BAY-1125976

Research use only, not for human use.

A potent and highly selective, allosteric AKT1/2 inhibitor with IC50 of 5.2/18 nM at 10 uM ATP.

A potent and highly selective, allosteric AKT1/2 inhibitor with IC50 of 5.2/18 nM at 10 uM ATP; binds to active AKT1 with Kd of 2.7 nM and inactive AKT1 with Kd of 1.3 nM. displays >86-fold less potent against AKT3; inhibits the phosphorylation of AKT1 at T308 and S473 (IC50=0.9 and 1.1 nM, respectively), PRAS40 at T246 and 4EBP1 at T70; targets tumors displaying PI3K/AKT/mTOR pathway activation, inhibits cell proliferation in a broad panel of human cancer cell lines, particularly in breast and prostate cancer cell lines expressing estrogen or androgen receptors; exhibits strong in vivo patient-derived xenograft models. Solid Tumors Phase 1 Clinical

BAY1125976

Cytoskeleton/Cell Adhesion Molecules

Akt

Akt

Cancer

Solid Tumors

1402608-02-9

383.45

C23H21N5O

>98% (HPLC)

DMSO: 10.33 mg/mL

C1CC(C1)(C2=CC=C(C=C2)C3=C(N4C(=N3)C=CC(=N4)C(=O)N)C5=CC=CC=C5)N

Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-

(-20℃)

With Ice Pack

≥ 2 years