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
|
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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
|
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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。 |