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LC-2

SKU: orb1693902

Description

LC-2 is a VHL-based PROTAC that covalently engages endogenous KRAS G12C via MRTX849 to induce its targeted degradation (DC50 ~0.25-0.76 µM) and suppress MAPK signaling. This tool compound is used in vitro for oncology research, particularly in studying KRAS-driven cancers and targeted protein degradation.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Images & Validation

Key Properties

CAS Number2502156-03-6
MW1132.78
Purity98.00%
FormulaC59H71ClFN11O7S
SMILESCc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCOCCCN2CCC[C@H]2COc2nc3CN(CCc3c(n2)N2CCN([C@@H](CC#N)C2)C(=O)C(F)=C)c2cccc3cccc(Cl)c23)C(C)(C)C)cc1
TargetKras,Ras,PROTACs
SolubilityDMSO:30 mg/mL (26.48 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (1.77 mM)

Bioactivity

Target IC50
KRas (G12C):0.25-0.76 μM (DC50)
In Vitro
LC-2 induces the degradation of endogenous KRASG12C in multiple KRAS mutant cancer cell lines (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23, and NCI-H358) with DC50 values ranging from 0.25 to 0.76 μM via a bona fide PROTAC mechanism. In MIA PaCa-2, NCI-H23, and SW1573 cells treated with 2.5 μM of LC-2 for up to 72 hours, maximal KRAS degradation occurred within 24 hours and was sustained for 72 hours, modulating Erk signaling in homozygous and heterozygous KRAS mutant cell lines, as confirmed by Western Blot Analysis of MIA PaCa-2 and NCI-H23 cells.

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

LC 2, LC2, LC-2, PROTAC, PROTAC KRASG12C Degrader-LC-2

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Key Properties

No computed properties available.

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Protocol Information

LC-2 (orb1693902)

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1 mg
$ 310.00
5 mg
$ 700.00