CCT241161 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. CCT241161 blocked growth of BRAF-mutant and NRAS-mutant melanoma cells, inhibiting MEK–ERK, in vitro and in vivo. CCT241161 also prevented growth of xenografts derived from patient tumours with acquired or intrinsic resistance to BRAF and MEK inhibitors. BRAF and MEK inhibitors are effective in BRAF mutant melanoma, but most patients eventually relapse with acquired resistance, and others present intrinsic resistance to these drugs.

CAS 1163719-91-2 MFCD263719912

化学结构图

1163719-91-2
SMILES: CSc1cc(Oc2ccnc3[nH]c(=O)cnc23)ccc1NC(=O)Nc1cc(C(C)(C)C)nn1-c1ccccc1

化学属性

Mol. Weight541.62
Appearance Solid powder
SolubilitySoluble in DMSO, not in water

别名和识别编码

Chemical NameCCT241161 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. CCT241161 blocked growth of BRAF-mutant and NRAS-mutant melanoma cells, inhibiting MEK–ERK, in vitro and in vivo. CCT241161 also prevented growth of xenografts derived from patient tumours with acquired or intrinsic resistance to BRAF and MEK inhibitors. BRAF and MEK inhibitors are effective in BRAF mutant melanoma, but most patients eventually relapse with acquired resistance, and others present intrinsic resistance to these drugs.
FormulaC28H27N7O3S
Synonym CCT241161; CCT-241161; CCT 241161.
IUPAC Name1-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl)-3-(2-(methylthio)-4-((3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yl)oxy)phenyl)urea
InChIKeyDPMYVVGAYAPQNS-UHFFFAOYSA-N
InChIInChI=1S/C28H27N7O3S/c1-28(2,3)22-15-23(35(34-22)17-8-6-5-7-9-17)32-27(37)31-19-11-10-18(14-21(19)39-4)38-20-12-13-29-26-25(20)30-16-24(36)33-26/h5-16H,1-4H3,(H,29,33,36)(H2,31,32,37)
Canonical SMILESCSC1=CC(OC2=C3C(NC(C=N3)=O)=NC=C2)=CC=C1NC(NC4=CC(C(C)(C)C)=NN4C5=CC=CC=C5)=O
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产品应用

  • CCT241161 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. CCT241161 blocked growth of BRAF-mutant and NRAS-mutant melanoma cells, inhibiting MEK–ERK, in vitro and in vivo. CCT241161 also prevented growth of xenografts derived from patient tumours with acquired or intrinsic resistance to BRAF and MEK inhibitors. BRAF and MEK inhibitors are effective in BRAF mutant melanoma, but most patients eventually relapse with acquired resistance, and others present intrinsic resistance to these drugs.

安全信息

Storage condition Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

系列性分类


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