Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H22N4O3 |
Molecular Weight | 354.403 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H]1CC2=C(C=CC=C2)N1C(=O)CC3=NC(=CC(=O)N3)N4CCOCC4
InChI
InChIKey=UAXHPOBBKRWJGA-ZDUSSCGKSA-N
InChI=1S/C19H22N4O3/c1-13-10-14-4-2-3-5-15(14)23(13)19(25)11-16-20-17(12-18(24)21-16)22-6-8-26-9-7-22/h2-5,12-13H,6-11H2,1H3,(H,20,21,24)/t13-/m0/s1
Molecular Formula | C19H22N4O3 |
Molecular Weight | 354.403 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Sanofi has developed SAR260301 as a selective inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) beta isoform with potential antineoplastic activity. It is known that the dysregulation of the PI3K/Akt/mTOR pathway is frequently found in solid tumors and contributes to increased tumor cell growth, tumor cell survival. SAR260301 participated in phase I clinical trials in patients with advanced solid tumors. It was found that the drug had an acceptable safety profile, but exposure sufficient to inhibit the PI3K pathway was unachievable because of rapid clearance, and clinical development was terminated.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3145 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24387221 |
49.0 nM [IC50] |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28976556
Twenty-one patients received treatment at doses ranging from 100 mg once daily to 440 mg/m2 twice daily. Dose-limiting toxicities included 1 episode of grade 3 pneumonitis (400 mg twice daily) and 1 grade 3 γ-glutamyltransferase increase (600 mg twice daily). The maximum tolerated dose was not reached.
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 22:27:48 GMT 2025
by
admin
on
Mon Mar 31 22:27:48 GMT 2025
|
Record UNII |
33639WNC7Q
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Common Name | English | ||
|
Preferred Name | English | ||
|
Systematic Name | English |
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
CHEMBL3545008
Created by
admin on Mon Mar 31 22:27:48 GMT 2025 , Edited by admin on Mon Mar 31 22:27:48 GMT 2025
|
PRIMARY | |||
|
DTXSID401352014
Created by
admin on Mon Mar 31 22:27:48 GMT 2025 , Edited by admin on Mon Mar 31 22:27:48 GMT 2025
|
PRIMARY | |||
|
1260612-13-2
Created by
admin on Mon Mar 31 22:27:48 GMT 2025 , Edited by admin on Mon Mar 31 22:27:48 GMT 2025
|
PRIMARY | |||
|
C116882
Created by
admin on Mon Mar 31 22:27:48 GMT 2025 , Edited by admin on Mon Mar 31 22:27:48 GMT 2025
|
PRIMARY | |||
|
135565159
Created by
admin on Mon Mar 31 22:27:48 GMT 2025 , Edited by admin on Mon Mar 31 22:27:48 GMT 2025
|
PRIMARY | |||
|
33639WNC7Q
Created by
admin on Mon Mar 31 22:27:48 GMT 2025 , Edited by admin on Mon Mar 31 22:27:48 GMT 2025
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
TARGET -> INHIBITOR |
IC50
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|