2772612-96-9
Chemical Structure
MS9449
- CAS No.: 2772612-96-9
- Formula:C60H76ClFN10O8S
- Molecular Weight:1151.82
IUPAC Name: (3S,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bS)-5a,5b,8,8,11a,13b-hexamethyl-3-(prop-1-en-2-yl)icosahydro-1H-cyclopenta[a]chrysen-9-ol
InChIKey: VDUPETHSNLCFNB-HHHFUCLFSA-N
SMILES: O=C([C@H]1N(C([C@@H](C2=CC(C)=NO2)C(C)C)=O)C[C@H](O)C1)N[C@H](C3=CC=C(C4=C(C)N=CS4)C=C3)CC(NCCCCCCCCCCC(N5CCN(CCCOC6=CC7=C(NC8=CC=C(F)C(Cl)=C8)N=CN=C7C=C6OC)CC5)=O)=O
Biological Activity: MS9449 is a potent PROTAC EGFR degrader, with Kd values of 17 nM and 10 nM for wild-type EGFR and mutant EGFRL858R, respectively, and a DC50 of 7.1 nM for EGFRDel19. MS9449 effectively induces the degradation of mutant EGFR through the ubiquitin-proteasome system (UPS) and the autophagy-lysosome pathway. MS9449 exhibits anticancer activity against non-small cell lung cancer. MS9449 can be applied in related research on non-small cell lung cancer[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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MS9449 | 98.95% | MS9449 is a potent PROTAC EGFR degrader, with Kd values of 17 nM and 10 nM for wild-type EGFR and mutant EGFRL858R, respectively, and a DC50 of 7.1 nM for EGFRDel19. MS9449 effectively induces the degradation of mutant EGFR through the ubiquitin-proteasome system (UPS) and the autophagy-lysosome pathway. MS9449 exhibits anticancer activity against non-small cell lung cancer. MS9449 can be applied in related research on non-small cell lung cancer. | ||||||||||||||||||||
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References
- [1]. Yu X, et al. Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras. Journal of medicinal chemistry. 2022 Jun 23;65(12):8416-8443. [Content Brief]
- [2]. Shen J, et al. EGFR degraders in non-small-cell lung cancer: Breakthrough and unresolved issue. Chemical biology & drug design. 2024 Apr;103(4):e14517.
