SAR260301 | CAS#1260612-13-2 | PI3Kbeta inhibitor

MedKoo Cat#: 206110 | Name: SAR260301

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SAR260301 is potent and selective Class I phosphatidylinositol-3-kinase (PI3K)β specific inhibitor. SAR260301 is being investigated for the treatment of PTEN-deficient tumors. SAR260301 displayed improved physicochemical and in vitro pharmacokinetic properties. SAR260301 demonstrated significant in vivo activity in a UACC-62 xenograft model in mice, warranting further preclinical investigation.

Chemical Structure

SAR260301

CAS#1260612-13-2

Theoretical Analysis

MedKoo Cat#: 206110

Name: SAR260301

CAS#: 1260612-13-2

Chemical Formula: C19H22N4O3

Exact Mass: 354.1692

Molecular Weight: 354.40

Elemental Analysis: C, 64.39; H, 6.26; N, 15.81; O, 13.54

Price and Availability

Size	Price	Availability
5mg	USD 350.00	2 Weeks
10mg	USD 650.00	2 Weeks
25mg	USD 1,050.00	2 Weeks

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Synonym

SAR260301; SAR260301; SAR 260301.

IUPAC/Chemical Name

(S)-2-(2-(2-methylindolin-1-yl)-2-oxoethyl)-6-morpholinopyrimidin-4(3H)-one

InChi Key

UAXHPOBBKRWJGA-ZDUSSCGKSA-N

InChi Code

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

SMILES Code

O=C1NC(CC(N2[C@@H](C)CC3=C2C=CC=C3)=O)=NC(N4CCOCC4)=C1

Appearance

white solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC50 of 23 nM.

In vitro activity:

In this study, SAR260301 demonstrated selectivity for the PI3Kβ isoform over other isoforms and a range of protein and lipid kinases. SAR260301 preferentially inhibited the PI3K pathway in PTEN-deficient human tumor models. SAR260301 exhibited synergistic anti-tumor activity when combined with BRAF or MEK inhibitors in melanoma tumor models. Reference: Mol Cancer Ther. 2016 Jul;15(7):1460-71. https://pubmed.ncbi.nlm.nih.gov/27196754/

In vivo activity:

In this first-in-human study, SAR260301, a potent PI3Kβ-selective inhibitor, was evaluated in patients with advanced solid tumors. While SAR260301 exhibited an acceptable safety profile, it was rapidly cleared from the body, and the exposure necessary to inhibit the PI3K pathway effectively was not maintained at the highest dose tested. These findings ultimately lead to the termination of SAR260301’s clinical development. Reference: Cancer. 2018 Jan 15;124(2):315-324. https://pubmed.ncbi.nlm.nih.gov/28976556/

Preparing Stock Solutions

The following data is based on the product molecular weight 354.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Bonnevaux H, Lemaitre O, Vincent L, Levit MN, Windenberger F, Halley F, Delorme C, Lengauer C, Garcia-Echeverria C, Virone-Oddos A. Concomitant Inhibition of PI3Kβ and BRAF or MEK in PTEN-Deficient/BRAF-Mutant Melanoma Treatment: Preclinical Assessment of SAR260301 Oral PI3Kβ-Selective Inhibitor. Mol Cancer Ther. 2016 Jul;15(7):1460-71. doi: 10.1158/1535-7163.MCT-15-0496. Epub 2016 May 12. PMID: 27196754. 2. Bédard PL, Davies MA, Kopetz S, Juric D, Shapiro GI, Luke JJ, Spreafico A, Wu B, Castell C, Gomez C, Cartot-Cotton S, Mazuir F, Dubar M, Micallef S, Demers B, Flaherty KT. First-in-human trial of the PI3Kβ-selective inhibitor SAR260301 in patients with advanced solid tumors. Cancer. 2018 Jan 15;124(2):315-324. doi: 10.1002/cncr.31044. Epub 2017 Oct 4. PMID: 28976556.

In vitro protocol:

In vivo protocol:

1. Bédard PL, Davies MA, Kopetz S, Juric D, Shapiro GI, Luke JJ, Spreafico A, Wu B, Castell C, Gomez C, Cartot-Cotton S, Mazuir F, Dubar M, Micallef S, Demers B, Flaherty KT. First-in-human trial of the PI3Kβ-selective inhibitor SAR260301 in patients with advanced solid tumors. Cancer. 2018 Jan 15;124(2):315-324. doi: 10.1002/cncr.31044. Epub 2017 Oct 4. PMID: 28976556.

1: Certal V, Carry JC, Halley F, Virone-Oddos A, Thompson F, Filoche-RommÃ© B, El-Ahmad Y, Karlsson A, Charrier V, Delorme C, Rak A, Abecassis PY, Amara C, Vincent L, Bonnevaux H, Nicolas JP, Mathieu M, Bertrand T, Marquette JP, Michot N, Benard T, Perrin MA, Lemaitre O, Guerif S, Perron S, Monget S, Gruss-Leleu F, Doerflinger G, Guizani H, Brollo M, Delbarre L, Bertin L, Richepin P, Loyau V, Garcia-Echeverria C, Lengauer C, Schio L. Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. J Med Chem. 2014 Feb 13;57(3):903-20. doi: 10.1021/jm401642q. Epub 2014 Jan 15. PubMed PMID: 24387221. 2: Bédard PL, Davies MA, Kopetz S, Juric D, Shapiro GI, Luke JJ, Spreafico A, Wu B, Castell C, Gomez C, Cartot-Cotton S, Mazuir F, Dubar M, Micallef S, Demers B, Flaherty KT. First-in-human trial of the PI3Kβ-selective inhibitor SAR260301 in patients with advanced solid tumors. Cancer. 2018 Jan 15;124(2):315-324. doi: 10.1002/cncr.31044. Epub 2017 Oct 4. PMID: 28976556.