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MRTX849 acid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MRTX849 acid图片
CAS NO:2561529-96-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
MRTX849 acid 可用来合成PROTAC LC-2。LC-2 是一种有效且首创的 PROTAC,能够降解内源性 KRAS G12C (DC50,介于0.25 和0.76 μM之间)。
生物活性

MRTX849 acid, a derivative of MRTX849, can be used in the synthesis ofPROTACLC-2 (HY-137516). LC-2 is a potent and first-in-classPROTACcapable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM)[1][2].

IC50& Target[1]

KRas G12C

 

体外研究
(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 abona fidePROTAC 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].

分子量

662.15

Formula

C34H37ClFN7O4

CAS 号

2561529-96-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.