LY2603618

Catalog No.S2626

LY2603618 is a selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. Phase 2.

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LY2603618 Chemical Structure

LY2603618 Chemical Structure
Molecular Weight: 436.3

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Product Description

Biological Activity

Description LY2603618 is a selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. Phase 2.
Targets Chk1 [1]
(Cell-free assay)
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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
BT474MWnLbY5ie2ViYYPzZZk>M3fITFEh|ryPM2HHWGROW09?MmH4bY5pcWKrdIOgVE1EUEtzIHzleoVtew>?M1\DZ|I{QTF5M{e4
MCF7MVPLbY5ie2ViYYPzZZk>NWX2cXljOSEQvF2=MonySG1UVw>?NUDkNVN6cW6qaXLpeJMhWC2FSFuxJIxmfmWucx?=NX24cnJXOjN7MUezO|g>
HelaNVz2TYpLU2mwYYPlJIF{e2G7MlzJN|MxOCCwTR?=M{T1dmROW09?NVz2b2Q5cW6qaXLpeJMhS2itMTDhZ5Rqfmm2eR?=NYPVN5ByOjRzMUSxNlQ>
Calu6MmryT4lv[XOnIHHzd4F6M3HlWFM{ODBibl2=NI\BdpZFVVORMWrpcohq[mm2czDDbIsyKGGldHn2bZR6M4PPWVI1OTF2MUK0
A549NVXLUpdRTnWwY4Tpc44h[XO|YYm=MYf+NVAh|ryPNGfNe2pFVVORM3zmbolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S=NW\LeJp5OjR7MkiyNFU>
H1299NGjrc5RHfW6ldHnvckBie3OjeR?=Moq2glExKM7:TR?=NIj6UXJFVVORMonKbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?=MXOyOFkzQDJyNR?=
A549MmnCSpVv[3Srb36gZZN{[Xl?M{nXRp4zOCEQvF2=MmK2SG1UVw>?MnvhZYN1cX[jdHXzJGRPSSCmYX3h[4Uhe2Wwc3;yJItqdmG|ZYO=MWqyOFkzQDJyNR?=
H1299NIrwZm1HfW6ldHnvckBie3OjeR?=MUP+NlAh|ryPMYLEUXNQMYjhZ5RqfmG2ZYOgSG5CKGSjbXHn[UB{\W6|b4Kgb4lv[XOncx?=M2nq[VI1QTJ6MkC1
A549NETBeHdCeG:ydH;zbZMh[XO|YYm=MU\+NlAh|ryPM3nGc2ROW09?M12yfolv\HWlZYOgZZBweHSxc3nzNUfp[Y1WOjR7MkiyNFU>
H1299M4q2[GFxd3C2b4Ppd{Bie3OjeR?=Ml7JglIxKM7:TR?=NYTtRWZVTE2VTx?=NIPuTZhqdmS3Y3XzJIFxd3C2b4Ppdy=>MX:yOFkzQDJyNR?=
A549M{\Mb2N6fG:6aXPpeJkh[XO|YYm=MVv+NlAh|ryPMVXEUXNQNG\FVFZqdmS3Y3XzJIF2fG:yaHHnfS=>M{\SVVI1QTJ6MkC1
H1299NGfXNJVEgXSxeHnjbZR6KGG|c3H5NX7vWHZbhjJyIN88US=>Mle2SG1UVw>?M4\3[olv\HWlZYOgZZV1d3CqYXf5Mn72NlQ6Ojh{MEW=
A549NV7wOINkTnWwY4Tpc44h[XO|YYm=MX3+NlAh|ryPM2HRN2ROW09?MkLJbY5kemWjc3XzJGpPUyCjbnSgdFM5KE2DUFugdIhwe3Cqb4L5cIF1cW:wNIP1ZmozPDl{OEKwOS=>
H1299NFLLcmtHfW6ldHnvckBie3OjeR?=MknxglIxKM7:TR?=NYG2NYk6TE2VTx?=M4W3bolv[3KnYYPld{BLVktiYX7kJJA{QCCPQWDLJJBpd3OyaH;yfYxifGmxbh?=M3jSTlI1QTJ6MkC1

... Click to View More Cell Line Experimental Data

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Dai Y, et al. Clin Cancer Res, 2010, 16(2), 376-383.

[2] Emiliano Calvo1, et al. Mol Cancer Ther, 2011, A94.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01358968 Completed Cancer Eli Lilly and Company June 2011 Phase 1
NCT01341457 Active, not recruiting Solid Tumors Eli Lilly and Company May 2011 Phase 1
NCT01139775 Completed Non Small Cell Lung Cancer Eli Lilly and Company February 2011 Phase 1|Phase 2
NCT01296568 Completed Advanced Cancer Eli Lilly and Company February 2011 Phase 1
NCT00988858 Completed Non Small Cell Lung Cancer Eli Lilly and Company November 2009 Phase 2

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Chemical Information

Download LY2603618 SDF
Molecular Weight (MW) 436.3
Formula

C18H22BrN5O3

CAS No. 911222-45-2
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms IC-83
Solubility (25°C) * In vitro DMSO 13 mg/mL (29.79 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG400+0.5% Tween80+5% Propylene glycol 30mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name (S)-1-(5-bromo-4-methyl-2-(morpholin-2-ylmethoxy)phenyl)-3-(5-methylpyrazin-2-yl)urea

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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