MS 39
| Code | Size | Price |
|---|
| TAR-T41156-5mg | 5mg | £850.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
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Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20°C
Documents
Further Information
Bioactivity:
MS 39 is a highly effective, highly affinity and selective depressant of mutant epidermal growth factor receptor (EGFR) with high efficiency, high affinity and selectivity. MS 39, conjured by gefitinib to VHL ligand via a linker, effectively induced the degradation of mutant EGFR (DC50 values in HCC827(exon 19 del) and H3255 (L858R mutation) lung cancer cell lines were 5 nM and 3.3 nM, respectively). However, there was no significant effect in wild-type EGFR cell lines with concentrations up to 10 uM. MS 39 inhibited the proliferation of H3255 lung cancer cells in vitro and was bioavailable in mice after administration.
CAS:
2675490-92-1
Molecular Weight:
1056.72
Purity:
0.98
SMILES:
N(C=1C2=C(C=C(OC)C(OCCCN3CCN(C(CCCCCCCCCC(N[C@H](C(=O)N4[C@H](C(NCC5=CC=C(C=C5)C=6SC=NC6C)=O)C[C@@H](O)C4)[C@@](C)(C)C)=O)=O)CC3)=C2)N=CN1)C7=CC(Cl)=C(F)C=C7
References
Cheng et al (2020) Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders. J.Med.Chem. 63 1216 PMID: 31895569