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Chemical Structure : SAR260301
CAS No.: 1260612-13-2
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 | Quantity |
|---|---|---|---|
| 5 mg | $138 | In stock | |
| 10 mg | $218 | In stock | |
| 25 mg | $368 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 354.41 | |
| Formula | C19H22N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-2-(2-(2-methylindolin-1-yl)-2-oxoethyl)-6-morpholinopyrimidin-4(1H)-one |
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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.
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