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)).
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- Formule: C66H79F2N13O6S
- Masse moléculaire:1220.48
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Stockage:
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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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
KRas G12D 4.2 nM (DC50) |
In Vitro
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.
Chemical Information
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Masse moléculaire 1220.48
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS243 Related Classifications
HY-181728 Related Classifications
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