SAR260301 |CAS:1260612-13-2 Probechem Biochemicals

Chemical Structure : SAR260301

CAS No.: 1260612-13-2

SAR260301 (SAR-260301;SAR 260301)

Catalog No.: PC-35880Not For Human Use, Lab Use Only.

SAR260301 (SAR-260301, SAR 260301) is a potent, selective, ATP-competitive PI3Kβ inhibitor with IC50 of 52 nM in TR-FRET assays, with littile to no actiivty against PI3Kα/γ/δ (IC50=1,869/>10,000/403 nM, respectively).

Packing	Price	Stock
5 mg	$138	In stock
10 mg	$218	In stock
25 mg	$368	In stock
50 mg		Get quote
100 mg		Get quote

Get Quotation Now

* Please select Quantity before adding items.

or Bulk Inquiry

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Biological Activity

SAR260301 (SAR-260301, SAR 260301) is a potent, selective, ATP-competitive PI3Kβ inhibitor with IC50 of 52 nM in TR-FRET assays, with littile to no actiivty against PI3Kα/γ/δ (IC50=1,869/>10,000/403 nM, respectively).
SAR260301 does not inhibit mTOR (IC50 >10 uM, the only other kinase inhibited by SAR260301 was VPS34 lipid kinase (IC50=180 nM) in a panel of >400 kinases.
SAR260301 inhibits AKT-Ser473 phosphorylation in cellular assays with IC50 of 32 nM, 26-fold, 88-fold, >94-fold, and >313-fold more potently than PI3Kδ, PI3Kα, PI3Kγ, and VPS34, respectively.
SAR260301 inhibits the PI3K pathway preferentially in PTEN-deficient cells, synergizes with MAPK pathway inhibitors to inhibit growth of PTEN-deficient and BRAF-mutant melanoma cells in vitro and in vivo.

Physicochemical Properties

M.Wt	354.41
Formula	C19H22N4O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-2-(2-(2-methylindolin-1-yl)-2-oxoethyl)-6-morpholinopyrimidin-4(1H)-one

References

1. Bonnevaux H, et al. Mol Cancer Ther. 2016 Jul;15(7):1460-71.

2. Certal V, et al. J Med Chem. 2014 Feb 13;57(3):903-20.

3. Bédard PL, et al. Cancer. 2018 Jan 15;124(2):315-324.

SAR260301 (SAR-260301;SAR 260301)

Biological Activity

Physicochemical Properties

References

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

Get Quote

* Indicates a Required FieldYour information is safe with us.