Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C19H19ClN6O |
| Molecular Weight | 382.847 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H](CN(C)C)OC1=NC(NC2=NC=C3C(Cl)=CC=CC3=C2)=CN=C1C#N
InChI
InChIKey=SRBJWIBAMIKCMV-GFCCVEGCSA-N
InChI=1S/C19H19ClN6O/c1-12(11-26(2)3)27-19-16(8-21)22-10-18(25-19)24-17-7-13-5-4-6-15(20)14(13)9-23-17/h4-7,9-10,12H,11H2,1-3H3,(H,23,24,25)/t12-/m1/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/20053762Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/22981708
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20053762
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/22981708
SAR-020106 is an ATP-competitive, potent, and selective inhibitor of CHK1, a serine/threonine kinase associated with DNA damage-linked S and G(2)-M checkpoint control. SAR-020106 is a potent radio- and chemosensitizer in tumor cell lines and in vivo xenograft models.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20053762
Curator's Comment: 2010
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL4630 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20053762 |
13.3 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Optimising measles virus-guided radiovirotherapy with external beam radiotherapy and specific checkpoint kinase 1 inhibition. | 2013-07 |
|
| Targeted radiosensitization by the Chk1 inhibitor SAR-020106. | 2013-03-15 |
|
| Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. | 2011-12-22 |
|
| The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106. | 2010-01 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20053762
mice: 40 mg/kg
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20053762
SAR-020106 abrogates an etoposide-induced G2 arrest with an IC50 of 55 nM in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion.
| Name | Type | Language | ||
|---|---|---|---|---|
|
Preferred Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
44203948
Created by
admin on Wed Apr 02 20:19:25 GMT 2025 , Edited by admin on Wed Apr 02 20:19:25 GMT 2025
|
PRIMARY | |||
|
43GTC52NG2
Created by
admin on Wed Apr 02 20:19:25 GMT 2025 , Edited by admin on Wed Apr 02 20:19:25 GMT 2025
|
PRIMARY | |||
|
1184843-57-9
Created by
admin on Wed Apr 02 20:19:25 GMT 2025 , Edited by admin on Wed Apr 02 20:19:25 GMT 2025
|
PRIMARY | |||
|
DTXSID601351967
Created by
admin on Wed Apr 02 20:19:25 GMT 2025 , Edited by admin on Wed Apr 02 20:19:25 GMT 2025
|
PRIMARY |
SUBSTANCE RECORD