1. PROTAC
    GPCR/G Protein
  2. PROTAC
    Ras
  3. LC-2

LC-2 

Cat. No.: HY-137516 Purity: >95.0%
Handling Instructions

LC-2 is a potent and first-in-class degrader of endogenous KRAS G12C with DC50 values between 0.25 and 0.76 μM. 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.

For research use only. We do not sell to patients.

LC-2 Chemical Structure

LC-2 Chemical Structure

CAS No. : 2502156-03-6

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1 mg USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
25 mg USD 4800 In-stock
Estimated Time of Arrival: December 31
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Description

LC-2 is a potent and first-in-class degrader of endogenous KRAS G12C with DC50 values 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].

IC50 & Target[1]

KRAS(G12C)

0.25-0.76 μM (DC50)

VHL

 

In Vitro

LC-2 induces degradation of endogenous KRASG12C in multiple KRAS mutant cancer cell (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23 and NCI-H358 cells) with DC50s between 0.25 and 0.76 μM. LC-2-induced KRASG12C degradation occurs via a bona fide PROTAC mechanism. MIA PaCa-2, NCI-H23, and SW1573 cells are treated with 2.5 μM of LC-2 for 6, 24, 48, and 72 h. In all three cell lines, maximal KRAS degradation occurred within 24 h and was sustained up to 72 h[1].
LC-2-induced (2.5 μM; 6-24 hours) KRAS G12C degradation modulates Erk signaling in homozygous and heterozygous KRAS mutant cell lines[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2 cells and NCI-H23 cells
Concentration: 2.5 μM
Incubation Time: 6-24 hours
Result: Inhibition and degradation of KRAS G12C decreases pErk signaling at 6 and 24 h in homozygous MIA PaCa-2 cells
Molecular Weight

1132.78

Formula

C₅₉H₇₁ClFN₁₁O₇S

CAS No.

2502156-03-6

SMILES

O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[[email protected]]3N(C[[email protected]@H](C3)O)C([[email protected]](C(C)(C)C)NC(CCOCCCN4[[email protected]@H](CCC4)COC5=NC(N6C[[email protected]@H](N(CC6)C(C(F)=C)=O)CC#N)=C7C(CN(CC7)C8=C9C(Cl)=CC=CC9=CC=C8)=N5)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (44.14 mM; ultrasonic and warming and heat to 80°C)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8828 mL 4.4139 mL 8.8278 mL
5 mM 0.1766 mL 0.8828 mL 1.7656 mL
10 mM 0.0883 mL 0.4414 mL 0.8828 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (1.84 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (1.84 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

LC-2LC2LC 2PROTACRasProteolysis-targeting chimeraundruggabledegraderphosphorylationNCI-H2030cellshomozygousheterozygousmutantcancerInhibitorinhibitorinhibit

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LC-2
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HY-137516
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