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目錄:MedChemExpress LLC>>生化試劑>> Sotorasib | MCE

Sotorasib | MCE
  • Sotorasib | MCE
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CAS 2296729-00-3 純度 99.94%
分子量 560.59 分子式 C??H??F?N?O?
供貨周期 現(xiàn)貨 規(guī)格 5 mg
貨號 HY-114277 應(yīng)用領(lǐng)域 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥
Sotorasib | MCESotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective <b>KRAS G12C</b> covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors<sup>[1]</sup><sup>[2]</sup>.

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Sotorasib

CAS No. : 2296729-00-3

產(chǎn)品活性:Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.

研究領(lǐng)域:GPCR/G Protein

作用靶點(diǎn):Ras

In Vitro: In cellular assays, Sotorasib (AMG-510) covalently modifies KRAS G12C and inhibits KRAS G12C signaling as measured by phosphorylation of ERK1/2 (p-ERK) in all KRAS p.G12C-mutant cell lines.
Sotorasib (AMG-510; 1-10 μM; 72 hours) also potently impairs cellular viability in both NCI-H358 and MIA PaCa-2 with IC50≈0.006 μM and 0.009 μM, respectively. Non-KRASG12C lines are insensitive to Sotorasib (IC50>7.5 μM).

In Vivo: In preclinical tumor models, Sotorasib (AMG-510) rapidly and irreversibly binds to KRAS G12C, providing durable suppression of the mitogen-activated protein kinase (MAPK) signaling pathway. Sotorasib (orally; once daily) is capable of inducing tumor regression in mouse models of KRAS G12C cancer.

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