| Identification | Back Directory | [Name]
PROTAC KRASG12C Degrader-LC-2 | [CAS]
2502156-03-6 | [Synonyms]
LC-2
PROTAC KRASG12C Degrader-LC-2 | [Molecular Formula]
C59H71ClFN11O7S | [MDL Number]
MFCD32857122 | [MOL File]
2502156-03-6.mol | [Molecular Weight]
1132.78 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
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