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LC-2

CAT: 0804-HY-137516-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-137516-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
CAS Number
2502156-03-6
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
PROTACs; Ras
Type
Reference compound
Related Pathways
GPCR/G Protein; MAPK/ERK Pathway; PROTAC
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/protac-krasg12c-degrader-lc-2.html
Purity
98.48
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@H](C(C)(C)C)NC(CCOCCCN4[C@@H](CCC4)COC5=NC(N6C[C@@H](N(CC6)C(C(F)=C)=O)CC#N)=C7C(CN(CC7)C8=C9C(Cl)=CC=CC9=CC=C8)=N5)=O)=O
Molecular Formula
C59H71ClFN11O7S
Molecular Weight
1132.78
Precautions
H302, H315, H319, H335
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
K-Ras; von Hippel-Lindau (VHL)