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JBJ-09-063

Chemical Structure : JBJ-09-063

CAS No.: 2820336-67-0

JBJ-09-063

Catalog No.: PC-73366Not For Human Use, Lab Use Only.

JBJ-09-063 is a potent, mutant-selective allosteric EGFR inhibitor against EGFR L858R, T790M and C797S mutations, with IC50 of <0.1 nM for recombinant EGFR L858R/T790M kinase domain.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JBJ-09-063 is a potent, mutant-selective allosteric EGFR inhibitor against EGFR L858R, T790M and C797S mutations, with IC50 of <0.1 nM for recombinant EGFR L858R/T790M kinase domain.
JBJ-09-063 demonstrated cell growth and EGFR phosphorylation inhibition in EGFRL858R/T790M and EGFRL858R/T790M/C797S Ba/F3 cells.
JBJ-09-063 exhibited in vivo anti-tumor activity against xenograft models harboring the EGFRL858R/T790M mutation, and EGFRL858R/T790M/C797S mutation.

Physicochemical Properties

M.Wt 556.656
Formula C31H29FN4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(5-(2-(1H-indol-3-yl)ethyl)-1,3,4-oxadiazol-2-yl)-N-(4-ethylbenzyl)-N-methylpropanamide

References

1. Ciric To, et al. Nat Cancer. 2022 Apr 14. doi: 10.1038/s43018-022-00351-8.

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