MRTX1133

製品コードE1051 バッチE105104

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C33H31F3N6O2
分子量 600.63 CAS No. 2621928-55-8
Solubility (25°C)* 体外 DMSO 100 mg/mL (166.49 mM)
 
 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS.
in vitro

MRTX1133 not only possesses single-digit nM potency in a cellular proliferation assay, but also demonstrates tumor regressions in the Panc 04.03 xenograft model.
in vivo

MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS [2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株
濃度 <2 nM (IC50)
反応時間
実験の流れ
動物実験 動物モデル CD-1 mice
投薬量 30 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Defining the KRAS- and ERK-dependent transcriptome in KRAS-mutant cancers [ Science, 2024, 384(6700):eadk0775] PubMed: 38843331
Determining the ERK-regulated phosphoproteome driving KRAS-mutant cancer [ Science, 2024, 384(6700):eadk0850] PubMed: 38843329
Macroautophagy/autophagy promotes resistance to KRASG12D-targeted therapy through glutathione synthesis [ Cancer Lett, 2024, 604:217258] PubMed: 39276914
Dual Inhibition of KRASG12D and Pan-ERBB Is Synergistic in Pancreatic Ductal Adenocarcinoma [ Cancer Res, 2023, 83(18):3001-3012] PubMed: 37378556
Feedback activation of EGFR/wild-type RAS signaling axis limits KRASG12D inhibitor efficacy in KRASG12D-mutated colorectal cancer [ Oncogene, 2023, 42(20):1620-1633] PubMed: 37020035
Feedback activation of EGFR/wild-type RAS signaling axis limits KRASG12D inhibitor efficacy in KRASG12D-mutated colorectal cancer [ Oncogene, 2023, 10.1038/s41388-023-02676-9 10.3322/caac.21660 10.1001/jama.2021.6021 10.1038/nrdp.2015.65 10.1038/s41575-019-0189-8 10.1038/nature11252 10.1038/s41392] PubMed: 37020035
Cetuximab Enhances the Efficacy of MRTX1133, a Novel KRASG12D Inhibitor, in Colorectal Cancer Treatment [ Anticancer Res, 2023, 43(10):4341-4348] PubMed: 37772552
Cetuximab Enhances the Efficacy of MRTX1133, a Novel KRASG12D Inhibitor, in Colorectal Cancer Treatment [ Anticancer Res, 2023, 43(10):4341-4348] PubMed: 37772552

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。