KRAS G12C PROTAC LC-2

Chemical Structure : KRAS G12C PROTAC LC-2

CAS No.: 2502156-03-6

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货号: PC-26457Not For Human Use, Lab Use Only.

KRAS G12C PROTAC LC-2 is a potent, selective VHL-Recruiting PROTAC degrader of KRASG12C with DC50 of 0.59 uM and Dmax of 80% in NCI-H2030 cells.

规格	价格	库存
1 mg	￥1880	In stock
5 mg	￥3980	In stock
10 mg		Get quote
25 mg		Get quote

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生物&药学活性

KRAS G12C PROTAC LC-2 is a potent, selective VHL-Recruiting PROTAC degrader of KRASG12C with DC50 of 0.59 uM and Dmax of 80% in NCI-H2030 cells.
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 has DC50 values between 0.25 and 0.76 μM as well as Dmax values ranging from ∼75-90% in 5 different KRASG12C cell lines.
LC-2 can degrade mutant KRAS in both homozygous and heterozygous cell lines with varying sensitivities to MRTX849.
LC-2 modulates Erk signaling in homozygous and heterozygous KRASG12C cell lines.

物理化学性质&存储条件

分子量	1132.80
分子式	C59H71ClFN11O7S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

参考文献

1. Bond MJ, et al. ACS Cent Sci. 2020 Aug 26;6(8):1367-1375.