PROTAC KRASG12C Degrader-LC-2
PROTAC KRASG12C Degrader-LC-2 Basic information
- Product Name:
- PROTAC KRASG12C Degrader-LC-2
- Synonyms:
-
- PROTAC KRASG12C Degrader-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-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
- CAS:
- 2502156-03-6
- MF:
- C59H71ClFN11O7S
- MW:
- 1132.78
- 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-2Supplier
- Tel
- 400-164-7117 13681763483
- product02@bidepharm.com
- Tel
- 18-086626237 18086626237
- 2693528373@qq.com
- Tel
- 177-54423994 17754423994
- 2853530910@QQ.com
- Tel
- 13504435624
- 1927928688@qq.com
- Tel
- 020-82000279 18988941452
- YN_research@163.com