MS243
MS243 is a potent KRASG12D PROTAC degrader with a DC50 of 4.2 nM. MS243 promotes the proximity between KRASG12D and the VHL E3 ubiquitin ligase, drives the ubiquitination and proteasomal degradation of KRASG12D, and inhibits the proliferation of cancer cells harboring KRASG12D. MS243 can be used in the research of KRASG12D-carrying cancers, such as colon cancer and pancreatic cancer.
(Pink: KRas G12D ligand (HY-181733); Blue: VHL ligand (HY-170348); Black: linker (HY-W895436)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C66H79F2N13O6S
- 分子量:1220.48
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
KRas G12D 4.2 nM (DC50) |
体外実験
MS243 (0-10 μM; 7 d) inhibits the proliferation of GP2 and AsPC-1 cells, with GI50 values of 84 nM and 283 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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分子量 1220.48
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分子式 C66H79F2N13O6S
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SMILES
FC(C=C1)=C(C#C)C(C1=CC(O)=C2)=C2C3=NC=C4C(N=C(OC[C@H]5N(CCC(NCCCCCCCCC6=CN([C@H](C(N7[C@H](C(N[C@@H](C)C8=CC=C(C9=C(C)N=CS9)C=C8)=O)C[C@@H](O)C7)=O)C(C)(C)C)N=N6)=O)CCC5)N=C4N%10C[C@H]%11N[C@H](CC%11)C%10)=C3F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MS243 関連分類
HY-181728 関連分類
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