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PROTAC KRASG12C Degrader-LC-2 |
| CAS No.: |
2502156-03-6 |
| 分子式： |
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| 分子量： |
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| 備注： |
中文名稱PROTACKRASG12CDegrader-LC-2中文同義詞(2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-氯萘-1-基)-4-((S)-3-(氰基甲基)-4-(2-氟丙烯?；?哌嗪-1-基)-5,6,7,8-四氫吡啶并[3,4-D]嘧啶-2-基)氧基)甲基)吡咯烷-1-基)丙氧基)丙酰胺基)-3,3-二甲基丁?；?-4-羥基-N-(4-(4-甲基噻唑-5-基)芐基)吡咯烷-2-甲酰胺;LC2|||PROTACKRASG12CDEGRADER-LC-2|||LC2英文名稱PROTACKRASG12CDegrader-LC-2英文同義詞PROTACKRASG12CDegrader-LC-2;LC-2;(2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-Chloronaphthalen-1-yl)-4-((S)-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)propoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;(2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-Chloronaphthalen-1-yl)-4-((S)-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)propoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-mCAS號2502156-03-6分子式C59H71ClFN11O7S分子量1132.78EINECS號相關(guān)類別Mol文件MolFile結(jié)構(gòu)式PROTACKRASG12CDegrader-LC-2性質(zhì)密度1.297±0.06g/cm3(PredChemicalbookicted)儲存條件Storeat-20°C溶解度DMSO：50mg/mL（44.14mM；超聲加熱并加熱至80°C）形態(tài)固體酸度系數(shù)(pKa)14.07±0.40(Predicted)顏色米白色至棕色PROTACKRASG12CDegrader-LC-2用途與合成方法生物活性LC-2是首創(chuàng)的內(nèi)源性KRASG12C的PROTAC降解劑，DC50在0.25和0.76μM之間。LC-2是一種PROTAC，與MRTX849共價結(jié)合KRASG12C并招募E3連接酶VHL，誘導(dǎo)KRASG12C快速持續(xù)降解，導(dǎo)致純合和雜合子KRASG12C細(xì)胞系MAPK信號的抑制。靶點(diǎn)KRAS(G12C)0.25-0.76μM(DC50)VHL體外研究LC-2inducesdegradationofendogenousKRASG12CinmultipleKRASmutantcancercell(NCI-H2030,MIAPaCa-2,SW1573,NCI-H23andNCI-H358cells)withDC50sbetween0.25and0.76μM.LC-2-inducedKRASG12CdegradationoccursviaabonafidePROTACmechanism.MIAPaCa-2,NCI-H23,andSW1573cellsaretreatedwith2.5μMofLC-2for6,24,48,and72h.Inallthreecelllines,maximalKRASdegradationoccurredwithin24handwassustainedupto72h.LC-2-induced(2.5μM;6-24hours)KRASG12CdegradationmodulatesErksignalinginhomozygousandheterozygousKRASmutantcelllines.WesternBlotAnalysisCellLine:MIAPaCa-2cellsandNCI-H23cellsConcentration:2.5μMIncubationTime:6-24hoursResult:InhibitionanddegradationofKRASG12CdecreasespErksignalingat6and24hinhomozygousMIAPaCa-2cells |
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金經(jīng)理 |
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430000 |
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