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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
Structure of SAR-260301

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

HIDE SMILES / InChI

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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
49.0 nM [IC50]
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

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 Sat Dec 16 09:03:53 UTC 2023
Edited
by admin
on Sat Dec 16 09:03:53 UTC 2023
Record UNII
33639WNC7Q
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SAR-260301
Common Name English
4(3H)-PYRIMIDINONE, 2-(2-((2S)-2,3-DIHYDRO-2-METHYL-1H-INDOL-1-YL)-2-OXOETHYL)-6-(4-MORPHOLINYL)-
Systematic Name English
SAR260301
Code English
Code System Code Type Description
ChEMBL
CHEMBL3545008
Created by admin on Sat Dec 16 09:03:53 UTC 2023 , Edited by admin on Sat Dec 16 09:03:53 UTC 2023
PRIMARY
CAS
1260612-13-2
Created by admin on Sat Dec 16 09:03:53 UTC 2023 , Edited by admin on Sat Dec 16 09:03:53 UTC 2023
PRIMARY
NCI_THESAURUS
C116882
Created by admin on Sat Dec 16 09:03:53 UTC 2023 , Edited by admin on Sat Dec 16 09:03:53 UTC 2023
PRIMARY
PUBCHEM
135565159
Created by admin on Sat Dec 16 09:03:53 UTC 2023 , Edited by admin on Sat Dec 16 09:03:53 UTC 2023
PRIMARY
FDA UNII
33639WNC7Q
Created by admin on Sat Dec 16 09:03:53 UTC 2023 , Edited by admin on Sat Dec 16 09:03:53 UTC 2023
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
IC50
Related Record Type Details
ACTIVE MOIETY