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BLU9931

Catalog No.: 60303
Cas No.: 1538604-68-0
Purity : 98% 
60303 - BLU9931 | CAS 1538604-68-0

Catalog number : 60303

CAS number : 1538604-68-0

分子式 : C26H22Cl2N4O3 

分子量 : 509.38 

Iupac 化学名称 : N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide 

Smile : C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O

InChiKey : TXEBNKKOLVBTFK-UHFFFAOYSA-N

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分子式C26H22Cl2N4O3 
分子量509.38 
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 as non-hazardous chemical. 
SmileC=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O
InChiKeyTXEBNKKOLVBTFK-UHFFFAOYSA-N
InChiInChI=1S/C26H22Cl2N4O3/c1-5-21(33)30-18-8-6-7-14(2)25(18)32-26-29-13-16-11-15(9-10-17(16)31-26)22-23(27)19(34-3)12-20(35-4)24(22)28/h5-13H,1H2,2-4H3,(H,30,33)(H,29,31,32)
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BLU9931 is a potent and irreversible small-molecule inhibitor of FGFR4, as a targeted therapy to treat patients with HCC whose tumors have an activated FGFR4 signaling pathway. BLU9931 is exquisitely selective for FGFR4 versus other FGFR family members and all other kinases. BLU9931 shows remarkable antitumor activity in mice bearing an HCC tumor xenograft that overexpresses FGF19 due to amplification as well as a liver tumor xenograft that overexpresses FGF19 mRNA but lacks FGF19 amplification. Approximately one third of patients with HCC whose tumors express FGF19 together with FGFR4 and its coreceptor klotho (KLB) could potentially respond to treatment with an FGFR4 inhibitor. These findings are the first demonstration of a therapeutic strategy that targets a subset of patients with HCC.
Cancer Discov; 5(4); 424-37. ©2015 AACR. See related commentary by Packer and Pollock, p. 355 This article is highlighted in the In This Issue feature, p. 333.

©2015 American Association for Cancer Research.

 

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