkpoint. By inhibiting the activity of chk1, LY2603618 prevents the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. However, preclinical data involving LY2603618 has not been published until now. [1] Inhibition of Chk1 is predicted to enhance the effects of antimetabolites, such as gemcitabine. [2] LY2603618 treatment impairs DNA synthesis, increases DNA damage (via mitotic defects), induces apoptosis, and has synergistic activity with pemetrexed, especially in p53 mutant tumor cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT474 MVHLbY5ie2ViYYPzZZk> M3uyR|Eh|ryP Ml3VSG1UVw>? NE\OXm9qdmirYnn0d{BRNUOKS{GgcIV3\Wy| MkHiNlM6OTd|N{i=
MCF7 Mo\mT4lv[XOnIHHzd4F6 M2i1Z|Eh|ryP MUHEUXNQ NYXH[|QycW6qaXLpeJMhWC2FSFuxJIxmfmWucx?= M3TWbVI{QTF5M{e4
Hela NV33NY9RU2mwYYPlJIF{e2G7 NUDRb2N6OzNyMDDuUS=> MnTzSG1UVw>? NIrrU4tqdmirYnn0d{BEcGtzIHHjeIl3cXS7 M2HuZVI1OTF2MUK0
Calu6 NXi4XoZsU2mwYYPlJIF{e2G7 Ml;NN|MxOCCwTR?= NW\hNFZrTE2VTx?= MoLHbY5pcWKrdIOgR4hsOSCjY4Tpeol1gQ>? NVHo[4pVOjRzMUSxNlQ>
A549 NHW5TpFHfW6ldHnvckBie3OjeR?= M{fJOJ4yOCEQvF2= MXPEUXNQ NGP1Vo5qdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MWWyOFkzQDJyNR?=
H1299 NXztUmlJTnWwY4Tpc44h[XO|YYm= M2[2Xp4yOCEQvF2= NGezdGlFVVOR Mn3jbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NGS3[|YzPDl{OEKwOS=>
A549 M2m1[GZ2dmO2aX;uJIF{e2G7 NY\XOmFJhjJyIN88US=> M2raVGROW09? NGH1e2hi[3SrdnH0[ZMhTE6DIHThcYFo\SC|ZX7zc5Ihc2mwYYPldy=> M4XyeFI1QTJ6MkC1
H1299 NWHObVIyTnWwY4Tpc44h[XO|YYm= M1vJcp4zOCEQvF2= NHnRfHBFVVOR Ml[3ZYN1cX[jdHXzJGRPSSCmYX3h[4Uhe2Wwc3;yJItqdmG|ZYO= NX;aRXhpOjR7MkiyNFU>
A549 MmP1RZBweHSxc3nzJIF{e2G7 MXH+NlAh|ryP NX[3WFZmTE2VTx?= NFXoT4RqdmS3Y3XzJIFxd3C2b4Ppdy=> MkWxNlQ6Ojh{MEW=
H1299 NIf3Z|FCeG:ydH;zbZMh[XO|YYm= NUj5fJMxhjJyIN88US=> M4jWNGROW09? MY\pcoR2[2W|IHHwc5B1d3Orcx?= M1XmRlI1QTJ6MkC1
A549 MVjDfZRwgGmlaYT5JIF{e2G7 MnfkglIxKM7:TR?= NEXh[nJFVVOR MoTubY5lfWOnczDheZRweGijZ4m= NUT1OoZQOjR7MkiyNFU>
H1299 MXPDfZRwgGmlaYT5JIF{e2G7 NYnWZpRRhjJyIN88US=> M1P6OmROW09? NWW5W5ZucW6mdXPld{BifXSxcHjh[5k> MnS5NlQ6Ojh{MEW=
A549 Mn3QSpVv[3Srb36gZZN{[Xl? NE\Vbol,OjBizszN MUfEUXNQ NU\OT5NScW6lcnXhd4V{KEqQSzDhcoQheDN6IF3BVGsheGixc4Doc5J6dGG2aX;u NV2yenUyOjR7MkiyNFU>
H1299 MmrRSpVv[3Srb36gZZN{[Xl? M1W0[p4zOCEQvF2= MnvJSG1UVw>? NXjrR4hqcW6lcnXhd4V{KEqQSzDhcoQheDN6IF3BVGsheGixc4Doc5J6dGG2aX;u NFnMc2wzPDl{OEKwOS=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-Chk1 / Chk1 / CDC25A ; 

PubMed: 29326282     

CHK1 inhibition was monitored by measuring levels of CHK1 p-S345 and CDC25A by western blots. Cells were treated with various concentrations of LY2603618 for 8 h. 

PARP / CF-PARP / p-CDC25C / p-CDK1 / p-CDK2 ; 

PubMed: 25458954     

BxPC-3 cells were treated with vehicle control, MK-1775 (MK), LY2603618 (LY) or MK-1775 plus LY2603618 for 48 h. Protein extracts were subjected to Western blotting and probed with anti-PARP, -p-CHK1, -CHK1, -p-CDC25C, -p-CDK1, -CDK1, -p-CDK2, -CDK2, -γH2AX, or -β-actin antibody. 

29326282 25458954
Growth inhibition assay
Cell viability; 

PubMed: 29326282     

MTT assay following CHK1 inhibition by LY2603618 in BC cells with higher RNF126 expression vs. BC cells with lower RNF126 expression. Cells were treated with various concentrations of LY2603618 for 72 h. n=3. (Two-way ANOVA, P(BT474 VS. MDA-MB-231)<0.001; P(BT474 VS. MDA-MB-468)<0.001; P(ZR751 VS. MDA-MB-231)<0.001; P(ZR751 VS. MDA-MB-468)<0.001).

In vivo In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed. [3]


Cell Research:


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  • Cell lines: A549 and H1299 cell
  • Concentrations: 5 or 10 μM
  • Incubation Time: 24 h
  • Method:

    Cells were treated with LY2603618 and DMSO as a control. After trypsinization, cells were fixed in 70 % ethanol at 4 C overnight. The cells were washed twice with PBS and incubated for 30 min in the dark in PBS containing propidium iodide (PI) and RNase A. Stained cells were analyzed by a FACScan flow cytometry and CellQuest analysis software.

    (Only for Reference)

Solubility (25°C)

In vitro DMSO 13 mg/mL (29.79 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG400+0.5% Tween80+5% Propylene glycol
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 436.3


CAS No. 911222-45-2
Storage powder
in solvent
Synonyms IC-83
Smiles CC1=NC=C(NC(=O)NC2=C(OCC3CNCCO3)C=C(C)C(=C2)Br)N=C1

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01341457 Completed Drug: LY2603618|Drug: Gemcitabine Solid Tumors Eli Lilly and Company May 2011 Phase 1
NCT01296568 Completed Drug: LY2603618|Drug: Pemetrexed|Drug: Gemcitabine Advanced Cancer Eli Lilly and Company February 2011 Phase 1
NCT01139775 Completed Drug: Pemetrexed|Drug: Cisplatin|Drug: LY2603618 Non Small Cell Lung Cancer Eli Lilly and Company February 2011 Phase 1|Phase 2
NCT00988858 Completed Drug: LY2603618|Drug: Pemetrexed Non Small Cell Lung Cancer Eli Lilly and Company November 2009 Phase 2
NCT00839332 Completed Drug: LY2603618|Drug: Gemcitabine Pancreatic Neoplasms Eli Lilly and Company February 2009 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID