LY2603618 | Potent and selective Chk1 inhibitor

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 from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$50.00
25 mg$195.00

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

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 from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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