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Cat. No. Product Name Target Signaling Pathways
T8369 Adagrasib

MRTX849

Ras GPCR/G Protein; MAPK
Adagrasib (MRTX849) 是一种 KRAS G12C 共价抑制剂,具有口服活性和选择性。Adagrasib 与 KRAS G12C 非活性构象的 GDP 状态结合,抑制 KRAS 及其下游信号的传导。Adagrasib 对 KRAS G12C 突变肿瘤具有抑制活性。
T40189 MRTX849 acid

MRTX849 acid

MRTX849 acid, a derivative of MRTX849, is employed in the synthesis of PROTAC LC-2. LC-2, a potent and pioneering PROTAC, exhibits the ability to efficiently degrade endogenous KRAS G12C with DC50 values ranging between 0.25 and 0.76 μM.
T40156 MRTX849 analog 24

MRTX849 analog 24

MRTX849 analog 24 is an alkyne-containing click probe analogue of the MRTX849 inhibitor for KRAS G12C. It is specifically designed for studying the functionality of MRTX849.
T40190 MRTX849 ethoxypropanoic acid

MRTX849 ethoxypropanoic acid is a compound that contains a ligand for KRAS G12C and a PROTAC linker. It is commonly employed in the synthesis of PROTAC LC-2, which is a highly effective and innovative PROTAC. LC-2 has been proven to degrade endogenous KRAS G12C with remarkable potency, exhibiting DC50 values ranging from 0.25 to 0.76 μM.
T36256 LC-2

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

PROTACs PROTAC
LC-2 (PROTAC KRASG12C Degrader-LC-2) 是一种新型基于von Hippel-Lindau的内源性 KRAS G12C 的 PROTAC 降解剂,DC50 在 0.25 和 0.76 μM 之间。LC-2 是一种与 MRTX849 共价结合 KRAS G12C 并招募 E3 连接酶 VH的 PROTAC,诱导 KRAS G12C 快速持续降解。LC-2 对纯合和杂合子 KRAS G12C 细胞系 MAPK 信号有抑制作用。
T74336 YF135

YF135为一种效能高的KRASG12CPROTAC,能可逆地促使共价结合。该化合物采用KRAS G12C inhibitor 48(compound 6d)作为配体,并以MRTX849搭配VHL配体作为框架进行设计与合成。通过E3连接酶VHL介导的蛋白酶体途径,YF135显著诱导KRASG12C的降解并可逆地降低ERK磷酸化水平。

化合物

Adagrasib
Cat.No: T8369
Synonym: MRTX849
Target: Ras
MRTX849 acid
Cat.No: T40189
Synonym: MRTX849 acid
Target:
MRTX849 analog 24
Cat.No: T40156
Synonym: MRTX849 analog 24
Target:
MRTX849 ethoxypropanoic acid
Cat.No: T40190
Synonym:
Target:
LC-2
Cat.No: T36256
Synonym: LC 2,PROTAC KRASG12C Degrader-LC-2,LC2
Target: PROTACs
YF135
Cat.No: T74336
Synonym:
Target:
TargetMol Loading
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