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LC-2 - CAS 2502156-03-6

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LC-2 is a PROTAC® Degrader of KRAS G12C containing a von-Hippel-Lindau (VHL) E3 ligase ligand and the covalently bound inhibitor MRTX849 with a DC50 value between 0.25 and 0.76 μM, which can induce rapid and sustained degradation of KRAS G12C.

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Molecular Formula

C59H71ClFN11O7S

Molecular Weight

1132.78

LC-2

- Specification
  - Purity
    
    ≥95%
    
    Solubility
    
    Soluble in DMSO
    
    Appearance
    
    White Solid
    
    Storage
    
    Store at 2-8°C for short term (days to weeks) or -20°C for long term (months to years)
    
    Shipping
    
    Room temperature in continental US; may vary elsewhere.
    
    IUPAC Name
    
    (2S,4R)-1-[(2S)-2-[3-[3-[(2S)-2-[[7-(8-chloronaphthalen-1-yl)-4-[(3S)-3-(cyanomethyl)-4-(2-fluoroprop-2-enoyl)piperazin-1-yl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-2-yl]oxymethyl]pyrrolidin-1-yl]propoxy]propanoylamino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
    
    Synonyms
    
    (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
- Properties
  - Density
    
    1.297±0.06 g/cm3
    
    InChI Key
    
    ZCGQZLKPUVGCBQ-HLMPTVQRSA-N
    
    InChI
    
    InChI=1S/C59H71ClFN11O7S/c1-37(61)56(76)71-27-26-70(32-42(71)19-22-62)54-45-20-25-69(48-14-7-11-40-10-6-13-46(60)51(40)48)34-47(45)65-58(67-54)79-35-43-12-8-23-68(43)24-9-28-78-29-21-50(74)66-53(59(3,4)5)57(77)72-33-44(73)30-49(72)55(75)63-31-39-15-17-41(18-16-39)52-38(2)64-36-80-52/h6-7,10-11,13-18,36,42-44,49,53,73H,1,8-9,12,19-21,23-35H2,2-5H3,(H,63,75)(H,66,74)/t42-,43-,44+,49-,53+/m0/s1
    
    Canonical SMILES
    
    N#CCC1N(C(=O)C(F)=C)CCN(C2=NC(=NC3=C2CCN(C4=CC=CC=5C=CC=C(Cl)C54)C3)OCC6N(CCCOCCC(=O)NC(C(=O)N7CC(O)CC7C(=O)NCC=8C=CC(=CC8)C=9SC=NC9C)C(C)(C)C)CCC6)C1
    
    Pub Chem ID
    
    154727765
- Reference Reading
  - 1. Targeted degradation of oncogenic KRASG12C by VHL-recruiting PROTACs.
    
    Bond, M.J., Chu, L., Nalawansha, D.A., Li, K. and Crews, C.M., 2020. ACS central science, 6(8), pp.1367-1375.
    
    KRAS is mutated in ~20% of human cancers and is one of the most sought-after targets for pharmacological modulation, despite having historically been considered "undruggable." The discovery of potent covalent inhibitors of the KRASG12C mutant in recent years has sparked a new wave of interest in small molecules targeting KRAS. While these inhibitors have shown promise in the clinic, we wanted to explore PROTAC-mediated degradation as a complementary strategy to modulate mutant KRAS. Herein, we report the development of LC-2, the first PROTAC capable of degrading endogenous KRASG12C. LC-2 covalently binds KRASG12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRASG12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRASG12C cell lines. LC-2 demonstrates that PROTAC-mediated degradation is a viable option for attenuating oncogenic KRAS levels and downstream signaling in cancer cells.
- Preparing Stock Solutions
  - ConcentrationVolumeMass 1 mg 5 mg 10 mg
    
    1 mM 0.88 mL 4.41 mL 8.83 mL
    
    5 mM 0.18 mL 0.88 mL 1.77 mL
    
    10 mM 0.09 mL 0.44 mL 0.88 mL
    
    50 mM 0.02 mL 0.09 mL 0.18 mL

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	0.88 mL	4.41 mL	8.83 mL
5 mM	0.18 mL	0.88 mL	1.77 mL
10 mM	0.09 mL	0.44 mL	0.88 mL
50 mM	0.02 mL	0.09 mL	0.18 mL

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