LY2603618

Bezeichnung:LY2603618

CAS-Nr911222-45-2

Englisch Name:LY2603618

CBNumberCB92538917

SummenformelC18H22BrN5O3

Molgewicht436.3

MOL-Datei911222-45-2.mol

LY2603618 physikalisch-chemischer Eigenschaften

Siedepunkt	503.1±50.0 °C(Predicted)
Dichte	1.461
storage temp.	-20°C
Löslichkeit	Soluble in DMSO (up to 10 mg/ml)
Aggregatzustand	solid
pka	12.06±0.70(Predicted)
Farbe	Off-white
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Sicherheit

HS Code

29349990

LY2603618 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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
Verwenden
LY2603618 is a selective Chk1 inhibitor that can treat idiopathic pulmonary fibrosis.
Definition
ChEBI: 1-[5-bromo-4-methyl-2-[[(2S)-2-morpholinyl]methoxy]phenyl]-3-(5-methyl-2-pyrazinyl)urea is a member of ureas.
Biologische Aktivität
Rabusertib (LY2603618, IC-83) is a highly selective inhibitor of Chk1 with potential antitumor activity in cell-free assays, IC50=7 nM, potency against Chk1 versus multiple other protein kinases tested 100 times higher. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
in vivo
experiment was carried out to determine the combining effect of ly2603618 with other chemotherapy[2] . in mice xenograft model that inculated with calu-6 lung cancer cell, combining administration of injected gemcitabine 150 mg/kg and orally uptake ly2603618 (200 mg/kg) resulted in increased dna damage of tumour, as was demonstrated by a 2-fold increase in chk1 s345 phosphorylation in comparison with mice treated with gemcitabine alone[2].
Lager
Store at -20°C
Einzelnachweise
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

LY2603618 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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