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JBJ-09-063

CAT: 0931-T63939-01Size: 25 mgDry Ice: NoHazardous: No
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CAT#:0931-T63939-01Size:25 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
2820336-67-0
Target
Others, EGFR
Related Pathways
Others, Tyrosine Kinase/Adaptors, Angiogenesis, JAK/STAT signaling
Bioactivity
JBJ-09-063 is a mutant-selective allosteric inhibitor of the epidermal growth factor receptor (EGFR), with potent inhibitory activity demonstrated by half-maximal inhibitory concentrations (IC50s) of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S. This compound effectively decreases phosphorylation of EGFR, Akt, and ERK1/2, showing efficacy in both EGFR tyrosine kinase inhibitor (TKI) -sensitive and resistant models. JBJ-09-063 holds potential for research into EGFR-mutant lung cancer.
Smiles
C(C(NC1=NC=CS1)=O)(N2C(=O)C=3C(C2)=CC=C(C3)C4=CC=C(C=C4)C5CCN(C)CC5)C6=C(O)C=CC(F)=C6
Molecular Formula
C31H29FN4O3S
Molecular Weight
556.65
Shipping Conditions
Ice Packs
Storage Temperature
-20°C