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Product Details

LY2603618 | Potent and selective Chk1 inhibitor

LY2603618 (911222-45-2)  is a potent (IC50 = 7nM) and selective (>1000x over Chk2) Checkpoint kinase 1 (Chk1) inhibitor.1 Chk1 is an important regulator of the DNA damage response – combination treatment of LY2603618 with other chemotherapeutic agents significantly increased tumor growth inhibition when compared to chemotherapeutic alone.2,3,4 LY2603618 caused a dramatic suppression of cell growth in MCF-7 and MDA-MB-231 human breast cancer cells via Chk1 inhibition induced upregulation of replication stress caused by oncogenes.5

References/Citations

1) King et al. (2014), Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor; Invest. New Drugs, 32 213
2) Calvo et al. (2014), Preclinical analyses and phase I evaluation of LY2603618 administered in combination with pemetrexed and cisplatin in patients with advanced cancer; Invest. New Drugs, 32 955
3) Calvo et al. (2016), Phase I Study of CHK1 Inhibitor LY2603618 in Combination with Gemcitabine in Patients with Solid Tumors; Oncology, 91 251
4) Zhao et al. (2016), Inhibition of CHK1 enhances cell death induced by the Bcl-1-selective inhibitor ABT-199 in acute myeloid leukemia cells; Oncotarget, 7 34785
5) Zhang et al. (2016), Targeting radioresistant breast cancer cells by single agent CHK1 inhibitor via enhancing replication stress; Oncotarget, 7 34688

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Catalog#  10-4123-0005

$75.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
911222-45-2
Catalog Number:
10-4123
Activity:
Potent and selective Chk1 inhibitor
Chemical Name:
N-[5-bromo-4-methyl-2-[(2S)-2-morpholinylmethoxy]phenyl]-N'-(5-methyl-2-pyrazinyl)urea
Alternate Names:
Rabusertib
Molecular Weight:
436.30
Molecular Formula:
C18H22BrN5O3
Solubility:
Soluble in DMSO (up to 10 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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