SAR-260301

Investigational

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 Search

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28976556 | https://www.ncbi.nlm.nih.gov/pubmed/27196754

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
PI3-kinase p110-beta subunit 31 Target ID: CHEMBL3145 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24387221	Inhibitor 8297		49.0 nM [IC50]

PubMed

Title	Date	PubMed

Patents

Sample Use Guides

In Vivo Use Guide

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 GMT 2023` Edited by `admin` on `Sat Dec 16 09:03:53 GMT 2023`
Record UNII	33639WNC7Q
Record Status	`Validated (UNII)`
Record Version

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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