XL-147
- Pilaralisib - SAR245408
- Soluble in DMSO
- MF: C25H25ClN6O4S
- MW: 541.02
Description
XL-147 is a potent, selective and orally bioavailable ATP-competitive small molecule inhibitor targeting pan-class I phosphatidylinositol 3 kinase (PI3K) family with IC50 values of 39, 383, 36 and 23 nM for p110 α, β, δ and γ isoforms, and is highly selective over mTOR (IC50 > 15000 nM), VPS34 (IC50 = 6975 nM), DNAPK (IC50 = 4750 nM).
More Information
| Parent CAS No. | 934526-89-3 |
|---|---|
| Chemical Name | 2-Amino-N-(3-(N-(3-(2-chloro-5-methoxyphenylamino)quinoxalin-2-yl)sulfamoyl)phenyl)-2-methylpropanamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C=C2N=C(NC3C=C(OC)C=CC=3Cl)C(NS(=O)(=O)C3C=C(NC(=O)C(C)(C)N)C=CC=3)=NC2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C25H25ClN6O4S/c1-25(2,27)24(33)28-15-7-6-8-17(13-15)37(34,35)32-23-22(29-19-9-4-5-10-20(19)30-23)31-21-14-16(36-3)11-12-18(21)26/h4-14H,27H2,1-3H3,(H,28,33)(H,29,31)(H,30,32) |
| InChiKey | QINPEPAQOBZPOF-UHFFFAOYSA-N |
| CID | 56599306 |
| Short Description | PI3K inhibitor |
References
- GI Shapiro et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors. Clin Cancer Res. 2014 Jan 1;20(1):233-45.
- CP Reynolds et al. Initial testing (stage 1) of the phosphatidylinositol 3' kinase inhibitor, SAR245408 (XL147) by the pediatric preclinical testing program. Pediatr Blood Cancer. 2013 May;60(5):791-8.
- L. Debussche, et al, Compositions comprising a pi3k inhibitor and a mek inhibitor and their use for treating cancer, WO2012078832A1, 2012.
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