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| | PROTAC KRASG12C Degrader-LC-2 Basic information |
| Product Name: | PROTAC KRASG12C Degrader-LC-2 | | Synonyms: | PROTAC KRASG12C Degrader-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-m;L-Prolinamide, N-[3-[3-[(2S)-2-[[[7-(8-chloro-1-naphthalenyl)-4-[(3S)-3-(cyanomethyl)-4-(2-fluoro-1-oxo-2-propen-1-yl)-1-piperazinyl]-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl]oxy]methyl]-1-pyrrolidinyl]propoxy]-1-oxopropyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-;LC-2 ，S6996;LC-2 | | CAS: | 2502156-03-6 | | MF: | C59H71ClFN11O7S | | MW: | 1132.78 | | EINECS: | | | Product Categories: | | | Mol File: | 2502156-03-6.mol |  |
| | PROTAC KRASG12C Degrader-LC-2 Chemical Properties |
| density | 1.297±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: 50 mg/mL (44.14 mM; ultrasonic and warming and heat to 80°C) | | form | Solid | | pka | 14.07±0.40(Predicted) | | color | Off-white to brown |
| | PROTAC KRASG12C Degrader-LC-2 Usage And Synthesis |
| Description | LC-2 is a von Hippel-Lindau-based PROTAC which can degrade endogenous KRAS G12C. It covalently binds KRAS G12C with a MARTX849 warhead and recruits the E3 ligase VHL which degrades the KRAS G12C and suppresses MAPK signaling in homozygous and heterzygous KRAS G12C cell lines. | | Uses | LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM[1]. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines[2]. | | IC 50 | KRAS(G12C): 0.25-0.76 μM (DC50); VHL | | storage | Store at -20°C | | References | [1] De Vita E, et al. The Missing Link between (Un)druggable and Degradable KRAS. ACS Cent Sci. 2020;6(8):1281-1284. DOI:10.1021/acscentsci.0c00920
[2] Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6(8):1367-1375. DOI:10.1021/acscentsci.0c00411 |
| | PROTAC KRASG12C Degrader-LC-2 Preparation Products And Raw materials |
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