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XL147

Catalog No.: 51506
Cas No.: 956958-53-5
Purity : 98% 
51506 - XL147 | CAS 956958-53-5

Catalog number : 51506

CAS number : 956958-53-5

分子式 : C21H16N6O2S2 

分子量 : 448.52 

Iupac 化学名称 : N-[3-(2,1,3-Benzothiadiazol-5-ylamino)-2-quinoxalinyl]-4-methylbenzenesulfonamide 

Smile : O=S(C1=CC=C(C)C=C1)(NC2=NC3=CC=CC=C3N=C2NC4=CC5=NSN=C5C=C4)=O

InChiKey : MQMKRQLTIWPEDM-UHFFFAOYSA-N

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同义词SAR245408;pilaralisib 
英文同义词SAR245408;pilaralisib 
分子式C21H16N6O2S2 
分子量448.52 
外观crystalline solid 
纯度98% 
可溶性Soluble in DMSO 
存储3 years -20ºCpowder 
运输条件Shipped under ambient temperature 
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)
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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.

 

 

 

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