Rabusertib (LY2603618)

Catalog No.S2626 Synonyms: IC-83

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.

Size Price Stock Quantity  
In DMSO USD 300 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 30 Publications

Purity & Quality Control

Choose Selective Chk Inhibitors

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.
Targets
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 NYXybZFqU2mwYYPlJIF{e2G7 NU\OR5JDOSEQvF2= NE[2PVVFVVOR MlrZbY5pcWKrdIOgVE1EUEtzIHzleoVtew>? MVGyN|kyPzN5OB?=
MCF7 NFrjXpJMcW6jc3WgZZN{[Xl? M3nOT|Eh|ryP MmHoSG1UVw>? NY\JS3lEcW6qaXLpeJMhWC2FSFuxJIxmfmWucx?= MUKyN|kyPzN5OB?=
Hela NVqxNVdDU2mwYYPlJIF{e2G7 MlzGN|MxOCCwTR?= NETJVJBFVVOR M2XG[IlvcGmkaYTzJGNpczFiYXP0bZZqfHl? NFGxc4UzPDFzNEGyOC=>
Calu6 NFzGZVFMcW6jc3WgZZN{[Xl? MlrSN|MxOCCwTR?= Mni5SG1UVw>? M4W4[IlvcGmkaYTzJGNpczFiYXP0bZZqfHl? NFvv[lAzPDFzNEGyOC=>
A549 MnHFSpVv[3Srb36gZZN{[Xl? MkPDglExKM7:TR?= NYrWXZhRTE2VTx?= NF\ESVVqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NIHvbGkzPDl{OEKwOS=>
H1299 MmfCSpVv[3Srb36gZZN{[Xl? M2nRcZ4yOCEQvF2= M17j[WROW09? M2Cxcolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NUXoU2dzOjR7MkiyNFU>
A549 MY\GeY5kfGmxbjDhd5NigQ>? MkTNglIxKM7:TR?= NELJeFFFVVOR NV20SFY2[WO2aY\heIV{KESQQTDkZY1i\2Vic3Xud49zKGurbnHz[ZM> M{DubFI1QTJ6MkC1
H1299 MVXGeY5kfGmxbjDhd5NigQ>? MnjaglIxKM7:TR?= NHXnRZpFVVOR M1T4U4FkfGm4YYTld{BFVkFiZHHtZYdmKHOnboPvdkBscW6jc3Xz M3XRRVI1QTJ6MkC1
A549 MXzBdI9xfG:|aYOgZZN{[Xl? MmjEglIxKM7:TR?= Mm[wSG1UVw>? NGrU[41qdmS3Y3XzJIFxd3C2b4Ppdy=> NIn3OXUzPDl{OEKwOS=>
H1299 NYm4dmY1SXCxcITvd4l{KGG|c3H5 NHXtOnJ,OjBizszN M{HLNGROW09? NGjIPHVqdmS3Y3XzJIFxd3C2b4Ppdy=> M4XoTFI1QTJ6MkC1
A549 M3TFN2N6fG:6aXPpeJkh[XO|YYm= M{jJd54zOCEQvF2= M2jmZmROW09? MkTJbY5lfWOnczDheZRweGijZ4m= NWftTY42OjR7MkiyNFU>
H1299 NVj6Slc6S3m2b4jpZ4l1gSCjc4PhfS=> MmPyglIxKM7:TR?= NGXw[G5FVVOR NHLJcpJqdmS3Y3XzJIF2fG:yaHHnfS=> M33PfFI1QTJ6MkC1
A549 MYTGeY5kfGmxbjDhd5NigQ>? MmroglIxKM7:TR?= NEfZPVNFVVOR M3nSNolv[3KnYYPld{BLVktiYX7kJJA{QCCPQWDLJJBpd3OyaH;yfYxifGmxbh?= M4PaZ|I1QTJ6MkC1
H1299 MUnGeY5kfGmxbjDhd5NigQ>? NWnBbnpvhjJyIN88US=> MWTEUXNQ M2\TR4lv[3KnYYPld{BLVktiYX7kJJA{QCCPQWDLJJBpd3OyaH;yfYxifGmxbh?= NGDCcXczPDl{OEKwOS=>

... Click to View More Cell Line Experimental Data

Assay
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).

29326282
In vivo In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed. [3]

Protocol

Cell Research:

[4]

- Collapse
  • 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.
30mg/mL

* 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
Formula

C18H22BrN5O3

CAS No. 911222-45-2
Storage powder
in solvent
Synonyms IC-83

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Chk Signaling Pathway Map

Chk Inhibitors with Unique Features

Related Chk Products

Tags: buy Rabusertib (LY2603618) | Rabusertib (LY2603618) supplier | purchase Rabusertib (LY2603618) | Rabusertib (LY2603618) cost | Rabusertib (LY2603618) manufacturer | order Rabusertib (LY2603618) | Rabusertib (LY2603618) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID