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1234015-52-1

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1234015-52-1 Usage

Description

LY 2606368 is a checkpoint kinase 1 (Chk1) inhibitor with a Ki value of 0.9 nM against the purified target and IC50 values of <13 nM in a viability study of multiple colorectal cancer cell lines. It is a novel chemopotentiating agent that causes double-stranded DNA breakage while simultaneously removing the protection of the DNA damage checkpoints, making it a promising drug candidate for the treatment of cancer and tumor growth inhibition.

Uses

Used in Oncology:
LY 2606368 is used as a chemopotentiating agent for the treatment of cancer and tumor growth inhibition. It inhibits the Chk1 enzyme, leading to double-strand DNA breakage in cells, causing an excessive cell damage burden and subsequent cell death. This makes it a potential therapeutic agent for various types of cancer.
Used in Colorectal Cancer Treatment:
In colorectal cancer cell lines, LY 2606368 has shown an IC50 value of <13 nM, indicating its effectiveness in inhibiting the viability of these cancer cells. It can be used as a targeted therapy for colorectal cancer treatment.
Used in Gastric Cancer Treatment:
LY 2606368, at 25 nM, has been shown to significantly induce apoptosis and inhibit colony formation in AGS and MKN1 gastric cancer cells. It can be used as a potential therapeutic agent for gastric cancer treatment.
Used in Enhancing Chemotherapy Efficacy:
In vitro, LY 2606368 inhibits the doxorubicin-activated G2/M checkpoint in p53-deficient HeLa cells with an EC50 value of 9 nM. This suggests that it can be used in combination with chemotherapy drugs to enhance their efficacy and overcome drug resistance in cancer treatment.

references

[1] wu w, bi c, bence a k, et al. antitumor activity of chk1 inhibitor ly2606368 as a single agent in sw1990 human pancreas orthotopic tumor model. cancer research, 2012, 72(8 supplement): 1776.[2] lainchbury m, matthews t p, mchardy t, et al. discovery of 3-alkoxyamino-5-(pyridin-2-ylamino) pyrazine-2-carbonitriles as selective, orally bioavailable chk1 inhibitors. journal of medicinal chemistry, 2012, 55(22): 10229-10240.[3] mcneely s c, burke t f, durlandbusbice s, et al. abstract a108: ly2606368, a second generation chk1 inhibitor, inhibits growth of ovarian carcinoma xenografts either as monotherapy or in combination with standard-of-care agents. molecular cancer therapeutics, 2011, 10(supplement 1): a108.

Check Digit Verification of cas no

The CAS Registry Mumber 1234015-52-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,3,4,0,1 and 5 respectively; the second part has 2 digits, 5 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1234015-52:
(9*1)+(8*2)+(7*3)+(6*4)+(5*0)+(4*1)+(3*5)+(2*5)+(1*2)=101
101 % 10 = 1
So 1234015-52-1 is a valid CAS Registry Number.

1234015-52-1SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 13, 2017

Revision Date: Aug 13, 2017

1.Identification

1.1 GHS Product identifier

Product name 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile

1.2 Other means of identification

Product number -
Other names LY 2606368

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1234015-52-1 SDS

1234015-52-1Relevant articles and documents

CHK1/2 INHIBITORS FOR USE IN THE TREATMENT OF NEUROBLASTOMAS AND/OR SOFT TISSUE SARCOMAS

-

, (2017/02/09)

The present invention provides 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-lH- pyrazol-3-ylamino)pyrazine~2~carbonitrile and pharmaceutically acceptable salts and solvates thereof, that is capable of inhibiting CHK1 and is useful in the treatment of neuroblastomas and/or soft tissue sarcomas.

COMPOUNDS USEFUL FOR INHIBITING CHK1

-

Page/Page column 20-21, (2010/08/04)

The present invention provides an aminopyrazole compound, or a pharmaceutically acceptable salt thereof or a solvate of the salt, that inhibits Chk1 and is useful in the treatment of cancer.

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