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)).
For research use only. We do not sell to patients.
- Formula: C66H79F2N13O6S
- Molecular Weight:1220.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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KRas G12D 4.2 nM (DC50) |
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.
Chemical Information
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Molecular Weight 1220.48
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)