AMG-510

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Sotorasib (AMG-510) 是一种一流的、口服生物利用的、选择性 KRAS G12C 共价抑制剂。 Sotorasib 通过将 KRAS G12C 锁定在不活跃的 GDP 结合状态来不可逆地抑制 KRAS G12C。

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.(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.

Cell Viability Assay Cell Line:NCI-H358 and MIA PaCa-2 cells Concentration:1-10 μM Incubation Time:72 hours Result:Potently impaired cellular viability in both NCI-H358 and MIA PaCa-2 (IC50≈0.006 μM and 0.009 μM respectively).

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MAPK/ERK Signaling

Ras

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2296729-00-3

560.59

C??H??F?N?O?

>98% (HPLC)

DMSO : 50 mg/mL (89.19 mM; Need ultrasonic);H2O : 33.33 mg/mL (59.46 mM; ultrasonic and adjust pH to 11 with NaOH)

O=C(C=C)N1C[C@H](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=C2C=C(F)C(C5=C(O)C=CC=C5F)=N4)=O)CC1

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(-20℃)

With Ice Pack

≥ 2 years