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.
1234015-52-1Relevant articles and documents
CHK1/2 INHIBITORS FOR USE IN THE TREATMENT OF NEUROBLASTOMAS AND/OR SOFT TISSUE SARCOMAS
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Paragraph 23; 24, (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
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Page/Page column 29, (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.
