BLU-667 (Pralsetinib) CAS No.:2097132-94-8
Chemical Structure: BLU-667
CAS Nr.: 2097132-94-8
Hauj lwm lawm
Chemical Structure: BLU-667
CAS Nr.: 2097132-94-8
BLU-667 (Pralsetinib; BLU667)
Catalog No.Qauv: URK-V764Tsuas yog siv rau Lab.
BLU{{0}} (Pralsetinib, BLU667) yog lub zog muaj zog, xaiv, tiam tom ntej RET inhibitor nrog IC50 ntawm 0.3-0.4 nM rau WT RET, RET mutants V804L, V804M, M918T thiab CCDC6-RET fusion.
Kev ua lom lom
BLU{{0}} (Pralsetinib, BLU667) yog lub zog muaj zog, xaiv, tiam tom ntej RET inhibitor nrog IC50 ntawm 0.3-0.4 nM rau WT RET, RET mutants V804L, V804M, M918T thiab CCDC6-RET fusion.
BLU-667 displays 8- to 28-fold more potent against WT RET than cabozantinib, vandetanib, and RXDX-105; shows 88-fold selectivity over VEGFR-2, >100-fold ntau xaiv rau RET tshaj 96 feem pua ntawm kinases hauv ib lub vaj huam sib luag ntawm 371 kinases.
BLU-667 inhibits RET autophosphorylation nrog cellular IC50 ntawm 5 nM, tsawg kawg 10 npaug ntau dua li cabozantinib, vandetanib, thiab RXDX-105. BLU-667 inhibits phosphorylation ntawm RET, SHC, thiab ERK1/2 nyob rau hauv ib lub vaj huam sib luag ntawm RET-tsav cell kab ntawm<10 nM, suppresses proliferation of KIF5B-RET Ba/F3 cells harboring V804L, V804M, or V804E variants as potently as WT RET.
BLU-667 qhia txog kev tiv thaiv qog nqaij hlav ntawm ntau hom RET-tsav hauv vivo qauv.
Physicochemical Properties
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M.Wt |
533.612 |
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Formula |
C27H32FN9O2 |
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CAS Nr. |
2097132-94-8 |
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Cia |
Hmoov hmoov -20 degree 3 xyoos; 4 degree 2 xyoos |
Hauv Solvent -80 degree 6 Lub Hlis -20 degree 1 Lub Hlis |
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Solubility |
100 mM hauv DMSO |
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Tshuaj npe |
(1s,4R)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-}yl)pyridin{10} }yl)ethyl)-1-methoxy-4-(4-methyl-6-}((5-methyl-1}H-pyrazol-3-}yl )amino)pyrimidin{19}}yl)cyclohexane-1-carboxamide |
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Cov ntaub ntawv
1. Subbiah V, et al. Cancer Discov. 2018 Apr 15. pii: CD-18-0338.
2. Piotrowska Z, et al. Cancer Discov. 2018 Dec; 8(12):1529-1539.
URK-V764_COAURK-V764_SDSURK-V764_TDSNco tseg: Tag nrho cov khoom ntawm Ureiko tsuas yog siv rau kev tshawb fawb tshawb fawb lossis kev tshaj tawm daim ntawv pov thawj tshuaj, thiab peb tsis muab cov khoom thiab cov kev pabcuam rau kev siv tus kheej!
Cim npe nrov: blu-667 (pralsetinib) cas no.:2097132-94-8
Xa kev nug
Koj Tseem Yuav Zoo Li
