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. Author manuscript; available in PMC: 2023 Jul 15.
Published in final edited form as: Bioorg Med Chem Lett. 2022 Apr 1;68:128718. doi: 10.1016/j.bmcl.2022.128718

Table 1.

EGFRL858R/T790M enzyme and Ba/F3 cell data, and mouse in vivo PK (3 mg/kg IV, 20 mg/kg PO) for isoindolinones

Cpd Enzyme
IC50 (nM)		 Cell IC50
(μM)		 Cell IC50
(μM)+cetux		 IV Cl
(mL/min/kg)		 IV T1/2
(hr)		 Vss
(L/kg)		 F
%		 Auc 8hr
(ng*hr/mL)
1, EAI045 3.3 > 10.0 0.221 - - - - -
2, JBJ-04-125-02 0.3 0.61 0.021 5.0 3.0 0.6 3 2523
3 0.3 0.49 0.006 10.3 2.8 1.8 2 1351
4, JBJ-09-063 0.1 0.05 0.006 15.7 2.3 2.5 15 2398
5 0.2 1.07 0.020 13.9 3.1 2.4 4 1002