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XL147 Catalog No : 51506

Chemical Information

Product NameXL147
Iupac Chemical NameN-[3-(2,1,3-Benzothiadiazol-5-ylamino)-2-quinoxalinyl]-4-methylbenzenesulfonamide 
SynonymsSAR245408;pilaralisib 
Molecular FormulaC21H16N6O2S2 
Molecular Weight448.52 
SmileO=S(C1=CC=C(C)C=C1)(NC2=NC3=CC=CC=C3N=C2NC4=CC5=NSN=C5C=C4)=O
InChiKeyMQMKRQLTIWPEDM-UHFFFAOYSA-N
InChiInChI=1S/C21H16N6O2S2/c1-13-6-9-15(10-7-13)31(28,29)27-21-20(23-16-4-2-3-5-17(16)24-21)22-14-8-11-18-19(12-14)26-30-25-18/h2-12H,1H3,(H,22,23)(H,24,27)
Cas956958-53-5

Technical Data

Appearancecrystalline solid 
Purity98% 
SolubilitySoluble in DMSO 
Storage3 years -20ºCpowder 
Shipping ConditionShipped under ambient temperature 
Quality control

Description

XL147 (SAR245408) is a potent and highly selective inhibitor of class I PI3Ks (, , , and ). Moreover, broad kinase selectivity profiling of >130 protein kinases revealed that XL147 is highly selective for class I PI3Ks over other kinases. In cellular assays, XL147 inhibits the formation of PIP3 in the membrane, and inhibits phosphorylation of AKT, p70S6K, and S6 in multiple tumor cell lines with diverse genetic alterations affecting the PI3K pathway. In a panel of tumor cell lines, XL147 inhibits proliferation with a wide range of potencies, with evidence of an impact of genotype on sensitivity. In mouse xenograft models, oral administration of XL147 results in dose-dependent inhibition of phosphorylation of AKT, p70S6K, and S6 with a duration of action of at least 24 hours. Repeat-dose administration of XL147 results in significant tumor growth inhibition in multiple human xenograft models in nude mice. Administration of XL147 in combination with chemotherapeutic agents results in antitumor activity in xenograft models that is enhanced over that observed with the corresponding single agents.

Reference:
1. Mol Cancer Ther. 2015 Apr;14(4):931-40. doi: 10.1158/1535-7163.MCT-14-0833. Epub 2015 Jan 30.
2.Clin Cancer Res. 2014 Jan 1;20(1):233-45. doi: 10.1158/1078-0432.CCR-13-1777. Epub 2013 Oct 28.

 

 

 

Chemical Structure

51506 - XL147 | CAS 956958-53-5

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