Bioactivity | KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf[1]. | ||||||||||||
Invitro | KRAS inhibitor-3 (0-5 μM) 降低稳定表达 KRASG12D 的 BHK 细胞中的 p-ERK 水平[1]。KRAS inhibitor-3 (1 μM,2 小时) 破坏 KRAS 与 Raf 的相互作用[1]。KRAS inhibitor-3 (0-5 μM) 降低表达 KRASG12D 和 KRASG12V 的 BHK 细胞中的 p-ERK 和 p-cRaf 水平[1]。 Western Blot Analysis[1] Cell Line: | ||||||||||||
Name | KRAS inhibitor-3 | ||||||||||||
CAS | 900897-56-5 | ||||||||||||
Formula | C25H27N5O | ||||||||||||
Molar Mass | 413.51 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. McCarthy MJ, et al. Discovery of High-Affinity Noncovalent Allosteric KRAS Inhibitors That Disrupt Effector Binding. ACS Omega. 2019 Feb 28;4(2):2921-2930. |