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LC-2

Catalog No. T36256 CAS 2502156-03-6

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

LC-2 (PROTAC KRASG12C Degrader-LC-2) is a novel von Hippel-Lindau-based PROTAC degrader of endogenous KRAS G12C with a DC50 between 0.25 and 0.76 μM.LC-2 is a PROTAC that covalently binds KRAS G12C with MRTX849 and recruits the E3 ligase, VH, to induce a rapid and sustained degradation of KRAS G12C. LC-2 inhibits MAPK signaling in pure and heterozygous KRAS G12C cell lines.

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LC-2, CAS 2502156-03-6

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1 mg	In stock	$ 263.00
5 mg	In stock	$ 659.00
10 mg	In stock	$ 939.00
25 mg	In stock	$ 1,380.00
50 mg	5 days	Inquiry

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Description	LC-2 (PROTAC KRASG12C Degrader-LC-2) is a novel von Hippel-Lindau-based PROTAC degrader of endogenous KRAS G12C with a DC50 between 0.25 and 0.76 μM.LC-2 is a PROTAC that covalently binds KRAS G12C with MRTX849 and recruits the E3 ligase, VH, to induce a rapid and sustained degradation of KRAS G12C. LC-2 inhibits MAPK signaling in pure and heterozygous KRAS G12C cell lines.
Targets&IC50	KRas (G12C):0.25-0.76 μM (DC50)
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]. Western Blot Analysis[1]Cell Line:MIA PaCa-2 cells and NCI-H23 cells

Synonyms	LC 2, PROTAC KRASG12C Degrader-LC-2, LC2
Molecular Weight	1132.78
Formula	C59H71ClFN11O7S
CAS No.	2502156-03-6

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (26.48 mM), Sonication and heating are recommended.

References and Literature

1. De Vita E, et al. The Missing Link between (Un)druggable and Degradable KRAS. ACS Cent Sci. 2020;6(8):1281-1284. 2. Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6(8):1367-1375.

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Keywords

LC-2 2502156-03-6 PROTAC PROTACs LC 2 PROTAC KRASG12C Degrader-LC-2 LC2 inhibitor inhibit

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