akt(wt)

Borussertib is a first-in-class covalent-allosteric inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

FLT3-IN-37 (Compound 6z) is a potent inhibitor of FLT3-ITD, with IC50 values of 1.5 nM for FLT3-ITD and 3.4 nM for TEL-VEGFR2. It exhibits high selectivity for FLT3 wild-type (WT) and c-Kit. The compound inhibits FLT3 phosphorylation and downregulates the expression of p-Akt, p-STAT5, and p-ERK. By causing cell cycle arrest and inducing apoptosis, FLT3-IN-37 demonstrates anti-leukemic activity, making it suitable for research into acute myeloid leukemia (AML).

EGFRT790M/L858R-IN-2 is a potent, selective inhibitor of EGFRT790M/L858R, exhibiting IC50 values of 3.5 nM for EGFRT790M/L858R and 1290 nM for EGFR WT. This compound effectively decreases the expression of p-EGFR, P-AKT, P-ERK1/2, and induces apoptosis as well as cell cycle arrest in the G1 phase, demonstrating anti-cancer activity [1].