Contact us: +91 9550333722 040 - 40102781
Structured search
India
Choose your country
Different countries will display different contents
Try our best to find the right business for you.
My chemicalbook

Welcome back!

HomeProduct name listLY2603618

LY2603618

LY2603618 Structural

What is LY2603618?

Description

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

The Uses of LY2603618

LY2603618 is a selective Chk1 inhibitor that can treat idiopathic pulmonary fibrosis.

What are the applications of Application

LY2603618 is a selective Chk1 inhibitor

Definition

ChEBI: 1-[5-bromo-4-methyl-2-[[(2S)-2-morpholinyl]methoxy]phenyl]-3-(5-methyl-2-pyrazinyl)urea is a member of ureas.

Biological Activity

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].

storage

Store at -20°C

References

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

Properties of LY2603618

Boiling point: 503.1±50.0 °C(Predicted)
Density  1.461
storage temp.  -20°C
solubility  Soluble in DMSO (up to 10 mg/ml)
form  solid
pka 12.06±0.70(Predicted)
color  Off-white
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.

Safety information for LY2603618

Computed Descriptors for LY2603618

Related products of tetrahydrofuran

You may like

  • LY2603618 CAS 911222-45-2
    LY2603618 CAS 911222-45-2
    911222-45-2
    View Details
  • 1-Methyl-6-oxo-1,6-dihydropyridazine-3-carbonitrile 98%
    1-Methyl-6-oxo-1,6-dihydropyridazine-3-carbonitrile 98%
    99903-60-3
    View Details
  • 1823368-42-8 98%
    1823368-42-8 98%
    1823368-42-8
    View Details
  • 2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%
    2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%
    1307449-08-6
    View Details
  • Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%
    Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%
    25408-95-1
    View Details
  • 2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%
    2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%
    1805639-70-6
    View Details
  • 1784294-80-9 98%
    1784294-80-9 98%
    1784294-80-9
    View Details
  • Lithium Clavulanate
    Lithium Clavulanate
    61177-44-4
    View Details
Statement: All products displayed on this website are only used for non medical purposes such as industrial applications or scientific research, and cannot be used for clinical diagnosis or treatment of humans or animals. They are not medicinal or edible.